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Page 1
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.
Han S, Narayanan S, Kim SH, Calderon I, Zhu X, Kawasaki A, Yue D, Lehmann J, Wong A, Buzard DJ, Semple G, Carroll C, Chu ZL, Al-Sharmma H, Shu HH, Tung SF, Unett DJ, Behan DP, Yoon WH, Morgan M, Usmani KA, Chen C, Sadeque A, Leonard JN, Jones RM. Han S, et al. Among authors: leonard jn. Bioorg Med Chem Lett. 2015 Aug 1;25(15):3034-8. doi: 10.1016/j.bmcl.2015.04.102. Epub 2015 May 23. Bioorg Med Chem Lett. 2015. PMID: 26048791
GPR119 agonists for the treatment of type 2 diabetes.
Jones RM, Leonard JN, Buzard DJ, Lehmann J. Jones RM, et al. Among authors: leonard jn. Expert Opin Ther Pat. 2009 Oct;19(10):1339-59. doi: 10.1517/13543770903153878. Expert Opin Ther Pat. 2009. PMID: 19780700 Review.
Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Semple G, Ren A, Fioravanti B, Pereira G, Calderon I, Choi K, Xiong Y, Shin YJ, Gharbaoui T, Sage CR, Morgan M, Xing C, Chu ZL, Leonard JN, Grottick AJ, Al-Shamma H, Liang Y, Demarest KT, Jones RM. Semple G, et al. Among authors: leonard jn. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. doi: 10.1016/j.bmcl.2011.03.007. Epub 2011 Mar 13. Bioorg Med Chem Lett. 2011. PMID: 21444206
Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.
Semple G, Lehmann J, Wong A, Ren A, Bruce M, Shin YJ, Sage CR, Morgan M, Chen WC, Sebring K, Chu ZL, Leonard JN, Al-Shamma H, Grottick AJ, Du F, Liang Y, Demarest K, Jones RM. Semple G, et al. Among authors: leonard jn. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5. doi: 10.1016/j.bmcl.2011.12.092. Epub 2011 Dec 30. Bioorg Med Chem Lett. 2012. PMID: 22264481
Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists.
Buzard DJ, Kim SH, Lehmann J, Han S, Calderon I, Wong A, Kawasaki A, Narayanan S, Bhat R, Gharbaoui T, Lopez L, Yue D, Whelan K, Al-Shamma H, Unett DJ, Shu HH, Tung SF, Chang S, Chuang CF, Morgan M, Sadeque A, Chu ZL, Leonard JN, Jones RM. Buzard DJ, et al. Among authors: leonard jn. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-5. doi: 10.1016/j.bmcl.2014.06.071. Epub 2014 Jul 3. Bioorg Med Chem Lett. 2014. PMID: 25088191
N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Chu ZL, Carroll C, Chen R, Alfonso J, Gutierrez V, He H, Lucman A, Xing C, Sebring K, Zhou J, Wagner B, Unett D, Jones RM, Behan DP, Leonard J. Chu ZL, et al. Mol Endocrinol. 2010 Jan;24(1):161-70. doi: 10.1210/me.2009-0239. Epub 2009 Nov 9. Mol Endocrinol. 2010. PMID: 19901198 Free PMC article.
Orphan GPCR target validation.
Thomsen W, Leonard J, Behan DP. Thomsen W, et al. Curr Opin Mol Ther. 2004 Dec;6(6):640-56. Curr Opin Mol Ther. 2004. PMID: 15663329 Review.
A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like Peptide-1 and glucose-dependent insulinotropic Peptide release.
Chu ZL, Carroll C, Alfonso J, Gutierrez V, He H, Lucman A, Pedraza M, Mondala H, Gao H, Bagnol D, Chen R, Jones RM, Behan DP, Leonard J. Chu ZL, et al. Endocrinology. 2008 May;149(5):2038-47. doi: 10.1210/en.2007-0966. Epub 2008 Jan 17. Endocrinology. 2008. PMID: 18202141
159 results