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6 results on '"Joanne Miura"'

1. Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure

Author

Haixia Wang, Marion Lanier, Jacques Ermolieff, Jason Pickens, Tony Gibson, Steve Swann, Joanne Miura, Anthony Ivetac, Erica L. Bradshaw-Pierce, Mark Sabat, Petro Halkowycz, Tyhonas John, Douglas R. Dougan, Derek C. Cole, Simone V. Bigi, Evan Nunez, Xiaolun Wang, Alison Chambers, Zacharia Cheruvallath, and Aki Hirokawa

Subjects
0301 basic medicine, MAP kinase kinase kinase, Kinase, Organic Chemistry, Pharmacology, Biology, medicine.disease, 01 natural sciences, Biochemistry, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, 03 medical and health sciences, chemistry.chemical_compound, 030104 developmental biology, chemistry, Apoptosis, Heart failure, Drug Discovery, medicine, ASK1, Protein kinase A, Reperfusion injury, Lead compound
Abstract

Apoptosis signal-regulating kinase 1 (ASK1/MAP3K) is a mitogen-activated protein kinase family member shown to contribute to acute ischemia/reperfusion injury. Using structure-based drug design, deconstruction, and reoptimization of a known ASK1 inhibitor, a lead compound was identified. This compound displayed robust MAP3K pathway inhibition and reduction of infarct size in an isolated perfused heart model of cardiac injury.

Published
2017

2. Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 1

Author

Corine Holub, Thu Ton-Nu, Artur Plonowski, Zacharia Cheruvallath, Christopher J. Larson, Darin Vanderpool, Mingnam Tang, Mallareddy Komandla, Douglas R. Dougan, Phil Erikson, Jun Feng, Pamela Farrell, Joanne Miura, Christopher McBride, J. David Lawson, and Yiqin Wu

Subjects
Models, Molecular, 0301 basic medicine, Indazoles, Clinical Biochemistry, Fragment-based lead discovery, Administration, Oral, Mice, Obese, Pharmaceutical Science, Aminopeptidases, 01 natural sciences, Biochemistry, Mice, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, Residue (chemistry), Drug Discovery, Animals, Humans, Methionyl Aminopeptidases, Obesity, Enzyme Inhibitors, Molecular Biology, Glycoproteins, chemistry.chemical_classification, Indazole, Methionine, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Body Weight, Organic Chemistry, METAP2, In vitro, 0104 chemical sciences, 030104 developmental biology, Enzyme, Structural biology, chemistry, Molecular Medicine
Abstract

Methionine aminopeptidase 2 (MetAP2) is an enzyme that cleaves an N-terminal methionine residue from a number of newly synthesized proteins. Pre-clinical and clinical studies suggest that MetAP2 inhibitors could be used as a novel treatment for obesity. Herein we describe our use of fragment screening methods and structural biology to quickly identify and elaborate an indazole fragment into a series of reversible MetAP2 inhibitors with

Published
2016

3. Design, synthesis and SAR of novel glucokinase activators

Author

Stephen L. Gwaltney, Mark Sabat, Yiqin Wu, Zacharia Cheruvallath, Bumsup Lee, Prasuna Guntupalli, David J. Hosfield, Andrew John Jennings, Jun Feng, Mingnam Tang, Joanne Miura, and Haixia Wang

Subjects
Models, Molecular, Pyridones, Clinical Biochemistry, Cell, Enzyme Activators, Mice, Obese, Pharmaceutical Science, Crystallography, X-Ray, Biochemistry, Diabetes Mellitus, Experimental, Mice, Structure-Activity Relationship, Glucokinase, Drug Discovery, Glucokinase activator, medicine, Animals, Hypoglycemic Agents, Structure–activity relationship, Molecular Biology, chemistry.chemical_classification, Molecular Structure, Organic Chemistry, Glucose Tolerance Test, Enzyme Activation, Mice, Inbred C57BL, Disease Models, Animal, Enzyme, medicine.anatomical_structure, chemistry, Design synthesis, Drug Design, Molecular Medicine
Abstract

Guided by co-crystal structures of compounds 15, 22 and 30, an SBDD approach led to the discovery of the 6-methyl pyridone series as a novel class of GKAs that potently activate GK in enzyme and cell assays. Anti-diabetic OGTT efficacy was demonstrated with 54 in a mouse model of type 2 diabetes.

Published
2013

4. Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)

Author

Yasuyoshi Arikawa, Pamela Farrell, Betty Lam, Lihong Shi, Zhe Nie, Jones Benjamin, Jonathan Zalevsky, Takahashi Masashi, Victoria A. Feher, Isaac Hoffman, Joshua Cramlett, Corey Wyrick, Hiroshi Miyake, Jennifer Matuszkiewicz, Joanne Miura, Ron de Jong, Charles E. Grimshaw, Jason Yano, Qing Dong, Srinivasa Reddy Natala, Ewan Taylor, and Andrew John Jennings

Subjects
0301 basic medicine, Clinical Biochemistry, Pharmaceutical Science, Syk, Antineoplastic Agents, Biochemistry, 03 medical and health sciences, Mice, Structure-Activity Relationship, 0302 clinical medicine, Mediator, Cell Line, Tumor, Drug Discovery, medicine, Animals, Humans, Syk Kinase, Molecular Biology, Protein Kinase Inhibitors, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, Drug discovery, Cell growth, Organic Chemistry, Neoplasms, Experimental, medicine.disease, Pyrrolidinones, Lymphoma, Mice, Inbred C57BL, Haematopoiesis, Leukemia, 030104 developmental biology, Pyrimidines, 030220 oncology & carcinogenesis, Cancer research, Molecular Medicine, Nivolumab, Drug Screening Assays, Antitumor
Abstract

Spleen Tyrosine Kinase (SYK) is a non-receptor cytoplasmic tyrosine kinase that is primarily expressed in hematopoietic cells. SYK is a key mediator for a variety of inflammatory cells, including B cells, mast cells, macrophages and neutrophils and therefore, an attractive approach for treatment of both inflammatory diseases and oncology indications. Using in house co-crystal structure information, and structure-based drug design, we designed and optimized a novel series of heteroaromatic pyrrolidinone SYK inhibitors resulting in the selection of the development candidate TAK-659. TAK-659 is currently undergoing Phase I clinical trials for advanced solid tumor and lymphoma malignancies, a Phase Ib study in advanced solid tumors in combination with nivolumab, and PhIb/II trials for relapsed/refractory AML.

Published
2016

5. Correction to 'Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure'

Author

Erica L. Bradshaw-Pierce, Mark Sabat, Xiaolun Wang, Jason Pickens, Marion Lanier, Zacharia Cheruvallath, Simone V. Bigi, Derek C. Cole, Jacques Ermolieff, Petro Halkowycz, Douglas R. Dougan, Alison Chambers, Haixia Wang, Anthony Ivetac, Tyhonas John, Joanne Miura, Christopher McBride, Evan Nunez, Aki Hirokawa, Tony Gibson, and Steve Swann

Subjects
0301 basic medicine, business.industry, Computer science, Organic Chemistry, Machine learning, computer.software_genre, medicine.disease, 01 natural sciences, Biochemistry, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, 03 medical and health sciences, 030104 developmental biology, Text mining, Heart failure, Drug Discovery, medicine, Structure based, Artificial intelligence, business, computer
Abstract

[This corrects the article DOI: 10.1021/acsmedchemlett.6b00481.].

Published
2017

6. Synthesis and Structure of Asymmetric Bis(sulfonamide) Based Copper(II) Complexes: Influence of Diastereomeric Interactions in the Solid State

Author

Chao-Kang Lee, Fernando Ortega, Patrick J. Walsh, Gerardo Aguirre, Joseph W. Ziller, Alaganandan Nanthakumar, Joanne Miura, and Sandra Diltz

Subjects
chemistry.chemical_classification, Chemistry, Ligand, Stereochemistry, Solid-state, Diastereomer, chemistry.chemical_element, Copper, Sulfonamide, Inorganic Chemistry, chemistry.chemical_compound, Monomer, Polymer chemistry, Physical and Theoretical Chemistry
Abstract

The new bis(sulfonamide) bis(pyridyl) ligand 1 readily binds to copper(II) in a tetradentate fashion giving monomeric, dimeric, and polymeric complexes. The solid state structures of these compounds were found to depend on the use of racemic vs resolved ligand.

Published
1999

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