Stearns RA - Search Results

1

Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques.

Samuel K, Yin W, Stearns RA, Tang YS, Chaudhary AG, Jewell JP, Lanza T Jr, Lin LS, Hagmann WK, Evans DC, Kumar S. Samuel K, et al. Among authors: stearns ra. J Mass Spectrom. 2003 Feb;38(2):211-21. doi: 10.1002/jms.434. J Mass Spectrom. 2003. PMID: 12577288

2

Extrapolation of diclofenac clearance from in vitro microsomal metabolism data: role of acyl glucuronidation and sequential oxidative metabolism of the acyl glucuronide.

Kumar S, Samuel K, Subramanian R, Braun MP, Stearns RA, Chiu SH, Evans DC, Baillie TA. Kumar S, et al. Among authors: stearns ra. J Pharmacol Exp Ther. 2002 Dec;303(3):969-78. doi: 10.1124/jpet.102.038992. J Pharmacol Exp Ther. 2002. PMID: 12438516

3

A novel P450-catalyzed transformation of the 2,2,6,6-tetramethyl piperidine moiety to a 2,2-dimethyl pyrrolidine in human liver microsomes: characterization by high resolution quadrupole-time-of-flight mass spectrometry and 1H-NMR.

Yin W, Doss GA, Stearns RA, Chaudhary AG, Hop CE, Franklin RB, Kumar S. Yin W, et al. Among authors: stearns ra. Drug Metab Dispos. 2003 Feb;31(2):215-23. doi: 10.1124/dmd.31.2.215. Drug Metab Dispos. 2003. PMID: 12527703

4

N-acetylation of the glutamate residue of intact glutathione conjugates in rats: a novel pathway for the metabolic processing of thiol adducts of xenobiotics.

Yin W, Doss GA, Stearns RA, Kumar S. Yin W, et al. Among authors: stearns ra. Drug Metab Dispos. 2004 Jan;32(1):43-8. doi: 10.1124/dmd.32.1.43. Drug Metab Dispos. 2004. PMID: 14709619

5

Conversion of the 2,2,6,6-tetramethylpiperidine moiety to a 2,2-dimethylpyrrolidine by cytochrome P450: evidence for a mechanism involving nitroxide radicals and heme iron.

Yin W, Mitra K, Stearns RA, Baillie TA, Kumar S. Yin W, et al. Among authors: stearns ra. Biochemistry. 2004 May 11;43(18):5455-66. doi: 10.1021/bi035944q. Biochemistry. 2004. PMID: 15122911

6

Metabolic activation of fluoropyrrolidine dipeptidyl peptidase-IV inhibitors by rat liver microsomes.

Xu S, Zhu B, Teffera Y, Pan DE, Caldwell CG, Doss G, Stearns RA, Evans DC, Beconi MG. Xu S, et al. Among authors: stearns ra. Drug Metab Dispos. 2005 Jan;33(1):121-30. doi: 10.1124/dmd.104.001842. Epub 2004 Oct 14. Drug Metab Dispos. 2005. PMID: 15486074

7

Metabolic activation of a 1,3-disubstituted piperazine derivative: evidence for a novel ring contraction to an imidazoline.

Doss GA, Miller RR, Zhang Z, Teffera Y, Nargund RP, Palucki B, Park MK, Tang YS, Evans DC, Baillie TA, Stearns RA. Doss GA, et al. Among authors: stearns ra. Chem Res Toxicol. 2005 Feb;18(2):271-6. doi: 10.1021/tx049711r. Chem Res Toxicol. 2005. PMID: 15720132

8

Evidence for the bioactivation of zomepirac and tolmetin by an oxidative pathway: identification of glutathione adducts in vitro in human liver microsomes and in vivo in rats.

Chen Q, Doss GA, Tung EC, Liu W, Tang YS, Braun MP, Didolkar V, Strauss JR, Wang RW, Stearns RA, Evans DC, Baillie TA, Tang W. Chen Q, et al. Among authors: stearns ra. Drug Metab Dispos. 2006 Jan;34(1):145-51. doi: 10.1124/dmd.105.004341. Epub 2005 Oct 26. Drug Metab Dispos. 2006. PMID: 16251255

9

The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.

Lin LS, Kopka IE, Mumford RA, Magriotis PA, Lanza T Jr, Durette PL, Kamenecka T, Young DN, de Laszlo SE, McCauley E, Riper GV, Kidambi U, Egger LA, Tong X, Lyons K, Vincent S, Stearns R, Colletti A, Teffera Y, Fenyk-Melody J, Schmidt JA, MacCoss M, Hagmann WK. Lin LS, et al. Among authors: stearns r. Bioorg Med Chem Lett. 2002 Feb 25;12(4):611-4. doi: 10.1016/s0960-894x(01)00818-6. Bioorg Med Chem Lett. 2002. PMID: 11844683

10

Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats.

Tang W, Stearns RA, Chen Q, Bleasby K, Teffera Y, Colletti A, Hafey M, Evers R, Dean DC, Magriotis PA, Lanza TJ, Lin LS, Hagmann WK, Baillie TA. Tang W, et al. Among authors: stearns ra. Xenobiotica. 2008 Feb;38(2):223-37. doi: 10.1080/00498250701744682. Xenobiotica. 2008. PMID: 18197560

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