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Items: 1 to 20 of 86

1.

Reactive metabolite trapping screens and potential pitfalls: bioactivation of a homomorpholine and formation of an unstable thiazolidine adduct.

Lenz EM, Martin S, Schmidt R, Morin PE, Smith R, Weston DJ, Bayrakdarian M.

Chem Res Toxicol. 2014 Jun 16;27(6):968-80. doi: 10.1021/tx5000409. Epub 2014 Jun 5.

PMID:
24855970
2.

Bioactivation of isothiazoles: minimizing the risk of potential toxicity in drug discovery.

Teffera Y, Choquette D, Liu J, Colletti AE, Hollis LS, Lin MH, Zhao Z.

Chem Res Toxicol. 2010 Nov 15;23(11):1743-52. doi: 10.1021/tx100208k. Epub 2010 Sep 8.

PMID:
20825217
4.

Bioactivation of phencyclidine in rat and human liver microsomes and recombinant P450 2B enzymes: evidence for the formation of a novel quinone methide intermediate.

Driscoll JP, Kornecki K, Wolkowski JP, Chupak L, Kalgutkar AS, O'Donnell JP.

Chem Res Toxicol. 2007 Oct;20(10):1488-97. Epub 2007 Sep 25.

PMID:
17892269
5.

Bioactivation of a dihydropyrazole-1-carboxylic acid-(4-chlorophenyl amide) scaffold to a putative p-chlorophenyl isocyanate in rat liver microsomes and in vivo in rats.

Chen H, Zhang Y, Edmunds J, Bigge C, Mutlib A.

Chem Res Toxicol. 2008 May;21(5):1095-106. doi: 10.1021/tx7004019. Epub 2008 Apr 5.

PMID:
18393453
6.

NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine.

Zhao SX, Dalvie DK, Kelly JM, Soglia JR, Frederick KS, Smith EB, Obach RS, Kalgutkar AS.

Chem Res Toxicol. 2007 Nov;20(11):1649-57. Epub 2007 Oct 2.

PMID:
17907785
8.

In vitro metabolism of N-(5-chloro-2-methylphenyl)-N'-(2-methylpropyl)thiourea: species comparison and identification of a novel thiocarbamide-glutathione adduct.

Stevens GJ, Hitchcock K, Wang YK, Coppola GM, Versace RW, Chin JA, Shapiro M, Suwanrumpha S, Mangold BL.

Chem Res Toxicol. 1997 Jul;10(7):733-41.

PMID:
9250406
9.

Bioactivation of substituted thiophenes including α-chlorothiophene-containing compounds in human liver microsomes.

Chen W, Caceres-Cortes J, Zhang H, Zhang D, Humphreys WG, Gan J.

Chem Res Toxicol. 2011 May 16;24(5):663-9. doi: 10.1021/tx100386z. Epub 2011 Apr 13.

PMID:
21417487
10.

Cytochrome P450-mediated epoxidation of 2-aminothiazole-based AKT inhibitors: identification of novel GSH adducts and reduction of metabolic activation through structural changes guided by in silico and in vitro screening.

Subramanian R, Lee MR, Allen JG, Bourbeau MP, Fotsch C, Hong FT, Tadesse S, Yao G, Yuan CC, Surapaneni S, Skiles GL, Wang X, Wohlhieter GE, Zeng Q, Zhou Y, Zhu X, Li C.

Chem Res Toxicol. 2010 Mar 15;23(3):653-63. doi: 10.1021/tx900414g.

PMID:
20095585
11.

Bioactivation of flutamide metabolites by human liver microsomes.

Kang P, Dalvie D, Smith E, Zhou S, Deese A, Nieman JA.

Drug Metab Dispos. 2008 Jul;36(7):1425-37. doi: 10.1124/dmd.108.020370. Epub 2008 Apr 14.

12.

Thiolactone sulfoxides as new reactive metabolites acting as bis-electrophiles: implication in clopidogrel and prasugrel bioactivation.

Dansette PM, Levent D, Hessani A, Bertho G, Mansuy D.

Chem Res Toxicol. 2013 May 20;26(5):794-802. doi: 10.1021/tx400083b. Epub 2013 Apr 9.

PMID:
23527615
13.
14.

Bioactivation of benzylamine to reactive intermediates in rodents: formation of glutathione, glutamate, and peptide conjugates.

Mutlib AE, Dickenson P, Chen SY, Espina RJ, Daniels JS, Gan LS.

Chem Res Toxicol. 2002 Sep;15(9):1190-207.

PMID:
12230413
15.

Metabolism and bioactivation of 3-methylindole by human liver microsomes.

Yan Z, Easterwood LM, Maher N, Torres R, Huebert N, Yost GS.

Chem Res Toxicol. 2007 Jan;20(1):140-8.

PMID:
17226936
16.

Bioactivation of 2,3-diaminopyridine-containing bradykinin B1 receptor antagonists: irreversible binding to liver microsomal proteins and formation of glutathione conjugates.

Tang C, Subramanian R, Kuo Y, Krymgold S, Lu P, Kuduk SD, Ng C, Feng DM, Elmore C, Soli E, Ho J, Bock MG, Baillie TA, Prueksaritanont T.

Chem Res Toxicol. 2005 Jun;18(6):934-45.

PMID:
15962928
17.

2'-Deoxyguanosine as a surrogate trapping agent for DNA reactive drug metabolites.

Häkkinen MR, Laine JE, Juvonen RO, Auriola S, Häyrinen J, Pasanen M.

Toxicol Lett. 2011 Nov 10;207(1):34-41. doi: 10.1016/j.toxlet.2011.08.020. Epub 2011 Sep 2.

PMID:
21907773
18.

Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation.

Chen Q, Ngui JS, Doss GA, Wang RW, Cai X, DiNinno FP, Blizzard TA, Hammond ML, Stearns RA, Evans DC, Baillie TA, Tang W.

Chem Res Toxicol. 2002 Jul;15(7):907-14.

PMID:
12119000
19.

Mechanism of bioactivation and covalent binding of 2,4,6-trinitrotoluene.

Leung KH, Yao M, Stearns R, Chiu SH.

Chem Biol Interact. 1995 Jun 30;97(1):37-51.

PMID:
7767940
20.

Mass spectrometric characterization of protein adducts of multiple P450-dependent reactive intermediates of diclofenac to human glutathione-S-transferase P1-1.

Boerma JS, Dragovic S, Vermeulen NP, Commandeur JN.

Chem Res Toxicol. 2012 Nov 19;25(11):2532-41. doi: 10.1021/tx300334w. Epub 2012 Oct 10.

PMID:
22998212

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