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Your search keyword '"Kern G"' showing total 333 results
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333 results on '"Kern G"'

1. Verteilung, Messung und Einrichtung

Author

E. Schilling, F. Kuckuk, G. Kern, G. Schneider, W. Eisele, E. Schilling, F. Kuckuk, G. Kern, G. Schneider, W. Eisele and E. Schilling, F. Kuckuk, G. Kern, G. Schneider, W. Eisele, E. Schilling, F. Kuckuk, G. Kern, G. Schneider, W. Eisele

Published
2019

2. An MTP Inhibitor that Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits

Author

Wetterau, John R., Gregg, Richard E., Harrity, Thomas W., Arbeeny, Cynthia, Cap, Michael, Connolly, Fergal, Chu, Ching-Hsuen, George, Rocco J., Gordon, David A., Jamil, Haris, Jolibois, Kern G., Kunselman, Lori K., Lan, Shih-Jung, Maccagnan, Thomas J., Ricci, Beverly, Yan, Mujing, Young, Douglas, Chen, Ying, Fryszman, Olga M., Musial, Christa L., Poss, Michael A., Robl, Jeffrey A., Simpkins, Ligaya M., Slusarchyk, William A., Sulsky, Richard, Taunk, Prakash, Magnin, David R., Tino, Joseph A., Lawrence, R. Michael, Dickson, John K., and Biller, Scott A.

Published
1998

34. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP

Author

John R. Wetterau, Thomas Harrity, Richard B. Sulsky, Jeffrey A. Robl, Kern G. Jolibois, Fergal Connolly, Scott A. Biller, and Lori Kunselman

Subjects
Male, medicine.drug_class, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Carboxamide, Stereoisomerism, In Vitro Techniques, Biochemistry, Chemical synthesis, Structure-Activity Relationship, chemistry.chemical_compound, Cricetinae, Drug Discovery, medicine, Organic chemistry, Animals, Humans, Structure–activity relationship, Molecular Biology, Chemistry, Organic Chemistry, Biological activity, General Medicine, Amides, Cyclic P-Oxides, Carrier protein, Microsome, Molecular Medicine, Benzimidazoles, Piperidine, Carrier Proteins
Abstract

5-Carboxamido-1,3,2-dioxaphosphorinanes have been identified as potent inhibitors of microsomal triglyceride-transfer protein. The 1,3,2-dioxaphosphorine functionality acted as a neutral and stable replacement for piperidine and piperidine N-oxide.

Published
2004

36. An MTP Inhibitor That Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits

Author

Douglas Young, Michael Cap, Olga M. Fryszman, Thomas J. Maccagnan, Mujing Yan, John R. Wetterau, Prakash Taunk, Shih-Jung Lan, Richard B. Sulsky, Michael A. Poss, William A. Slusarchyk, Fergal Connolly, Jeffrey A. Robl, Joseph A. Tino, Kern G. Jolibois, R.J. George, Beverly Ricci, Scott A. Biller, David R. Magnin, Janette V. H. Logan, Thomas Harrity, Lori Kunselman, Ying Chen, R. Michael Lawrence, Jamil Haris, C.M. Arbeeny, John K. Dickson, Christa L. Musial, Ligaya M. Simpkins, Ching-Hsuen Chu, David A. Gordon, and Richard E. Gregg

Subjects
medicine.medical_specialty, Apolipoprotein B, Lipoproteins, Drug Evaluation, Preclinical, Hyperlipidemias, Familial hypercholesterolemia, Microsomal triglyceride transfer protein, Hyperlipoproteinemia Type II, Mice, chemistry.chemical_compound, Piperidines, In vivo, Cricetinae, Internal medicine, Tumor Cells, Cultured, medicine, Animals, Humans, Secretion, Aspartate Aminotransferases, Triglycerides, Apolipoproteins B, Fluorenes, Multidisciplinary, Dose-Response Relationship, Drug, biology, Triglyceride, Abetalipoproteinemia, Alanine Transaminase, medicine.disease, Lipids, Rats, Disease Models, Animal, Cholesterol, Endocrinology, Liver, chemistry, Drug Design, biology.protein, lipids (amino acids, peptides, and proteins), Rabbits, Carrier Proteins, Lipoprotein
Abstract

Patients with abetalipoproteinemia, a disease caused by defects in the microsomal triglyceride transfer protein (MTP), do not produce apolipoprotein B–containing lipoproteins. It was hypothesized that small molecule inhibitors of MTP would prevent the assembly and secretion of these atherogenic lipoproteins. To test this hypothesis, two compounds identified in a high-throughput screen for MTP inhibitors were used to direct the synthesis of a highly potent MTP inhibitor. This molecule (compound 9 ) inhibited the production of lipoprotein particles in rodent models and normalized plasma lipoprotein levels in Watanabe-heritable hyperlipidemic (WHHL) rabbits, which are a model for human homozygous familial hypercholesterolemia. These results suggest that compound 9 , or derivatives thereof, has potential applications for the therapeutic lowering of atherogenic lipoprotein levels in humans.

Published
1998

38. Orally Active Squalene Synthase Inhibitors: Bis((acyloxy)alkyl) Prodrugs of the α-Phosphonosulfonic Acid Moiety

Author

J. K. Rinehart, Shih-Jung Lan, Kern G. Jolibois, Richard E. Gregg, Lori Kunselman, John K. Dickson, D. C. Hsieh, Edward W. Petrillo, J. W. Hillyer, Stephen S. Kalinowski, T. W. Harrity, Kasim A. Mookhtiar, D. R. Magnin, Carl P. Ciosek, and Scott A. Biller

Subjects
chemistry.chemical_classification, Farnesyl-diphosphate farnesyltransferase, biology, Stereochemistry, Guinea Pigs, Administration, Oral, Ether, Prodrug, Chemical synthesis, Rats, chemistry.chemical_compound, Squalene, Farnesyl-Diphosphate Farnesyltransferase, chemistry, Enzyme inhibitor, Drug Discovery, biology.protein, Animals, Molecular Medicine, Moiety, Prodrugs, Enzyme Inhibitors, Sulfonic Acids, Alkyl, Hypolipidemic Agents
Published
1996

39. Evolution of the big O.

Author

Wright, K. and Kern, G.

Subjects
*SEX (Biology)
Abstract

Examines the reasons orgasms play a role in sex. Physical characteristics of orgasm; Difficulties in ascertaining orgasms in females; Why orgasm doesn't automatically occur at male ejaculation; Benefits of male and female orgasms; Orgasm as an adaptive behavior in females; Theory stating that female orgasm is a sexual byproduct; Benefits of lack of orgasms in females according to scientists.

Published
1992

43. Lipophilic 1,1-bisphosphonates are potent squalene synthase inhibitors and orally active cholesterol lowering agents in vivo

Author

R. M. Lawrence, Janette V. H. Logan, Eric M. Gordon, Carl P. Ciosek, Lori Kunselman, John K. Dickson, Kern G. Jolibois, K A Hamilton, Thomas Harrity, and D. R. Magnin

Subjects
chemistry.chemical_classification, Farnesyl-diphosphate farnesyltransferase, biology, Cholesterol, Cell Biology, Biochemistry, chemistry.chemical_compound, Squalene, Dolichol, Enzyme, chemistry, Biosynthesis, Enzyme inhibitor, biology.protein, medicine, lipids (amino acids, peptides, and proteins), Lovastatin, Molecular Biology, medicine.drug
Abstract

Squalene synthase catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene at the final branchpoint of the cholesterol biosynthetic pathway. We report herein that isoprenyl 1,1-bisphosphonates and related analogs are potent inhibitors of rat microsomal squalene synthase (I50 = 0.7-32 nM). In addition, members of this family are potent inhibitors of cholesterol biosynthesis in rats on intravenous and oral dosing, as well as cholesterol lowering agents in rats and hamsters. Significant inhibition of cholesterol biosynthesis in rats by lovastatin occurs with a concomitant inhibition of dolichol and coenzyme-Q9 synthesis. In contrast, bisphosphonate 4 has no effect on dolichol and coenzyme-Q9 biosynthesis in rats under conditions where cholesterol biosynthesis is > 90% inhibited.

Published
1993

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