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16 results
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Benzylic oxidation of gemfibrozil-1-O-beta-glucuronide by P450 2C8 leads to heme alkylation and irreversible inhibition.
Baer BR, DeLisle RK, Allen A. Baer BR, et al. Chem Res Toxicol. 2009 Jul;22(7):1298-309. doi: 10.1021/tx900105n. Chem Res Toxicol. 2009. PMID: 19445523
Time-dependent inactivation of P450 3A4 by raloxifene: identification of Cys239 as the site of apoprotein alkylation.
Baer BR, Wienkers LC, Rock DA. Baer BR, et al. Chem Res Toxicol. 2007 Jun;20(6):954-64. doi: 10.1021/tx700037e. Epub 2007 May 12. Chem Res Toxicol. 2007. PMID: 17497897
Sites of covalent attachment of CYP4 enzymes to heme: evidence for microheterogeneity of P450 heme orientation.
Baer BR, Schuman JT, Campbell AP, Cheesman MJ, Nakano M, Moguilevsky N, Kunze KL, Rettie AE. Baer BR, et al. Biochemistry. 2005 Oct 25;44(42):13914-20. doi: 10.1021/bi051267j. Biochemistry. 2005. PMID: 16229480
Bioactivation of 4-ipomeanol by CYP4B1: adduct characterization and evidence for an enedial intermediate.
Baer BR, Rettie AE, Henne KR. Baer BR, et al. Chem Res Toxicol. 2005 May;18(5):855-64. doi: 10.1021/tx0496993. Chem Res Toxicol. 2005. PMID: 15892579
Discovery of 2-pyridylureas as glucokinase activators.
Hinklin RJ, Aicher TD, Anderson DA, Baer BR, Boyd SA, Condroski KR, DeWolf WE Jr, Kraser CF, McVean M, Rhodes SP, Sturgis HL, Voegtli WC, Williams L, Houze JB. Hinklin RJ, et al. Among authors: baer br. J Med Chem. 2014 Oct 9;57(19):8180-6. doi: 10.1021/jm501204z. Epub 2014 Sep 17. J Med Chem. 2014. PMID: 25203462
CYP4B1: an enigmatic P450 at the interface between xenobiotic and endobiotic metabolism.
Baer BR, Rettie AE. Baer BR, et al. Drug Metab Rev. 2006;38(3):451-76. doi: 10.1080/03602530600688503. Drug Metab Rev. 2006. PMID: 16877261 Review.
Covalent heme binding to CYP4B1 via Glu310 and a carbocation porphyrin intermediate.
Zheng YM, Baer BR, Kneller MB, Henne KR, Kunze KL, Rettie AE. Zheng YM, et al. Among authors: baer br. Biochemistry. 2003 Apr 22;42(15):4601-6. doi: 10.1021/bi020667t. Biochemistry. 2003. PMID: 12693958
Mechanism of formation of the ester linkage between heme and Glu310 of CYP4B1: 18O protein labeling studies.
Baer BR, Kunze KL, Rettie AE. Baer BR, et al. Biochemistry. 2007 Oct 16;46(41):11598-605. doi: 10.1021/bi701064b. Epub 2007 Sep 19. Biochemistry. 2007. PMID: 17880109 Free PMC article.
Rabbit CYP4B1 engineered for high-level expression in Escherichia coli: ligand stabilization and processing of the N-terminus and heme prosthetic group.
Cheesman MJ, Baer BR, Zheng YM, Gillam EM, Rettie AE. Cheesman MJ, et al. Among authors: baer br. Arch Biochem Biophys. 2003 Aug 1;416(1):17-24. doi: 10.1016/s0003-9861(03)00278-9. Arch Biochem Biophys. 2003. PMID: 12859977
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.
Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB. Du X, et al. Among authors: baer br. ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25516785 Free PMC article.
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