49 results on '"Tourwé, D."'
Search Results
2. Synergetic effects of DNA demethylation and histone deacetylase inhibition in primary rat hepatocytes.
- Author
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Fraczek JE, Vinken M, Tourwé D, Vanhaecke T, and Rogiers V
- Subjects
- Albumins metabolism, Animals, Azacitidine analogs & derivatives, Azacitidine pharmacology, Biomarkers metabolism, CDC2 Protein Kinase metabolism, Cell Cycle drug effects, Cell Proliferation drug effects, Cell Shape drug effects, Cells, Cultured, DNA biosynthesis, Decitabine, Drug Synergism, Epidermal Growth Factor pharmacology, Hepatocytes cytology, Hepatocytes enzymology, Hydroxamic Acids pharmacology, Rats, DNA Methylation drug effects, Hepatocytes drug effects, Hepatocytes metabolism, Histone Deacetylase Inhibitors pharmacology
- Abstract
Both, DNA methylation and histone deacetylation play a crucial role in cancer development by silencing the expression of specific tumour suppressor genes. Several studies describe the use of combinations of DNA methyltransferase inhibitors (DNMT-i) and histone deacetylase inhibitors (HDAC-i) as an improved strategy to treat neoplasms. However, no information is available concerning their biological impact on healthy, non-malignant cells, including hepatocytes. Therefore, the effects of the combination of the DNMT-i decitabine (DAC) with the HDAC-i 6-[(4-pyrrolidine-1-ylbenzoyl) amino] hexanoic acid hydroxamate (AN-8) on cell proliferation and differentiation were examined in primary rat hepatocyte cultures. We found that, upon simultaneous exposure of the cells to both compounds, a synergetic anti-proliferative outcome was achieved. This inhibition of DNA synthesis was accompanied by a reduced expression of cyclin-dependent kinase 1 (cdk1), a key cell cycle marker that controls the S/G2/M transition. Compared to exposure of the cells to each agent separately, the combination of lower concentrations of both DAC and AN-8 promoted the maintenance of the differentiated phenotype of the cells as a function of culture time. The functionality of the hepatocytes was evidenced by an increased expression of the phase I biotransformation enzyme cytochrome P 450 (CYP) 1A1 and albumin secretion capacity when both agents were used in combination.
- Published
- 2012
- Full Text
- View/download PDF
3. Screening of amide analogues of Trichostatin A in cultures of primary rat hepatocytes: search for potent and safe HDAC inhibitors.
- Author
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Fraczek J, Deleu S, Lukaszuk A, Doktorova T, Tourwé D, Geerts A, Vanhaecke T, Vanderkerken K, and Rogiers V
- Subjects
- Amides chemistry, Amides toxicity, Animals, Cells, Cultured, Drug Evaluation, Preclinical, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Enzyme Inhibitors toxicity, Hepatocytes metabolism, Histone Deacetylase 1, Hydroxamic Acids chemistry, Hydroxamic Acids toxicity, Male, Rats, Rats, Sprague-Dawley, Amides pharmacology, Hepatocytes drug effects, Histone Deacetylase Inhibitors, Hydroxamic Acids pharmacology
- Abstract
The vast majority of preclinical studies of HDAC inhibitors (HDAC-I) focus on the drug-target (cancer) cell interaction, whereas little attention is paid to the effects on non-target healthy cells, which could provide decisive information to eliminate potential cytotoxic compounds at a very early stage during drug development. In the current study we used cultures of primary rat hepatocytes as a read out system to select for the most potent HDAC-I in the group of structural analogues of an archetypal HDAC-I, namely Trichostatin A. This kind of approach allowed selecting compounds with high biological activity and with no apparent toxicity towards cultured hepatocytes.
- Published
- 2009
- Full Text
- View/download PDF
4. Development and Preclinical Evaluation of 99m Tc- and 186 Re-Labeled NOTA and NODAGA Bioconjugates Demonstrating Matched Pair Targeting of GRPR-Expressing Tumors.
- Author
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Makris G, Bandari RP, Kuchuk M, Jurisson SS, Smith CJ, and Hennkens HM
- Subjects
- Animals, Inhibitory Concentration 50, Ligands, Mice, SCID, Peptides chemistry, Single Photon Emission Computed Tomography Computed Tomography, Tissue Distribution, Whole Body Imaging, Mice, Acetates chemistry, Heterocyclic Compounds, 1-Ring chemistry, Neoplasms diagnostic imaging, Radioisotopes chemistry, Receptors, Bombesin metabolism, Rhenium chemistry, Technetium chemistry
- Abstract
Purpose: The goal of this work was to develop hydrophilic gastrin-releasing peptide receptor (GRPR)-targeting complexes of the general formula fac-[M(CO)
3 (L)]+ [M =nat Re,99m Tc,186 Re; L: NOTA for 1, NODAGA for 2] conjugated to a powerful GRPR peptide antagonist (D Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 ) via a 6-aminohexanoic acid linker., Procedures: Metallated-peptides were prepared employing the [M(OH2 )3 (CO)3 ]+ [M = Re,99m Tc,186 Re] precursors. Re-1/2 complexes were characterized with HR-MS. IC50 studies were performed for peptides 1/2 and their respective Re-1/2 complexes in a binding assay utilizing GRPR-expressing human PC-3 prostate cancer cells and [125 I]I-Tyr4 -BBN as the competing ligand. The99m Tc/186 Re-complexes were identified by HPLC co-injection with their Re-analogues. All tracers were challenged in vitro at 37 °C against cysteine/histidine (phosphate-buffered saline 10 mM, pH 7.4) and rat serum. Biodistribution and micro-SPECT/CT imaging of [99m Tc]Tc-1/2 and [186 Re]Re-2 were performed in PC-3 tumor-bearing ICR SCID mice., Results: High in vitro receptor affinity (IC50 2-3 nM) was demonstrated for all compounds. The99m Tc/186 Re-tracers were found to be hydrophilic (log D7.4 ≤ - 1.35) and highly stable. Biodistribution in PC-3 xenografted mice revealed good tumor uptake (%ID/g at 1 h: 4.3 ± 0.7 for [99m Tc]Tc-1, 8.3 ± 0.9 for [99m Tc]Tc-2 and 4.2 ± 0.8 for [186 Re]Re-2) with moderate retention over 24 h. Rapid renal clearance was observed for [99m Tc]Tc-2 and [186 Re]Re-2 (> 84 % at 4 h), indicating favorable pharmacokinetics. Micro-SPECT/CT images for the99m Tc-tracers clearly visualized PC-3 tumors in agreement with the biodistribution data and with superior imaging properties found for [99m Tc]Tc-2., Conclusions: [99m Tc]Tc-2 shows promise for further development as a GRPR-imaging agent. [186 Re]Re-2 demonstrated very similar in vivo behavior to [99m Tc]Tc-2, and further studies are therefore justified to explore the theranostic potential of our approach for targeting of GRPR-positive cancers.- Published
- 2021
- Full Text
- View/download PDF
5. Click Chemistry
- Author
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Vinod K. Tiwari, Manoj K. Jaiswal, Sanchayita Rajkhowa, Sumit K. Singh, Vinod K. Tiwari, Manoj K. Jaiswal, Sanchayita Rajkhowa, and Sumit K. Singh
- Subjects
- Chemical processes, Catalysis
- Abstract
This book comprehensively covers the fundamentals and latest advancements in the area of click chemistry. It discusses notable applications of click chemistry in various emerging areas ranging from chemical biology to catalysis and from medicinal chemistry to material sciences. Various topics covered in this book are catalysis in regioselectivity in click chemistry, organocatalysis in triazole synthesis, Bertozzi's Bioorthogonal Concept, photo-triggered click chemistry, SuFFEx Click, Thiol-Ene Click, MCR Click, Intramolecular Click Chemistry, synthesis of diverse triazoles and their applications, Click's Post Functionalization, etc. The book is a valuable reference for beginners, researchers and professionals interested in sustainable click concept and its diverse applications in allied fields.
- Published
- 2024
6. Beyond Becquerel and Biology to Precision Radiomolecular Oncology: Festschrift in Honor of Richard P. Baum
- Author
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Vikas Prasad and Vikas Prasad
- Subjects
- Oncology, Radiotherapy
- Abstract
This open access book is written by world-renowned experts on radiomolecular precision oncology to celebrate the work, life, principles and ideology of Richard P Baum.It includes commentaries, reviews and some thought provoking novel ideas on radionuclide precision oncology, covering topics such as various aspects of theranostics and molecular radiotherapy like radiolabeled peptides, radiolabeled antibodies, dosimetry, and quality control as well as the diagnosis and treatment of specific tumor types. Featuring contributions by biologists, physicists, chemists, mathematicians, geneticists, and physicians from a range of specialties, this Festschrift is highly interdisciplinary and will be a valuable resource for future precision oncologists.
- Published
- 2024
7. Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays
- Author
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Franz J. Hock, Michael K. Pugsley, Franz J. Hock, and Michael K. Pugsley
- Subjects
- Pharmacology, Pharmaceutical chemistry, Medicinal chemistry
- Abstract
Many aspects of drug safety have become an outstanding and even persistent issue and may occur during the process of both drug discovery and development. Until 15 years ago, drug discovery and evaluation was primarily a sequential process starting with the selection of the most pharmacologically active compound from a series of newly synthesized small molecule chemical series by means of distinctive pharmacological assays. Safety aspects were addressed by evaluation of the selected compound at high doses in a series of specific studies directed at indications other than the intended indication of the new compound. These tests are then followed by pharmacokinetic studies, which are primarily conducted to confirm whether the selected compound possesses a suitable half-life for sufficient exposure and efficacy and, whether it has the desired properties specificity to the intended route of administration. Safety aspects relied predominantly on the conduct of single and repeat toxicologydose studies, which inform changes in organ structure rather than organ function. Both toxicological and pharmacokinetic studies are adapted to the progress of studies in clinical pharmacology and clinical trials. The new edition of this well and broadly accepted reference work contains several innovative and distinguished chapters. This'sequential'strategy has been abandoned with this new version of the book for several reasons: - Of the possible multitude of negative effects that novel drugs may impart on organ function, e.g. ventricular tachy-arrhythmia, many are detected too late in non-clinical studies to inform clinicians. On the other hand, negative findings in chronic toxicity studies in animals may turn out to be irrelevant for human beings. - New scientific approaches, e.g. high-throughput screening, human pluripotent stem cells, transgenic animals, knock-out animals, in silico models, pharmaco-genomics and pharmaco-proteomics, as well as Artificial Intelligence (AI) methods offered new possibilities. - There are several examples, that show that the'druggability'of compounds was considerably underestimated when the probability of success of a new project was assessed. The success rate in the pharmaceutical industry and the introduction of new chemical entities to the market per year dropped dramatically, whereas the development time for a new compound increased, sometimes exceeding the patent protection. Research and development scientists, involving the following changes, therefore adopted a change of strategy: - Parallel instead of sequential involvement of the various disciplines (multidimensional compound optimization). - The term'Safety Pharmacology'was coined. The International Conference on Harmonization (ICH) founded a Safety Pharmacology Working Group and the Safety Pharmacology Society (SPS) was launched. The discipline provided for evaluation, development and validation of a multitude of safety tests outlined in the'Core Battery of Studies'. - Characterizing the exposure profile of a drug by conducting pharmacokinetic studies that evaluates the absorption, distribution, metabolism and excretion should to be investigated at an early stage of development as results contribute to the selection of a compound for further development. Advancements in Toxicology were achieved by the introduction of new methods, e.g., in silico methods, genetic toxicology, computational toxicology and AI. The book is a landmark in the continuously changing world of drug research and developments. As such, it is essential reading for many groups: not only for all students of pharmacology and toxicology but also for industry scientists and physicians, especially those involved in clinical trials of drugs, and for pharmacists who must know the safety requirements of drugs. &nb
- Published
- 2024
8. Radiopharmaceutical Therapy
- Author
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Lisa Bodei, Jason S. Lewis, Brian M. Zeglis, Lisa Bodei, Jason S. Lewis, and Brian M. Zeglis
- Subjects
- Radiotherapy, Diagnostic imaging, Cancer--Radiotherapy, Radiopharmaceuticals--Therapeutic use, Nuclear medicine, Biochemistry
- Abstract
This book covers foundational topics in the emerging field of radiopharmaceutical therapy. It is divided into three sections: fundamentals, deeper dives, and special topics. In the first section, the authors examine the field from a bird's-eye view, covering topics including the history of radiopharmaceutical therapy, the radiobiology of radiopharmaceutical therapy, and the radiopharmaceutical chemistry of both metallic and non-metallic radionuclides. The second section provides a more in-depth look at specific radiotherapeutics. Chapters include broader discussions of the different platforms for radiopharmaceutical therapy as well as more focused case studies covering individual radiotherapeutics. The third and final section explores a number of areas for further study, including medical physics, artificial intelligence, in vivo pretargeting, theranostic imaging, and the regulatory review process for radiotherapeutics.This book is the first of its kind andis useful for a broad audience of scientists, researchers, physicians, and students across a range of fields, including biochemistry, cancer biology, nuclear medicine, radiology, and radiation oncology.
- Published
- 2023
9. The Kappa Opioid Receptor
- Author
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Lee-Yuan Liu-Chen, Saadet Inan, Lee-Yuan Liu-Chen, and Saadet Inan
- Subjects
- Opioids--Receptors, Pharmacology
- Abstract
This book covers the latest knowledge in structure, signaling, and biochemical pharmacology of KOR as well as preclinical research and clinical applications (including clinical phase studies and approved for human use) of KOR compounds. It is divided up into the three parts: Molecular aspects of KOR, Preclinical research on pharmacology of KOR agonists and antagonists in animals and KOR agonists and antagonists in clinical use and in past and present clinical trials.The chapters'Biosensors monitor ligand-selective effects at kappa opioid receptors'and'The role of dynorphin and the kappa opioid receptor in schizophrenia and major depressive disorder: a translational approach'of this book are available open access under a Creative Commons Attribution 4.0 International License via link.springer.com.
- Published
- 2022
10. Clinical Nuclear Medicine
- Author
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Hojjat Ahmadzadehfar, Hans-Jürgen Biersack, Leonard M. Freeman, Lionel S. Zuckier, Hojjat Ahmadzadehfar, Hans-Jürgen Biersack, Leonard M. Freeman, and Lionel S. Zuckier
- Subjects
- Radioisotope scanning, Nuclear medicine
- Abstract
In the new edition of this very successful book, European and North American experts present the state of the art in diagnostic and therapeutic radionuclide procedures. The aim is to examine established and emerging clinical applications in detail, rather than to consider everything included in the comprehensive texts already available within the field. This “practical” approach ensures that the book will be a valuable guide for nuclear medicine physicians, technologists, students, and interested clinicians alike. This edition of Clinical Nuclear Medicine has been extensively revised to take account of recent developments. The roles of SPECT/CT, PET/CT, and PET/MRI are clearly explained and illustrated, and the coverage extended to encompass, for example, novel PET tracers and therapeutic radionuclides, advanced techniques of brain imaging, and the development of theranostics. Readers will be fully persuaded of the ever-increasing value of nuclear medicine techniques in depicting physiology and function and complementing anatomic modalities such as CT, MRI, and ultrasound.
- Published
- 2020
11. Chemical Epigenetics
- Author
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Antonello Mai and Antonello Mai
- Subjects
- Medicinal chemistry, Genetics, Enzymology, Chemistry, Technical
- Abstract
This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
- Published
- 2020
12. CPP, Cell-Penetrating Peptides
- Author
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Ülo Langel and Ülo Langel
- Subjects
- Drug carriers (Pharmacy), Medicine, Peptides, Biochemistry
- Abstract
In this book, a summary and update of the most important areas of cell-penetrating peptides (CPP) research are presented, while raising relevant questions for further development. The CPP sequences are presented and discussed throughout the book. The methods for testing CPP mechanisms are discussed in detail. Various approaches for the testing of endocytotic pathways of CPP uptake are also described. Different CPP uptake experiments are compared since it is becoming clear that it is often best to apply several methods in a complementary manner in order to most comprehensively evaluate CPP uptake mechanisms due to the complexity of these processes. A brief summary of functionality issues of CPPs, both in vitro and in vivo, is discussed. Therapeutic potential of CPPs and commercial developments are discussed. The present, second edition of this book is the updated and expanded version of the first edition, published in 2019. The development of the field of cell-penetrating peptides in these five years has been obvious and exciting. This second edition of the book has been partly reorganized and comprehensively expanded with the exciting research in 2019-2023. Around 2500 novel scientific articles have become available, most of them are reviewed in the second edition. Additional rapidly growing areas of high impact presented in this second edition are therapeutic developments (Chapter 16) and delivery of oligonucleotides and proteins/peptides (Chapters 5 and 6) including novel reports on genome editing with CPP assistance. Also, several additional examples are available now on clinical trials using CPPs (Chapter 15). The book is written for researchers and students in the field.
- Published
- 2019
13. Applications of Ion Exchange Materials in Biomedical Industries
- Author
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Inamuddin and Inamuddin
- Subjects
- Pharmaceutical chemistry, Separation (Technology), Chemistry, Technical
- Abstract
This book presents the applications of ion-exchange materials in the biomedical industries. It includes topics related to the application of ion exchange chromatography in determination, extraction and separation of various compounds such as amino acids, morphine, antibiotics, nucleotides, penicillin and many more. This title is a highly valuable source of knowledge on ion-exchange materials and their applications suitable for postgraduate students and researchers but also to industrial R&D specialists in chemistry, chemical, and biochemical technology. Additionally, this book will provide an in-depth knowledge of ion-exchange column and operations suitable for engineers and industrialists.
- Published
- 2019
14. Radiopharmaceutical Chemistry
- Author
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Jason S. Lewis, Albert D. Windhorst, Brian M. Zeglis, Jason S. Lewis, Albert D. Windhorst, and Brian M. Zeglis
- Subjects
- Radiopharmaceuticals, Pharmaceutical chemistry
- Abstract
This book is a comprehensive guide to radiopharmaceutical chemistry. The stunning clinical successes of nuclear imaging and targeted radiotherapy have resulted in rapid growth in the field of radiopharmaceutical chemistry, an essential component of nuclear medicine and radiology. However, at this point, interest in the field outpaces the academic and educational infrastructure needed to train radiopharmaceutical chemists. For example, the vast majority of texts that address radiopharmaceutical chemistry do so only peripherally, focusing instead on nuclear chemistry (i.e. nuclear reactions in reactors), heavy element radiochemistry (i.e. the decomposition of radioactive waste), or solely on the clinical applications of radiopharmaceuticals (e.g. the use of PET tracers in oncology). This text fills that gap by focusing on the chemistry of radiopharmaceuticals, with key coverage of how that knowledge translates to the development of diagnostic and therapeutic radiopharmaceuticals for the clinic. The text is divided into three overarching sections: First Principles, Radiochemistry, and Special Topics. The first is a general overview covering fundamental and broad issues like “The Production of Radionuclides” and “Basics of Radiochemistry”. The second section is the main focus of the book. In this section, each chapter's author will delve much deeper into the subject matter, covering both well established and state-of-the-art techniques in radiopharmaceutical chemistry. This section will be divided according to radionuclide and will include chapters on radiolabeling methods using all of the common nuclides employed in radiopharmaceuticals, including four chapters on the ubiquitously used fluorine-18 and a “Best of the Rest” chapter to cover emerging radionuclides. Finally, the third section of the book is dedicated to special topics with important information for radiochemists, including “Bioconjugation Methods,” “Click Chemistry in Radiochemistry”, and “Radiochemical Instrumentation.” This is an ideal educational guide for nuclear medicine physicians, radiologists, and radiopharmaceutical chemists, as well as residents and trainees in all of these areas.
- Published
- 2019
15. The Nociceptin/Orphanin FQ Peptide Receptor
- Author
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Mei-Chuan Ko, Girolamo Caló, Mei-Chuan Ko, and Girolamo Caló
- Subjects
- Neurotransmitter receptors
- Abstract
The aim of this book is not only to introduce readers with a broad spectrum of biological actions of the NOP receptor, but also to feature a detailed look at the N/OFQ-NOP receptor system, medicinal chemistry, pharmacology, and clinical data of NOP-targeted ligands. This special volume book - for the first time focusing on the NOP receptor - is designed to serve as a useful reference, stimulate more research on the N/OFQ-NOP receptor system, and lead to more development of NOP-related ligands for several therapeutic applications.
- Published
- 2019
16. Delta Opioid Receptor Pharmacology and Therapeutic Applications
- Author
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Emily M. Jutkiewicz and Emily M. Jutkiewicz
- Subjects
- Ligands, Toxicology, Opioids--Receptors, Pharmacology, Experimental
- Abstract
This volume describes our current understanding of the biological role of the delta-opioid receptor (DOR) system, focusing on its unique mechanisms of receptor trafficking and signaling in disease states. Part 1 covers the endogenous ligands that regulate the DOR system as well as novel compounds and therapies used to modulate the DOR system. Part 2 describes new insights into the localization and trafficking of the DOR and how ligand-directed signaling alters the fate of the receptor. Part 3 concentrates on the potential role of the DOR system in disease states, such as pain, mood, addiction, and Parkinson's disease. Throughout the book, the DOR system as a target for drug development will be discussed.
- Published
- 2018
17. Peptidomimetics I
- Author
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William D. Lubell and William D. Lubell
- Subjects
- Chemistry, Organic, Medicinal chemistry, Biotechnology
- Abstract
The series Topics in Heterocyclic Chemistry presents critical reviews on present and future trends in the research of heterocyclic compounds. Overall the scope is to cover topics dealing with all areas within heterocyclic chemistry, both experimental and theoretical, of interest to the general heterocyclic chemistry community. The series consists of topic related volumes edited by renowned editors with contributions of experts in the field. All chapters from Topics in Heterocyclic Chemistry are published Online First with an individual DOI. In references, Topics in Heterocyclic Chemistry is abbreviated as Top Heterocycl Chem and cited as a journal.
- Published
- 2017
18. Synthesis of Heterocycles by Metathesis Reactions
- Author
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Joëlle Prunet and Joëlle Prunet
- Subjects
- Chemistry, Organic, Chemistry, Technical, Inorganic chemistry
- Abstract
The series Topics in Heterocyclic Chemistry presents critical reviews on present and future trends in the research of heterocyclic compounds. Overall the scope is to cover topics dealing with all areas within heterocyclic chemistry, both experimental and theoretical, of interest to the general heterocyclic chemistry community. The series consists of topic related volumes edited by renowned editors with contributions of experts in the field. All chapters from Topics in Heterocyclic Chemistry are published Online First with an individual DOI. In references, Topics in Heterocyclic Chemistry is abbreviated as Top Heterocycl Chem and cited as a journal.
- Published
- 2016
19. Analytical Techniques in the Pharmaceutical Sciences
- Author
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Anette Müllertz, Yvonne Perrie, Thomas Rades, Anette Müllertz, Yvonne Perrie, and Thomas Rades
- Subjects
- Biomedical engineering, Pharmacology--Technique, Drugs--Analysis--Technique
- Abstract
The aim of this book is to present a range of analytical methods that can be used in formulation design and development and focus on how these systems can be applied to understand formulation components and the dosage form these build. To effectively design and exploit drug delivery systems, the underlying characteristic of a dosage form must be understood--from the characteristics of the individual formulation components, to how they act and interact within the formulation, and finally, to how this formulation responds in different biological environments. To achieve this, there is a wide range of analytical techniques that can be adopted to understand and elucidate the mechanics of drug delivery and drug formulation. Such methods include e.g. spectroscopic analysis, diffractometric analysis, thermal investigations, surface analytical techniques, particle size analysis, rheological techniques, methods to characterize drug stability and release, and biological analysis in appropriate cell and animal models. Whilst each of these methods can encompass a full research area in their own right, formulation scientists must be able to effectively apply these methods to the delivery system they are considering. The information in this book is designed to support researchers in their ability to fully characterize and analyze a range of delivery systems, using an appropriate selection of analytical techniques. Due to its consideration of regulatory approval, this book will also be suitable for industrial researchers both at early stage up to pre-clinical research.
- Published
- 2016
20. Peptidomimetics II
- Author
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William D. Lubell and William D. Lubell
- Subjects
- Chemistry, Organic, Medicinal chemistry, Biotechnology
- Abstract
The series Topics in Heterocyclic Chemistry presents critical reviews on present and future trends in the research of heterocyclic compounds. Overall the scope is to cover topics dealing with all areas within heterocyclic chemistry, both experimental and theoretical, of interest to the general heterocyclic chemistry community. The series consists of topic related volumes edited by renowned editors with contributions of experts in the field. All chapters from Topics in Heterocyclic Chemistry are published Online First with an individual DOI. In references, Topics in Heterocyclic Chemistry is abbreviated as Top Heterocycl Chem and cited as a journal.
- Published
- 2016
21. Molecular Imaging of Small Animals : Instrumentation and Applications
- Author
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Habib Zaidi and Habib Zaidi
- Subjects
- Laboratory animals, Biology--Research--Technique, Veterinary diagnostic imaging, Imaging systems in biology, Medicine--Research--Technique
- Abstract
This book examines the fundamental concepts of multimodality small-animal molecular imaging technologies and their numerous applications in biomedical research. Driven primarily by the widespread availability of various small-animal models of human diseases replicating accurately biological and biochemical processes in vivo, this is a relatively new yet rapidly expanding field that has excellent potential to become a powerful tool in biomedical research and drug development.In addition to being a powerful clinical tool, a number of imaging modalities including but not limited to CT, MRI, SPECT and PET are also used in small laboratory animal research to visualize and track certain molecular processes associated with diseases such as cancer, heart disease and neurological disorders in living small animal models of disease. In vivo small-animal imaging is playing a pivotal role in the scientific research paradigm enabling to understand human molecular biology andpathophysiology using, for instance, genetically engineered mice with spontaneous diseases that closely mimic human diseases.
- Published
- 2014
22. Applications of MALDI-TOF Spectroscopy
- Author
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Zongwei Cai, Shuying Liu, Zongwei Cai, and Shuying Liu
- Subjects
- Mass spectrometry, Biomolecules--Analysis
- Abstract
MALDI-ToF Mass Spectrometry for Studying Noncovalent Complexes of Biomolecules, by Stefanie Mädler, Elisabetta Boeri Erba, Renato Zenobi Application of MALDI-TOF-Mass Spectrometry to Proteome Analysis Using Stain-Free Gel Electrophoresis, by Iuliana Susnea, Bogdan Bernevic, Michael Wicke, Li Ma, Shuying Liu, Karl Schellander, Michael Przybylski MALDI Mass Spectrometry for Nucleic Acid Analysis, by Xiang Gao, Boon-Huan Tan, Richard J. Sugrue, Kai Tang Determination of Peptide and Protein Disulfide Linkages by MALDI Mass Spectrometry, by Hongmei Yang, Ning Liu, Shuying Liu MALDI In-Source Decay, from Sequencing to Imaging, by Delphine Debois, Nicolas Smargiasso, Kevin Demeure, Daiki Asakawa, Tyler A. Zimmerman, Loïc Quinton, Edwin De Pauw Advances of MALDI-TOF MS in the Analysis of Traditional Chinese Medicines, by Minghua Lu, Zongwei Cai Chemical and Biochemical Applications of MALDI TOF-MS Based on Analyzing the Small Organic Compounds, by Haoyang Wang, Zhixiong Zhao, Yinlong Guo Bioinformatic Analysis of Data Generated from MALDI Mass Spectrometry for Biomarker Discovery, by Zengyou He, Robert Z. Qi, Weichuan Yu
- Published
- 2014
23. Peptides: The Wave of the Future : Proceedings of the Second International and the Seventeenth American Peptide Symposium, June 9–14, 2001, San Diego, California, U.S.A.
- Author
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Richard A. Houghten, Michal Lebl, Richard A. Houghten, and Michal Lebl
- Subjects
- Biochemistry, Anatomy, Comparative, Polymers
- Abstract
This volume contains the proceedings of the Second International Peptide Symposium and the Seventeenth American Peptide Symposium, held on 9-14 June, 2001, at the Town and Country Resort in San Diego, California. The biennial meeting was held under the auspices of the American Peptide Society. In addition to the main Symposium, we were honored to have the Merrifield Satellite Symposium, honoring Bruce Merrifield's accomplishments on his 80th birthday. Over 1250 participants from around the world attended the lectures, posters, and exhibits. Reflecting the international nature of the Symposium, there were participants from 37 countries in attendance. In addition to the 75 plenary lectures, there were over 575 poster presentations, and 70 commercial exhibits as well as booths from the American, Australian, Chinese, European, and Japanese Peptide Societies. These proceedings include plenary lectures and oral and poster presentations collected from a wide diversity of topics providing a truly comprehensive and up-to-date overview of the field of peptide science. This publication contains essential reference information for researchers active in peptide science.
- Published
- 2014
24. Hydroxamic Acids : A Unique Family of Chemicals with Multiple Biological Activities
- Author
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Satya P. Gupta and Satya P. Gupta
- Subjects
- Chemistry, Organic, Pharmaceutical technology, Hydroxamic acids, Biochemistry
- Abstract
Satya P. Gupta's Hydroxamics Acids is the first book to compile invited articles written by international experts on the class of compounds hydroxamic acids. Found to possess a wide spectrum of biological activities, the hydroxamic acids are of interest to theoretical and experimental chemists who can study and make use of them in drug design and development. Chapters in this book provide a diverse and comprehensive coverage of this compound class and consequently this publication is a valuable resource for researchers in chemical, pharmaceutical and biological sciences.
- Published
- 2013
25. Hagers Handbuch der Pharmazeutischen Praxis : Drogen P-Z Folgeband 2
- Author
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Rudolf Hänsel, Konstantin Keller, Horst Rimpler, Georg Schneider, Rudolf Hänsel, Konstantin Keller, Horst Rimpler, and Georg Schneider
- Subjects
- Pharmacy, Medicine—Research, Biology—Research
- Abstract
Der dritte Band des Gebietes Drogen der Neuauflage enthält in alphabetischer Reihenfolge von P - Z Monographien über Arzneipflanzengattungen. Jede einzelne Monographie umfaßt die für die pharmazeutische Praxis wichtigen Arzneipflanzen mit den dazugehörigen allopathischen und homöopathischen Zubereitungen. In den Monographien werden Aussagen über die Botanik, Chemotaxonomie, Analytik, Wirkung, medizinische Anwendung und Toxikologie gemacht. Von besonderer Bedeutung sind Drogen des DAB/HAB und von in Europa gültigen Arzneibüchern.
- Published
- 2013
26. Fortschritte Der Chemie Organischer Naturstoffe / Progress in the Chemistry of Organic Natural Products
- Subjects
- Chemistry, Organic, Biochemistry, Pharmacology, Botany, Pharmacy
- Abstract
Since the late 1950's when proton n. m. r. spectroscopy was first used in organic natural products studies the technique has increasingly con of this important area of chemistry. tributed to the rapid advancement Although the potential utility of 13C n. m. r. was recognized very early, essentially no application of 13C n. m. r. appeared in the literature prior to 1966 and 95% of the existing data are less than five years old. The initially slow growth had its cause in inadequate instrumentation, insufficient sensitivity being the main obstacle. This situation drastically changed with the advent and commercial availability of broadband ex citation and Fourier transform methods, giving natural-abundance 13C n. m. r. and its numerous chemical applications a tremendous impetus. Today BC spectra can be recorded on sample quantities down to the submilligram level, which until recently even withstood proton n. m. r. Paralleling the development of experimental techniques considerable progress has also been made on an understanding of spectral parameters, in particular their stereochemical implications on natural products. Although the large majority of data present up to now deals with known structures, an adequate basis now exists which allows the chemist to use the technique for tackling real problems on unknown molecules.
- Published
- 2013
27. Molecular Biology of Brain and Endocrine Peptidergic Systems
- Author
-
M. Chretien and M. Chretien
- Subjects
- Brain chemistry--Congresses, Molecular neurobiology--Congresses, Neuropeptides--Congresses, Neuroendocrinology--Congresses, Neurobiology--congresses
- Abstract
We had the pleasure and the great opportunity to organize a symposium on'Molecular Biology of Brain and Endocrine Peptidergic Systems'under the auspices of the Canadian Biochemical society and the International Foundation for Biochemical Endocrinology. We were indeed very happy to ass~ble a series of first rate speakers who delivered excellent papers on a variety of subjects from the synthesis of complicated peptide analogs, to the creation of trangenic mice, site-directed mutagenesis, enzyme characterization and DNA binding sites. One hundred and seventy-five participants attended the 40 conferences while having the opportunity to look at 24 posters presented by senior scientists as well as students. We, of the organizing committee, feel extremely pleased to have received an overwhelming response from such a group of scholars. We wish to express our sincere gratitude to Mrs. Diane Marcil who arranged most aspects of the meeting with efficiency. We also thank the different organizations and companies for their generous grants which made the reunion possible. We hope that the participants have gained scientifically while having a pleasant sojourn in beautiful Montreal. The organizing committee was made up of a group of dedicated people, particularly its secretary, Dr. Philippe Crine. To all speakers and sessions chairpersons, we are indebted for the excellence of their participation.
- Published
- 2013
28. Peptides in Oncology II : Somatostatin Analogues and Bombesin Antagonists
- Author
-
K. Höffken and K. Höffken
- Subjects
- Somatostatin--Derivatives--Therapeutic use--, Bombesin--Antagonists--Therapeutic use--Test, Cancer--Chemotherapy, Neoplasms--drug therapy, Somatostatin--therapeutic use, Somatostatin--analogs & derivatives, Bombesin--therapeutic use, Bombesin--antagonists & inhibitors
- Published
- 2012
29. Isoquinoline Alkaloids Research 1972–1977
- Author
-
Maurice Shamma and Maurice Shamma
- Subjects
- Alkaloids, Isoquinoline
- Published
- 2012
30. Stereochemical Analysis of Alicyclic Compounds by C-13 NMR Spectroscopy
- Author
-
J. A. Whitesell and J. A. Whitesell
- Subjects
- Nuclear magnetic resonance spectroscopy, Carbon--Isotopes--Analysis, Stereochemistry, Alicyclic compounds--Analysis
- Abstract
Through numerous conversations with other synthetic chemists it became apparent that the great power of carbon nuclear magnetic resonance was being significantly underutilized. In our own work we have found that 13C spectroscopy is a more powerful tool than IH NMR spectroscopy, especially for probing subtle stereochemical questions in complicated systems. This is especially true in five membered ring compounds where IH NMR is at a particular disadvantage. The two techniques can be used independently to solve the same question-that of stereochemistry - but they do so in different ways. Advantage can be taken in IH NMR of a relatively consistent relationship between stereochemical orientation and coupling constants between vicinal protons, while in 13C NMR it is the correlation between spatial relationships of non-hydrogen, y substituents and their effect on chemical shift that can be used to assign stereochemistry. It was also clear that the use of 13C NMR required a different approach to problem solving than that typically used with IH NMR. While the latter technique could be employed with a very general approach (e.g., the Karplus equation), 13C NMR would, at least for the immediate future, require a relatively extensive set of model systems from which the consequences of stereochemical changes could be derived for any given carbon framework.
- Published
- 2012
31. Non-fibrillar Amyloidogenic Protein Assemblies - Common Cytotoxins Underlying Degenerative Diseases
- Author
-
Farid Rahimi, Gal Bitan, Farid Rahimi, and Gal Bitan
- Subjects
- Chronic diseases, Amyloid, Degeneration (Pathology)
- Abstract
Amyloid-forming proteins are implicated in over 30 human diseases. The proteins involved in each disease have unrelated sequences and dissimilar native structures, but they all undergo conformational alterations to form fibrillar polymers. The fibrillar assemblies accumulate progressively into disease-specific lesions in vivo. Substantial evidence suggests these lesions are the end state of aberrant protein folding whereas the actual disease-causing culprits likely are soluble, non-fibrillar assemblies preceding the aggregates. The non-fibrillar protein assemblies range from small, low-order oligomers to spherical, annular, and protofibrillar species. Oligomeric species are believed to mediate various pathogenic mechanisms that lead to cellular dysfunction, cytotoxicity, and cell loss, eventuating in disease-specific degeneration and systemic morbidity. The particular pathologies thus are determined by the afflicted cell types, organs, systems, and the proteins involved. Evidence suggests that the oligomeric species may share structural features and possibly common mechanisms of action. In many cases, the structure–function interrelationships amongst the various protein assemblies described in vitro are still elusive. Deciphering these intricate structure–function correlations will help understanding a complex array of pathogenic mechanisms, some of which may be common across different diseases albeit affecting different cell types and systems.
- Published
- 2012
32. Glucagon III
- Author
-
Pierre J. Lefebvre and Pierre J. Lefebvre
- Subjects
- Pharmacology, Diseases, Human physiology, Biochemistry
- Abstract
Glucagon III complements Glucagon I and II published in 1983 in this series as Vols. 66/I and II. These three volumes truly represent a'glucagon encyclopedia'and as such have no competitors in the scientific literature worldwide. In this volume, the most recent data on glucagon molecular biology are reviewed together with clinically relevant information on the role of glucagon in the pathophysiology of diabetes, the place of glucagon in medical imaging or in emergency medicine. Chapters are devoted to newly identified members of the glucagon family such as glucagon-like peptide-1 (GLP-1) and oxyntomodulin. Glucagon III is a comprehensive review of all information published on this important hormone since 1983 and is the reference book on the subject.
- Published
- 2012
33. Click Triazoles
- Author
-
Janez Košmrlj and Janez Košmrlj
- Subjects
- Chemistry, Organic, Medicinal chemistry, Pharmacy
- Abstract
B. R. Buckley and H. Heaney: Mechanistic Investigations of Copper(I)- Catalyzed Alkyne–Azide Cycloaddition Reactions.- J. D. Crowley and D. A. McMorran: “Click-Triazole” Coordination Chemistry: Exploiting 1,4-Disubstituted-1,2,3-Triazoles as Ligands.- S. Lee and A. H. Flood: Binding Anions in Rigid and Reconfigurable Triazole Receptors.- M. Watkinson: Click Triazoles as Chemosensors.- H.-F. Chow, C.-M. Lo and Y. Chen: Triazole-Based Polymer Gels.- T. Zheng, S. H. Rouhanifard, A. S. Jalloh, P. Wu: Click Triazoles for Bioconjugation.- S. Mignani, Y. Zhou, T. Lecourt and L. Micouin: Recent Developments in the Synthesis 1,4,5-Trisubstituted Triazoles.
- Published
- 2012
34. Design and Synthesis of Organic Molecules Based on Molecular Recognition : Proceedings of the XVIIIth Solvay Conference on Chemistry Brussels, November 28 - December 01, 1983
- Author
-
Georges van Binst and Georges van Binst
- Subjects
- Chemistry, Organic
- Abstract
A topic for a Solvay Conference should be general enough to conform with the great tradition of previous conferences. On the other hand it should not be so broad that it can not be covered during the limited time of the conference. After discussion of several such topics,'Design and Synthesis of Organic Molecules Based on Molecular Recognition'was chosen. According to Albert Einstein we live in an era of perfect methods and confused aims. For example in organic chemistry the known synthetic methods allow us to prepare an astronomical number of compounds; the gap between the possible and the relevant becomes larger every day. After discovery and classification of the main types of reactions, the study of the selectivity of reactions becomes of paramount importance. One can learn quite a lot from Nature, which uses molecular recognition to achieve selec tivity in a degree so far unattainable by mere mortals. To analyze the structural features applied by Nature, to accomplish high molecular recog nition, and to simulate these features by synthesis have recently become therefore favorite occupations of chemists. The purpose of this conference was to bring together two groups, the analysts and the syntheticists, to discuss the present status of the knowledge. This monograph contains the chairman's introduction in which he has summarized the main points at issue and the contributions of the renowned scientists who participated. The organizers hope that it will stimulate further research in this fascinating field.
- Published
- 2012
35. Recent Advances in Chiral Separations
- Author
-
D. Stevenson, I.D. Wilson, D. Stevenson, and I.D. Wilson
- Subjects
- Liquid chromatography--Congresses, Enantiomers--Separation--Congresses
- Abstract
This volume represents the proceedings of the second international meeting on chiral separations held at the University of Surrey between the 12th and 15th of September 1989. Like the preceding meeting, it was jointly organised by the Chromatographic Society and the Robens Institute of the University of Surrey in response to the continued interest in this area of separation science. Of particular interest to the organisers was the very clear change in the nature of the delegates attending this second symposium as compared with the first. At the previous meeting the majority of the delegates were composed of chromatographers with problems in the area of chiral separations who were keen to learn as much as possible about these techniques from the handful of recognised experts in this area. In this second symposium the divide between expert and novice was much less apparent, with the latter providing many interesting and useful contributions to the scientific programme in termt; of both oral and poster presentations.
- Published
- 2012
36. Peroxisomal Disorders and Regulation of Genes
- Author
-
Frank Roels, Myriam Baes, Sylvia Delanghe, Frank Roels, Myriam Baes, and Sylvia Delanghe
- Subjects
- Medical genetics, Internal medicine, Biochemistry, Neurology, Pediatrics
- Abstract
In most peroxisomal disorders the nervous system is severely affected which explains the clinical and community burden they represent. This is the first book to focus not only on the mutations causing these inherited illnesses, but also on mechanisms that regulate, suppress or enhance expression of genes and their products (enzymes). Indeed since the success and completion of the Human Genome Project all genes (coding DNA sequences) are known. However, of many, their function, and the role of the gene product has not been determined. An example is X-linked adrenoleukodystrophy, the most frequent peroxisomal disorder. Children are born healthy, but in more than 1 out of 3, demyelination of the brain starts unpredictably and they die in a vegetative state. The gene mutated in most families has been known for 10 years; but the true role of the encoded protein, ALDp, is still speculative; and within the same family, very severe and asymptomatic clinical histories co-exist, unexplained by the mutation.
- Published
- 2012
37. Chiral Recognition in Separation Methods : Mechanisms and Applications
- Author
-
Alain Berthod and Alain Berthod
- Subjects
- Chromatographic analysis, Toxicology, Enantiomers--Separation, Chirality
- Abstract
What drives a scientist to edit a book on a speci c scienti c subject such as chiral mechanisms in separation methods? Until December 2005, the journal Analytical Chemistry of the American Chemical Society (Washington, DC) had an A-page section that was dedicated to simple and clear presentations of the most recent te- niques or the state of the art in a particular eld or topic. The “A-page” section was prepared for a broad audience of chemists including industrial professionals, s- dents as well as academics looking for information outside their eld of expertise. 1 Daniel W. Armstrong, one of the editors of this journal and a twenty-year+ long friend, invited me to present my view on chiral recognition mechanisms in a simple and clear way in an “A-page” article. In 2006, the “A-page” section was maintained as the rst articles at the beginning of each rst bi-monthly issue but the pagination was no longer page distinguished from the regular research articles published by the journal. During the time between the invitation and the submission, the A-page section was integrated into the rest of the journal and the article appeared as (2006) Anal Chem (78):2093–2099.
- Published
- 2010
38. C-X Bond Formation
- Author
-
Arkadi Vigalok and Arkadi Vigalok
- Subjects
- Organometallic chemistry
- Abstract
Contents: Kilian Muñiz: Transition Metal Catalyzed Electrophilic Halogenation of C-H bonds in alpha-Position to Carbonyl Groups; Arkadi Vigalok • and Ariela W Kaspi: Late Transition Metal-Mediated Formation of Carbon-Halogen Bonds; Paul Bichler and Jennifer A. Love•: Organometallic Approaches to Carbon-Sulfur Bond Formation; David S. Glueck: Recent Advances in Metal-Catalyzed C-P Bond Formation; Andrei N. Vedernikov: C-O Reductive Elimination from High Valent Pt and Pd Centers; Lukas Hintermann: Recent Developments in Metal-Catalyzed Additions of Oxygen Nucleophiles to Alkenes and Alkynes; Moris S. Eisen: Catalytic C-N, C-O and C-S bond formation promoted by organoactinide complexes.
- Published
- 2010
39. Medicinal Organometallic Chemistry
- Author
-
Gérard Jaouen, Nils Metzler-Nolte, Gérard Jaouen, and Nils Metzler-Nolte
- Subjects
- Organometallic chemistry, Medicinal chemistry, Cancer, Pharmaceutical chemistry, Biotechnology
- Abstract
Contents: Gérard Jaouen, Nils Metzler-Nolte : Introduction ; Stéphane GIBAUD and Gérard JAOUEN: Arsenic - based drugs: from Fowler's solution to modern anticancer chemotherapy; Ana M. Pizarro, Abraha Habtemariam and Peter J. Sadler : Activation Mechanisms for Organometallic Anticancer Complexes; Angela Casini, Christian G. Hartinger, Alexey A. Nazarov, Paul J. Dyson : Organometallic antitumour agents with alternative modes of action; Elizabeth A. Hillard, Anne Vessières, Gerard Jaouen : Ferrocene functionalized endocrine modulators for the treatment of cancer; Megan Hogan and Matthias Tacke : Titanocenes – Cytotoxic and Anti-Angiogenic Chemotherapy Against Advanced Renal-Cell Cancer; Seann P. Mulcahy and Eric Meggers : Organometallics as Structural Scaffolds for Enzyme Inhibitor Design; Christophe Biot and Daniel Dive : Bioorganometallic Chemistry and Malaria; Nils Metzler-Nolte : Biomedical applications of organometal-peptide conjugates; Roger Alberto : Organometallic Radiopharmaceuticals; Brian E. Mann : Carbon Monoxide – an essential signaling molecule.
- Published
- 2010
40. Peptides for Youth : The Proceedings of the 20th American Peptide Symposium
- Author
-
Susan Valle, Emanuel Escher, William D. Lubell, Susan Valle, Emanuel Escher, and William D. Lubell
- Subjects
- Peptides--Congresses
- Abstract
The American Peptide Society (APS) provides a forum for advancing and promoting knowledge of the chemistry and biology of peptides. The approximately one thousand members of the Society come from North America and from more than thirty other countries throughout the world. Establishment of the APS was a result of the rapid worldwide growth that has occurred in peptide-related research, and of the increasing interaction of peptide scientists with virtually all fields of science. Peptides for Youth: The Proceedings of the the 20th American Peptide Symposium will highlight many of the recent developments in peptide science, with a particular emphasis on how these advances are being applied to basic problems in biology and medicine. The 20th American Peptide Symposium will take place June 26 - 30, 2007 in Montreal, Canada.
- Published
- 2009
41. Molecular Imaging II
- Author
-
Wolfhard Semmler, Markus Schwaiger, Wolfhard Semmler, and Markus Schwaiger
- Subjects
- Molecular diagnosis, Diagnostic imaging
- Abstract
The aim of this textbook of molecular imaging is to provide an up to date review of this rapidly growing field and to discuss basic methodological aspects necessary for the interpretation of experimental and clinical results. Emphasis is placed on the interplay of imaging technology and probe development, since the physical properties of the imaging approach need to be closely linked with the biologic application of the probe (i.e. nanoparticles and microbubbles). Various chemical strategies are discussed and related to the biologic applications. Reporter-gene imaging is beeing addressed not only in experimental protocols, but also first clinical applications are discussed. Finally, strategies of imaging to characterize apoptosis and angiogenesis are described and discussed in the context of possible clinical translation.
- Published
- 2008
42. Technetium-99m Pharmaceuticals : Preparation and Quality Control in Nuclear Medicine
- Author
-
Ilse Zolle and Ilse Zolle
- Subjects
- Radiology, Nuclear medicine
- Abstract
Radioactive drug development is a multi-disciplinary task, therefore, in a concerted effort, dedicated scientists and experts from different fields of specialisation have contributed to this book. It is presented in two sections. Section 1 contains basic principles and methods used for analysis, information on the chemistry of technetium and on radiopharmaceuticals labelled with technetium-99m, the characteristics of the 99 Mo/99mTc-generator, of'kits'and formulations for in-vitro labelling, and special safety aspects for in-vivo labelling of blood cells. Section 2 contains monographs of 99mTc-radiopharmaceuticals used in nuclear medicine. Each monograph includes information on the chemistry, formulation, commercial products and trade names, factors affecting in-vivo performance, clinical information on pharmacokinetics, as well as details concerning the clinical application and the radiation dose to patients.
- Published
- 2007
43. Understanding Biology Using Peptides : Proceedings of the Nineteenth American Peptide Symposium
- Author
-
Sylvie E. Blondelle and Sylvie E. Blondelle
- Subjects
- Proteins, Cytology, Medicine—Research, Biology—Research, Medical microbiology, Medicinal chemistry
- Abstract
Understanding Biology Using Peptides: Proceedings of the 19th American Peptide Symposium highlights many of the recent developments in peptide science, with a particular emphasis on how these advances are being applied to basic problems in biology and medicine. Specific topics covered include novel synthetic strategies, peptides in biological signaling, post-translational modifications of peptides and proteins, peptide quaternary structure in material science and disease, and peptides as tools in drug discovery.
- Published
- 2007
44. Combinatorial Chemistry on Solid Supports
- Author
-
Stefan Braese and Stefan Braese
- Subjects
- Chemistry, Organic, Biochemistry, Organometallic chemistry, Medicinal chemistry
- Abstract
With contributions by numerous experts
- Published
- 2007
45. PET Chemistry : The Driving Force in Molecular Imaging
- Author
-
P.A. Schubiger, L. Lehmann, M. Friebe, P.A. Schubiger, L. Lehmann, and M. Friebe
- Subjects
- Tomography, Emission, Tomography, Emission--Congresses, Radioactive tracers
- Abstract
Personalized medicine employing patient-based tailor-made therapeutic drugs is taking over treatment paradigms in a variety of?elds in oncology and the central nervous system. The success of such therapies is mainly dependent on ef?cacious therapeutic drugs and a selective imaging probe for identi?cation of potential responders as well as therapy monitoring for an early bene?t assessment. Molecular imaging (MI) is based on the selective and speci?c interaction of a molecular probe with a biological target which is visualized through nuclear, magnetic resonance, near infrared or other methods. Therefore it is the method of choice for patient selection and therapy monitoring as well as for speci?c e- point monitoring in modern drug development. PET (positron emitting tomography), a nuclear medical imaging modality, is ideally suited to produce three-dimensional images of various targets or processes. The rapidly increasing demand for highly selective probes for MI strongly pushes the development of new PET tracers and PET chemistry. ‘PET chemistry'can be de?ned as the study of positron-emitting compounds regarding their synthesis, structure, composition, reactivity, nuclear properties and processes and their properties in natural and - natural environments. In practice PET chemistry is strongly in?uenced by the unique properties of the radioisotopes used (e. g., half-life, che- cal reactivity, etc.) and integrates scienti?c aspects of nuclear-, organic-, inorganic- and biochemistry.
- Published
- 2007
46. Radioionidation Reactions for Pharmaceuticals : Compendium for Effective Synthesis Strategies
- Author
-
H.H. Coenen, John Mertens, Bernard Mazière, H.H. Coenen, John Mertens, and Bernard Mazière
- Subjects
- Single-photon emission computed tomography, Radiopharmaceuticals--Synthesis--Handbooks, manuals, etc, Drugs--Effectiveness--Handbooks, manuals, etc, Radioactive tracers
- Abstract
Molecules of biological interest for in-vivo and in-vitro research or diagnostics of metabolic functions and of neuro-transmission are very often labeled with iodine. Based on state-of-the-art research, this compendium describes the major production routes of the six most relevant iodine radio isotopes and the various methods of labeling molecules of biological, diagnostic or pharmaceutical interest with them. The chapters describe the basic reaction mechanisms, and the influence of iodine introduction on physical/chemical and pharmacological properties. They also include examples of important reaction pathways for the preparation of radio-iodine compounds. The volume is completed by an expert system providing guidelines to obtain the most suitable method of synthesis regarding also cost and time aspects. Worked examples support the novices confronted with radio-iodination reactions.
- Published
- 2006
47. Peptide Science — Present and Future : Proceedings of the 1st International Peptide Symposium
- Author
-
Yasutsugu Shimonishi and Yasutsugu Shimonishi
- Subjects
- Peptides--Synthesis
- Abstract
In the late 1980s, Peptide Societies were established in Europe, the United States, and Japan, and more recently, in the Asian and the Pacific Rim regions including Australia, China, and Korea. At the time of the establishment of the American, European and Japanese Peptide Societies, the International Liaison Organizing Committee representing these Peptide Societies, along with the Australian Peptide Society, began discussions for holding international confer ences which would supercede or be held in lieu of the numerous individual meetings, held by the peptide societies of each individual country or region. The representative of the Chinese Peptide Society participated in these discus sion in the International Liaison Organizing Committee at the meeting of the American Peptide Symposium in Nashville, in June 1997. After lengthy discus sions over several years, we agreed to organize and host the International Peptide Symposium in Japan. The First International Peptide Symposium (IPS'97) was held on November 30–December 5, 1997, in Kyoto, and was co sponsored by four Peptide Societies. The attendance at this Symposium was 550 participants, including representatives from 32 different countries. We were very pleased with this outcome and anticipate an even larger attendance for forthcoming Symposia in future years. The revolution and advances in science and technology during the past two decades has caused traditional peptide chemistry to expand to peptide science, spreading from physical science to biology, pharmacology, and medicine.
- Published
- 2002
48. Peptides for the New Millennium : Proceedings of the 16th American Peptide Symposium June 26–July 1, 1999, Minneapolis, Minnesota, U.S.A.
- Author
-
Gregg B. Fields, James P. Tam, George Barany, Gregg B. Fields, James P. Tam, and George Barany
- Subjects
- Peptides--Congresses
- Abstract
“Have you tried peptides? Small proteins, the best in the land! Won't you try peptides? Keep all your body processes in hand! For labor and lactation oxytocin you must buy! Enkephalin always gives a good runner's high! So won't you try peptides? Small proteins, the best in the land!” The above words [1], penned by Gary Gisselman to open Peptide Ångst: La Triviata, the opera which made its world premiere on July 1, 1999, also serve as a fitting charge to the th 16 American Peptide Symposium. This latest edition of a premier biennial series was held under the auspices of the American Peptide Society, June 26–July 1, 1999, at the Minneapolis Convention Center, Minneapolis,Minnesota, with the undersigned serving as Co-Chairs. The fortunate coincidence of the calendar allowed us to set as the theme “Peptides for the New Millennium”, and in our judgment, the approximately 1200 participants [2] who converged in the Twin Cities from academic and industrial institutions in 36 countries were treated to an exciting and stimulating conference that left most everyone with an enthusiastic vision for the future of our field. The present Proceedings volume should serve as a handy reference source and succinct snapshot of peptide science at essentially its century mark – the clock having started with the initial contributions of Emil Fischer and Th. Curtius.
- Published
- 2000
49. Peptides : Frontiers of Peptide Science
- Author
-
James P. Tam, Pravin T.P. Kaumaya, James P. Tam, and Pravin T.P. Kaumaya
- Subjects
- Peptides--Congresses
- Abstract
The Fifteen American Peptide Symposium (15APS) was held in Nashville, Tennessee, on June 14-19, 1997. This biennial meeting was jointly sponsored by the American Peptide Society and Vanderbilt University. The attendance of 1,081 participants from 37 countries was lower than the two previously held Symposia. However, the number of participating countries was the largest. Thus, it was gratifying to see that this meeting retained both its international flavor and participant loyalty at a time when there are many more symposia held each year on similar subjects. The scientific program, thanks to the insights and efforts of the Program Committee as well as Dr. Peter Schiller, the President of the American Peptide Society, was extraordinarily rich, diverse, and exciting. It was comprised of 124 oral and 550 poster presentations. Three prominent format changes were installed. First, the Symposium started on Saturday instead of Sunday. Second, the program opened on Saturday afternoon with a Mini-symposium by the Young Investigators to give them an early start and attention. Finally, 40 short and definitive reports were given in two parallel sessions. The expanded format permitted an unprecedented number of lectures and enabled wider participation by the attending delegates.
- Published
- 1999
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