[HTML][HTML] Raising HDL cholesterol without inducing hepatic steatosis and hypertriglyceridemia by a selective LXR modulator

…, S Zondlo, S Gibbs, D Cromley, VP Hosagrahara… - Journal of lipid …, 2004 - ASBMB
Liver X receptors (LXRs) are ligand-activated transcription factors that belong to the nuclear
receptor superfamily. LXRs activate transcription of a spectrum of genes that regulate …

Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis

…, V Balasubramanian, VP Hosagrahara… - Journal of medicinal …, 2017 - ACS Publications
The approval of bedaquiline to treat tuberculosis has validated adenosine triphosphate (ATP)
synthase as an attractive target to kill Mycobacterium tuberculosis (Mtb). Herein, we report …

Concise review of the cytochrome P 450 s and their roles in toxicology

…, RP Remmel, VP Hosagrahara - Toxicological Sciences, 1999 - hero.epa.gov
BIOSIS COPYRIGHT: BIOL ABS. RRM JOURNAL ARTICLE MAMMAL HUMAN CYTOCHROME
P450 GENE FAMILY POLYMORPHISM CYTOCHROME P450 ENZYMES SUBSTRATE …

Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity

…, SS Rudrapatna, VP Hosagrahara… - Journal of medicinal …, 2014 - ACS Publications
A novel pyrazolopyridone class of inhibitors was identified from whole cell screening against
Mycobacterium tuberculosis (Mtb). The series exhibits excellent bactericidality in vitro, …

Functional analysis of human microsomal epoxide hydrolase genetic variants

VP Hosagrahara, AE Rettie, C Hassett… - Chemico-biological …, 2004 - Elsevier
Human microsomal epoxide hydrolase (EPHX1) is active in the metabolism of many potentially
carcinogenic or otherwise genotoxic epoxides, such as those derived from the oxidation …

The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 …

…, LA Hardegger, VP Hosagrahara… - Journal of medicinal …, 2018 - ACS Publications
A noninvasive topical ocular therapy for the treatment of neovascular or “wet” age-related
macular degeneration would provide a patient administered alternative to the current standard …

[PDF][PDF] Reactivity of mefenamic acid 1-o-acyl glucuronide with proteins in vitro and ex vivo.

KA McGurk, RP Remmel, VP Hosagrahara… - Drug metabolism and …, 1996 - Citeseer
Mefenamic acid is a nonsteroidal anti-inflammatory drug cornrnonly used in analgesia. The
use of this drug has been irnplicated in several cases of nephrotoxicity including acute renal …

Discovery of oral VEGFR-2 inhibitors with prolonged ocular retention that are efficacious in models of wet age-related macular degeneration

…, F Liu, VP Hosagrahara, W Lee, P Tarsa… - Journal of Medicinal …, 2015 - ACS Publications
The benefit of intravitreal anti-VEGF therapy in treating wet age-related macular degeneration
(AMD) is well established. Identification of VEGFR-2 inhibitors with optimal ADME …

Scaffold morphing leading to evolution of 2, 4-diaminoquinolines and aminopyrazolopyrimidines as inhibitors of the ATP synthesis pathway

…, P Iyer, K Mukherjee, VP Hosagrahara… - …, 2016 - pubs.rsc.org
The success of bedaquiline as an anti-tubercular agent for the treatment of multidrug-resistant
tuberculosis has validated the ATP synthesis pathway and in particular ATP synthase as …

Identification and mitigation of a reactive metabolite liability associated with aminoimidazoles

…, SP Hameed, VK Ahuja, VP Hosagrahara - Chemical Research …, 2014 - ACS Publications
Reactive metabolites (RMs) have been implicated as causal factors in many drug-associated
idiosyncratic toxicities. This study aims at identification and mitigation of an RM liability …