G
George A. Doss
Researcher at Merck & Co.
Publications - 114
Citations - 3107
George A. Doss is an academic researcher from Merck & Co.. The author has contributed to research in topics: Metabolite & Glutathione. The author has an hindex of 31, co-authored 113 publications receiving 2998 citations. Previous affiliations of George A. Doss include National Institutes of Health & University of California, San Diego.
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Journal Article
Studies on Cytochrome P-450-Mediated Bioactivation of Diclofenac in Rats and in Human Hepatocytes: Identification of Glutathione Conjugated Metabolites
Wei Tang,Ralph A. Stearns,Stelvio M. Bandiera,Yong Zhang,Conrad E. Raab,Matthew P. Braun,Dennis C. Dean,Jianmei Pang,Kwan H. Leung,George A. Doss,John R. Strauss,Gloria Y. Kwei,Thomas H. Rushmore,Shuet Hing L Chiu,Thomas A. Baillie +14 more
TL;DR: The data suggest that diclofenac undergoes biotransformation to reactive metabolites in rats and that CYP isoforms of the 2B, 2C, and 3A subfamilies are involved in this bioactivation process.
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Metabolic activation of diclofenac by human cytochrome P450 3A4: role of 5-hydroxydiclofenac.
TL;DR: The results suggest that for appreciable P450-mediated bioactivation of diclofenac to occur in vivo, an individual may have to have both high activities of P450 3A4 and perhaps low activities of other enzymes that catalyze competing pathways of metabolism ofdicl ofenac.
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Omarigliptin (MK-3102): A Novel Long-Acting DPP-4 Inhibitor for Once-Weekly Treatment of Type 2 Diabetes.
Tesfaye Biftu,Ranabir SinhaRoy,Ping Chen,Xiaoxia Qian,Dennis Feng,Jeffrey T. Kuethe,Giovanna Scapin,Ying-Duo Gao,Youwei Yan,Davida Krueger,Annette Bak,George J. Eiermann,Jiafang He,Jason M. Cox,Jacqueline D. Hicks,Kathy Lyons,Huaibing He,Gino Salituro,Sharon Tong,Sangita B. Patel,George A. Doss,Aleksandr Petrov,Joseph K. Wu,Shiyao Sherrie Xu,Charles Sewall,Xiaoping Zhang,Bei Zhang,Nancy A. Thornberry,Ann E. Weber +28 more
TL;DR: MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate.
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Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation.
Qing Chen,Jason S. Ngui,George A. Doss,Regina W. Wang,Xiaoxin Cai,Frank P. DiNinno,Timothy A. Blizzard,Milton L. Hammond,Ralph A. Stearns,David C. Evans,Thomas A. Baillie,Wei Tang +11 more
TL;DR: Data indicate that P450 3A4-mediated bioactivation of raloxifene in vitro is accompanied by loss of enzyme activity, which is effective in the treatment of osteoporosis in postmenopausal women.
Journal Article
The metabolism of DuP 753, a nonpeptide angiotensin II receptor antagonist, by rat, monkey, and human liver slices.
Ralph A. Stearns,Randy R. Miller,George A. Doss,P. K. Chakravarty,Avery Rosegay,G. J. Gatto,Shuet-Hing Lee Chiu +6 more
TL;DR: The oxidative conversion to the carboxylic acid metabolite, along with the low level of glucuronidation observed in incubations with rat liver slices, may be responsible for the prolonged duration observed in vivo in the rat.