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Page 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. Zhuang L, et al. Among authors: kruk ba. Bioorg Med Chem. 2017 Jul 15;25(14):3649-3657. doi: 10.1016/j.bmc.2017.04.033. Epub 2017 Apr 29. Bioorg Med Chem. 2017. PMID: 28528082
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. Tice CM, et al. Among authors: kruk ba. Bioorg Med Chem Lett. 2010 Feb 1;20(3):881-6. doi: 10.1016/j.bmcl.2009.12.082. Epub 2010 Jan 4. Bioorg Med Chem Lett. 2010. PMID: 20064717
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. Tice CM, et al. Among authors: kruk ba. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6725-9. doi: 10.1016/j.bmcl.2010.08.142. Epub 2010 Sep 7. Bioorg Med Chem Lett. 2010. PMID: 20864344
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. Xu Z, et al. Among authors: kruk ba. J Med Chem. 2011 Sep 8;54(17):6050-62. doi: 10.1021/jm2005354. Epub 2011 Aug 4. J Med Chem. 2011. PMID: 21786805
Discovery of Potent Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 Using a Novel Growth-Based Protocol of in Silico Screening and Optimization in CONTOUR.
Liu Z, Singh SB, Zheng Y, Lindblom P, Tice C, Dong C, Zhuang L, Zhao Y, Kruk BA, Lala D, Claremon DA, McGeehan GM, Gregg RD, Cain R. Liu Z, et al. Among authors: kruk ba. J Chem Inf Model. 2019 Aug 26;59(8):3422-3436. doi: 10.1021/acs.jcim.9b00198. Epub 2019 Aug 8. J Chem Inf Model. 2019. PMID: 31355641