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Items: 14

1.

The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients.

Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue JY, Gatto S, Fernandez-Banet J, Pavlicek A, Velastegui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Janne PA, Olson P, Christensen JG.

Cancer Discov. 2019 Oct 28. pii: CD-19-1167. doi: 10.1158/2159-8290.CD-19-1167. [Epub ahead of print]

PMID:
31658955
2.

Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.

Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG.

ACS Med Chem Lett. 2018 Nov 7;9(12):1230-1234. doi: 10.1021/acsmedchemlett.8b00382. eCollection 2018 Dec 13.

PMID:
30613331
3.

The Crystal Structure of Cytochrome P450 4B1 (CYP4B1) Monooxygenase Complexed with Octane Discloses Several Structural Adaptations for ω-Hydroxylation.

Hsu MH, Baer BR, Rettie AE, Johnson EF.

J Biol Chem. 2017 Mar 31;292(13):5610-5621. doi: 10.1074/jbc.M117.775494. Epub 2017 Feb 6.

4.

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.

ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11.

5.

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.

J Med Chem. 2014 Oct 9;57(19):8180-6. doi: 10.1021/jm501204z. Epub 2014 Sep 17.

PMID:
25203462
6.

Characterization of a novel glucokinase activator in rat and mouse models.

Lu M, Li P, Bandyopadhyay G, Lagakos W, Dewolf WE Jr, Alford T, Chicarelli MJ, Williams L, Anderson DA, Baer BR, McVean M, Conn M, Véniant MM, Coward P.

PLoS One. 2014 Feb 12;9(2):e88431. doi: 10.1371/journal.pone.0088431. eCollection 2014.

7.

Benzylic oxidation of gemfibrozil-1-O-beta-glucuronide by P450 2C8 leads to heme alkylation and irreversible inhibition.

Baer BR, DeLisle RK, Allen A.

Chem Res Toxicol. 2009 Jul;22(7):1298-309. doi: 10.1021/tx900105n.

PMID:
19445523
8.

Mechanism of formation of the ester linkage between heme and Glu310 of CYP4B1: 18O protein labeling studies.

Baer BR, Kunze KL, Rettie AE.

Biochemistry. 2007 Oct 16;46(41):11598-605. Epub 2007 Sep 19.

9.

Time-dependent inactivation of P450 3A4 by raloxifene: identification of Cys239 as the site of apoprotein alkylation.

Baer BR, Wienkers LC, Rock DA.

Chem Res Toxicol. 2007 Jun;20(6):954-64. Epub 2007 May 12.

PMID:
17497897
10.

CYP4B1: an enigmatic P450 at the interface between xenobiotic and endobiotic metabolism.

Baer BR, Rettie AE.

Drug Metab Rev. 2006;38(3):451-76. Review.

PMID:
16877261
11.

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.

Biochemistry. 2005 Oct 25;44(42):13914-20.

PMID:
16229480
12.

Bioactivation of 4-ipomeanol by CYP4B1: adduct characterization and evidence for an enedial intermediate.

Baer BR, Rettie AE, Henne KR.

Chem Res Toxicol. 2005 May;18(5):855-64.

PMID:
15892579
13.

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.

Arch Biochem Biophys. 2003 Aug 1;416(1):17-24.

PMID:
12859977
14.

Covalent heme binding to CYP4B1 via Glu310 and a carbocation porphyrin intermediate.

Zheng YM, Baer BR, Kneller MB, Henne KR, Kunze KL, Rettie AE.

Biochemistry. 2003 Apr 22;42(15):4601-6.

PMID:
12693958

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