User profiles for G A Doss
George A DossPrincipal Scientist, Merck & Co, Inc. Verified email at merck.com Cited by 4751 |
Metabolic activation of diclofenac by human cytochrome P450 3A4: role of 5-hydroxydiclofenac
…, MR Marchick, MR Davis, GA Doss… - Chemical research in …, 1999 - ACS Publications
Cytochrome P450 2C11 in rats was recently found to metabolize diclofenac into a highly
reactive product that covalently bound to this enzyme before it could diffuse away and react with …
reactive product that covalently bound to this enzyme before it could diffuse away and react with …
Studies on cytochrome P-450-mediated bioactivation of diclofenac in rats and in human hepatocytes: identification of glutathione conjugated metabolites
…, DC Dean, J Pang, KH Leung, GA Doss… - Drug Metabolism and …, 1999 - ASPET
The nonsteroidal anti-inflammatory drug diclofenac causes a rare but potentially fatal
hepatotoxicity that may be associated with the formation of reactive metabolites. In this study, three …
hepatotoxicity that may be associated with the formation of reactive metabolites. In this study, three …
Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation
Q Chen, JS Ngui, GA Doss, RW Wang… - Chemical research in …, 2002 - ACS Publications
Raloxifene is a selective estrogen receptor modulator which is effective in the treatment of
osteoporosis in postmenopausal women. We report herein that cytochrome P450 (P450)3A4 …
osteoporosis in postmenopausal women. We report herein that cytochrome P450 (P450)3A4 …
Metabolic profiles of montelukast sodium (Singulair), a potent cysteinyl leukotriene1 receptor antagonist, in human plasma and bile
…, C Dufresne, RR Miller, BH Arison, GA Doss… - Drug metabolism and …, 1997 - ASPET
Montelukast sodium [1-{[(1(R)-(3-(2-(7-chloro-2-quinolinyl)-(E)- ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio]methyl}cyclopropylacetic
acid sodium salt] (MK-476, …
acid sodium salt] (MK-476, …
Addressing metabolic activation as an integral component of drug design
GA Doss, TA Baillie - Drug metabolism reviews, 2006 - Taylor & Francis
… 3 ) exhibited high levels of covalent binding in both rat and human liver microsomes (Doss
et al., Citation2005). The binding was attenuated by GSH, but a search for typical GSH …
et al., Citation2005). The binding was attenuated by GSH, but a search for typical GSH …
Bioactivation of diclofenac via benzoquinone imine intermediates—identification of urinary mercapturic acid derivatives in rats and humans
…, JS Ngui, PR Griffin, MP Braun, GA Doss… - Drug metabolism and …, 2001 - ASPET
The metabolism of diclofenac has been reported to produce reactive benzoquinone imine
intermediates. We describe the identification of mercapturic acid derivatives of diclofenac in …
intermediates. We describe the identification of mercapturic acid derivatives of diclofenac in …
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of …
…, B Zhang, J Wu, X Zhang, GA Doss… - Bioorganic & medicinal …, 2007 - Elsevier
Molecular modeling was used to design a rigid analog of sitagliptin 1. The X-ray crystal
structure of sitagliptin bound to DPP-4 suggested that the central β-amino butyl amide moiety …
structure of sitagliptin bound to DPP-4 suggested that the central β-amino butyl amide moiety …
Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
…, RM Sisco, H Dong, KA Lyons, H He, GA Doss… - Bioorganic & medicinal …, 2005 - Elsevier
A series of β-aminoacylpiperidines bearing various fused five-membered heterocyclic rings
was synthesized as dipeptidyl peptidase IV inhibitors. Potent and relatively selective …
was synthesized as dipeptidyl peptidase IV inhibitors. Potent and relatively selective …
The metabolism of DuP 753, a nonpeptide angiotensin II receptor antagonist, by rat, monkey, and human liver slices.
RA Stearns, RR Miller, GA Doss, PK Chakravarty… - Drug metabolism and …, 1992 - ASPET
The in vitro metabolism of DuP 753, a novel nonpeptide angiotensin II receptor antagonist,
has been investigated in incubations with liver slice preparations from rats, monkeys and …
has been investigated in incubations with liver slice preparations from rats, monkeys and …
Comparison of subcutaneous dexmedetomidine–midazolam versus alfaxalone–midazolam sedation in leopard geckos (Eublepharis macularius)
Objective To compare dexmedetomidine–midazolam with alfaxalone–midazolam for
sedation in leopard geckos (Eublepharis macularius). Study design Prospective, randomized, …
sedation in leopard geckos (Eublepharis macularius). Study design Prospective, randomized, …