Výsledky vyhledávání - "Gary P. Hingorani"

Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator

Autor: Scott Alan Pratt, Patrice Lee, Thomas Daniel Aicher, John Fischer, Kevin Ronald Condroski, Brian R. Baer, Boyd Steven A, Mark D. Chicarelli, Walter C. Voegtli, Walter E. DeWolf, Francis X. Sullivan, Eli M. Wallace, Nickolas A. Neitzel, Lance A. Williams, Ronald Jay Hinklin, Turner Timothy M, Ajay Singh, Gary P. Hingorani, Michele Frank

Publikováno v: Bioorganicmedicinal chemistry. 28(1)

Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is also responsible for reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to hav

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ede6ef02815e56689c6fa169c7a73d2
https://pubmed.ncbi.nlm.nih.gov/31818630

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An In Vitro, High Throughput, Seven CYP Cocktail Inhibition Assay for the Evaluation of New Chemical Entities Using LC-MS/MS

Autor: Jennifer N. Otten, Gary P. Hingorani, Dylan P. Hartley, Scott D. Kragerud, Ronald B. Franklin

Publikováno v: Drug Metabolism Letters. 5:17-24

A validated method for the simultaneous characterization of xenobiotic compound-mediated inhibition of seven major cytochrome P450 (CYP) enzymes in pooled human liver microsomes through the use of specific CYP probe substrates (cocktail assay) with l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::031046a253641a13252d3775b9d601c3
https://doi.org/10.2174/187231211794455235

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Preclinical Characteristics of the Hepatitis C Virus NS3/4A Protease Inhibitor ITMN-191 (R7227)

Publikováno v: Antimicrobial Agents and Chemotherapy. 52:4432-4441

Future treatments for chronic hepatitis C virus (HCV) infection are likely to include agents that target viral components directly. Here, the preclinical characteristics of ITMN-191, a peptidomimetic inhibitor of the NS3/4A protease of HCV, are descr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9981ec4b6c65bf78b0076564bdd6d18a
https://doi.org/10.1128/aac.00699-08

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Structure-activity relationships in a series of monocyclic endothelin analogues

Autor: Gary P. Hingorani, Wayne L. Cody, John X. He, David T. Dudley, P. L. DePue, E. E. Reynolds, Annette Marian Doherty, Stephen T. Rapundalo, Kristen E. Hill

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:567-572

Monocyclic fragment analogues of endothelin-1 (ET-1) were prepared to explore the importance of the bicyclic structure of ET-1 to its binding affinity and functional activity. Most of the monocyclic analogues prepared showed low micro to high nanomol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::97f229e6d121c3bbe647943d88029b00
https://doi.org/10.1016/s0960-894x(01)80156-6

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Simultaneous assessment of cytochrome P450 activity in cultured human hepatocytes for compound-mediated induction of CYP3A4, CYP2B6, and CYP1A2

Autor: Dylan P. Hartley, Jennifer N. Otten, Gary P. Hingorani, Susan P. Rhodes, Ronald B. Franklin

Publikováno v: Journal of pharmacological and toxicological methods. 63(3)

Introduction The human nuclear receptors pregnane X receptor (PXR), constitutive androstane receptor (CAR), and aryl hydrocarbon receptor ( Ah R) are known to regulate gene expression of the cytochrome P450 (CYP) enzymes, 3A4, 2B6, and 1A2, respectiv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87e0f32b9b28dfea14608fff6528a600
https://pubmed.ncbi.nlm.nih.gov/21111054

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Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones

Autor: Tammie C. Yeh, Gregory K. Poch, Patrice Lee, Jennifer N. Otten, Joseph P. Lyssikatos, Rich Woessner, Gary P. Hingorani, James D. Winkler, Kevin Koch, Jeongbeob Seo, Michele Perrier, Michelle Goyette Livingston, Heidi Jarski, Hong Woon Yang, Vivienne Marsh, Eli M. Wallace, James F. Blake

Publikováno v: Journal of medicinal chemistry. 49(2)

The role of MEK 1,2 in cancer tumorgenesis has been clearly demonstrated preclinically, and two selective inhibitors are currently undergoing clinical evaluation to determine their role in the human disease. We have discovered 4-(4-bromo-2-fluorophen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::574974bbed237e9e30f865e697503a6c
https://pubmed.ncbi.nlm.nih.gov/16420026

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Structure-Activity Studies of the C-Terminal Region of the Endothelins and the Sarafotoxins

Autor: N. L. Leitz, P. L. DePue, D G Taylor, M. D. Taylor, Gary P. Hingorani, Annette Marian Doherty, Stephen T. Rapundalo, Robert L. Panek, Wayne L. Cody, Terry C. Major

Publikováno v: Journal of Cardiovascular Pharmacology. 17:S59-61

Peptides corresponding to the C-terminal 16-21 hexapeptide of the endothelins (-His-Leu-Asp-Ile-Ile-Trp) and sarafotoxins (a-c) (-His-Gln-Asp-Val-Ile-Trp) were prepared to study the role of the individual amino acids in receptor recognition and activ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::616742eef5cc05834def0f3fa36454a1
https://doi.org/10.1097/00005344-199100177-00016

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