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Page 1
Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes.
Hamilton BS, Himmelsbach F, Nar H, Schuler-Metz A, Krosky P, Guo J, Guo R, Meng S, Zhao Y, Lala DS, Zhuang L, Claremon DA, McGeehan GM. Hamilton BS, et al. Among authors: claremon da. Eur J Pharmacol. 2015 Jan 5;746:50-5. doi: 10.1016/j.ejphar.2014.10.053. Epub 2014 Nov 8. Eur J Pharmacol. 2015. PMID: 25445047
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: claremon da. 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 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: claremon da. 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
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: claremon da. 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
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: 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. 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: 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. Bioorg Med Chem Lett. 2010. PMID: 20864344
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. Zheng Y, et al. Among authors: claremon da. J Med Chem. 2016 Apr 14;59(7):3264-71. doi: 10.1021/acs.jmedchem.5b02029. Epub 2016 Mar 29. J Med Chem. 2016. PMID: 26990539
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. Tice CM, et al. Among authors: 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. Bioorg Med Chem Lett. 2016. PMID: 27599745
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. Yuan J, et al. Among authors: 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. Bioorg Med Chem Lett. 2011. PMID: 21741239
40 results