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Items: 20

1.

Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor.

Zhuang L, Tice CM, Xu Z, Zhao W, Cacatian S, Ye YJ, Singh SB, Lindblom P, McKeever BM, Krosky PM, Zhao Y, Lala D, Kruk BA, Meng S, Howard L, Johnson JA, Bukhtiyarov Y, Panemangalore R, Guo J, Guo R, Himmelsbach F, Hamilton B, Schuler-Metz A, Schauerte H, Gregg R, McGeehan GM, Leftheris K, Claremon DA.

Bioorg Med Chem. 2017 Jul 15;25(14):3649-3657. doi: 10.1016/j.bmc.2017.04.033. Epub 2017 Apr 29.

PMID:
28528082
2.

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.

Tice CM, Noto PB, Fan KY, Zhao W, Lotesta SD, Dong C, Marcus AP, Zheng YJ, Chen G, Wu Z, Van Orden R, Zhou J, Bukhtiyarov Y, Zhao Y, Lipinski K, Howard L, Guo J, Kandpal G, Meng S, Hardy A, Krosky P, Gregg RE, Leftheris K, McKeever BM, Singh SB, Lala D, McGeehan GM, Zhuang L, Claremon DA.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):5044-5050. doi: 10.1016/j.bmcl.2016.08.089. Epub 2016 Aug 29.

PMID:
27599745
3.

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist.

Zheng Y, Zhuang L, Fan KY, Tice CM, Zhao W, Dong C, Lotesta SD, Leftheris K, Lindblom PR, Liu Z, Shimada J, Noto PB, Meng S, Hardy A, Howard L, Krosky P, Guo J, Lipinski K, Kandpal G, Bukhtiyarov Y, Zhao Y, Lala D, Van Orden R, Zhou J, Chen G, Wu Z, McKeever BM, McGeehan GM, Gregg RE, Claremon DA, Singh SB.

J Med Chem. 2016 Apr 14;59(7):3264-71. doi: 10.1021/acs.jmedchem.5b02029. Epub 2016 Mar 29.

PMID:
26990539
4.

Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists.

Lotesta SD, Marcus AP, Zheng Y, Leftheris K, Noto PB, Meng S, Kandpal G, Chen G, Zhou J, McKeever B, Bukhtiyarov Y, Zhao Y, Lala DS, Singh SB, McGeehan GM.

Bioorg Med Chem. 2016 Mar 15;24(6):1384-91. doi: 10.1016/j.bmc.2016.02.014. Epub 2016 Feb 9.

PMID:
26897089
5.

Regulation of sphingomyelin phosphodiesterase acid-like 3A gene (SMPDL3A) by liver X receptors.

Noto PB, Bukhtiyarov Y, Shi M, McKeever BM, McGeehan GM, Lala DS.

Mol Pharmacol. 2012 Oct;82(4):719-27. Epub 2012 Jul 18.

PMID:
22810003
6.

Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.

Jia L, Simpson RD, Yuan J, Xu Z, Zhao W, Cacatian S, Tice CM, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Bukhtiyarov Y, Johnson JA, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.

ACS Med Chem Lett. 2011 Aug 9;2(10):747-51. doi: 10.1021/ml200137x. eCollection 2011 Oct 13.

7.

Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11β-hydroxysteroid dehydrogenase type 1.

Xu Z, Tice CM, Zhao W, Cacatian S, Ye YJ, Singh SB, Lindblom P, McKeever BM, Krosky PM, Kruk BA, Berbaum J, Harrison RK, Johnson JA, Bukhtiyarov Y, Panemangalore R, Scott BB, Zhao Y, Bruno JG, Togias J, Guo J, Guo R, Carroll PJ, McGeehan GM, Zhuang L, He W, Claremon DA.

J Med Chem. 2011 Sep 8;54(17):6050-62. doi: 10.1021/jm2005354. Epub 2011 Aug 4.

PMID:
21786805
8.

Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.

Yuan J, Simpson RD, Zhao W, Tice CM, Xu Z, Cacatian S, Jia L, Flaherty PT, Guo J, Ishchenko A, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Panemangalore R, Bentley R, Doe CP, Harrison RK, McGeehan GM, Singh SB, Dillard LW, Baldwin JJ, Claremon DA.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4836-43. doi: 10.1016/j.bmcl.2011.06.043. Epub 2011 Jun 17.

PMID:
21741239
9.

Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1.

Tice CM, Zhao W, Krosky PM, Kruk BA, Berbaum J, Johnson JA, Bukhtiyarov Y, Panemangalore R, Scott BB, Zhao Y, Bruno JG, Howard L, Togias J, Ye YJ, Singh SB, McKeever BM, Lindblom PR, Guo J, Guo R, Nar H, Schuler-Metz A, Gregg RE, Leftheris K, Harrison RK, McGeehan GM, Zhuang L, Claremon DA.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6725-9. doi: 10.1016/j.bmcl.2010.08.142. Epub 2010 Sep 7.

PMID:
20864344
10.

Spirocyclic ureas: orally bioavailable 11 beta-HSD1 inhibitors identified by computer-aided drug design.

Tice CM, Zhao W, Xu Z, Cacatian ST, Simpson RD, Ye YJ, Singh SB, McKeever BM, Lindblom P, Guo J, Krosky PM, Kruk BA, Berbaum J, Harrison RK, Johnson JJ, Bukhtiyarov Y, Panemangalore R, Scott BB, Zhao Y, Bruno JG, Zhuang L, McGeehan GM, He W, Claremon DA.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):881-6. doi: 10.1016/j.bmcl.2009.12.082. Epub 2010 Jan 4.

PMID:
20064717
11.

Optimization of orally bioavailable alkyl amine renin inhibitors.

Xu Z, Cacatian S, Yuan J, Simpson RD, Jia L, Zhao W, Tice CM, Flaherty PT, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Bentley R, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):694-9. doi: 10.1016/j.bmcl.2009.11.066. Epub 2009 Dec 1.

PMID:
19959358
12.

Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.

Tice CM, Xu Z, Yuan J, Simpson RD, Cacatian ST, Flaherty PT, Zhao W, Guo J, Ishchenko A, Singh SB, Wu Z, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Müller D, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3541-5. doi: 10.1016/j.bmcl.2009.04.140. Epub 2009 May 5.

PMID:
19457666
13.

Purification and characterization of recombinant human renin for X-ray crystallization studies.

Wu Z, Cappiello MG, Scott BB, Bukhtiyarov Y, McGeehan GM.

BMC Biochem. 2008 Jun 26;9:19. doi: 10.1186/1471-2091-9-19.

14.

Cloning, characterization and site-directed mutagenesis of canine renin.

Bukhtiyarov Y, Zecher M, Panemangalore R, Wu Z, Bruno JG, Yuan J, Xu Z, Dillard LW, McGeehan GM, Harrison RK, Scott BB.

J Biochem. 2007 Dec;142(6):671-80. Epub 2007 Oct 17.

PMID:
17942478
15.

Identification of inhibitors of bacterial transcription/translation machinery utilizing a miniaturized 1536-well format screen.

Kariv I, Cao H, Marvil PD, Bobkova EV, Bukhtiyarov YE, Yan YP, Patel U, Coudurier L, Chung TD, Oldenburg KR.

J Biomol Screen. 2001 Aug;6(4):233-43.

PMID:
11689123
16.

Photolabile derivatives of oligonucleotides as probes of ribosomal structure.

Cooperman BS, Alexander RW, Bukhtiyarov Y, Vladimirov SN, Druzina Z, Wang R, Zuño N.

Methods Enzymol. 2000;318:118-36. No abstract available.

PMID:
10889984
17.

Identification of 23S rRNA nucleotides neighboring the P-loop in the Escherichia coli 50S subunit.

Bukhtiyarov Y, Druzina Z, Cooperman BS.

Nucleic Acids Res. 1999 Nov 15;27(22):4376-84.

18.

Three-dimensional placement of the conserved 530 loop of 16 S rRNA and of its neighboring components in the 30 S subunit.

Wang R, Alexander RW, VanLoock M, Vladimirov S, Bukhtiyarov Y, Harvey SC, Cooperman BS.

J Mol Biol. 1999 Feb 19;286(2):521-40.

PMID:
9973568
20.

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