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Page 1
Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.
Sinz C, Bittner A, Brady E, Candelore M, Dallas-Yang Q, Ding V, Jiang G, Lin Z, Qureshi S, Salituro G, Saperstein R, Shang J, Szalkowski D, Tota L, Vincent S, Wright M, Xu S, Yang X, Zhang B, Tata J, Kim R, Parmee ER. Sinz C, et al. Among authors: saperstein r. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7124-30. doi: 10.1016/j.bmcl.2011.09.105. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22030028
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Duffy JL, Kirk BA, Konteatis Z, Campbell EL, Liang R, Brady EJ, Candelore MR, Ding VD, Jiang G, Liu F, Qureshi SA, Saperstein R, Szalkowski D, Tong S, Tota LM, Xie D, Yang X, Zafian P, Zheng S, Chapman KT, Zhang BB, Tata JR. Duffy JL, et al. Among authors: saperstein r. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5. doi: 10.1016/j.bmcl.2005.01.003. Bioorg Med Chem Lett. 2005. PMID: 15713396
Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.
Shen DM, Zhang F, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Dragovic J, Feeney WP, Jiang G, McCann PE, Mock S, Qureshi SA, Saperstein R, Shen X, Tamvakopoulos C, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER. Shen DM, et al. Among authors: saperstein r. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4564-9. doi: 10.1016/j.bmcl.2005.06.101. Bioorg Med Chem Lett. 2005. PMID: 16102966
Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.
Liang R, Abrardo L, Brady EJ, Candelore MR, Ding V, Saperstein R, Tota LM, Wright M, Mock S, Tamvakopolous C, Tong S, Zheng S, Zhang BB, Tata JR, Parmee ER. Liang R, et al. Among authors: saperstein r. Bioorg Med Chem Lett. 2007 Feb 1;17(3):587-92. doi: 10.1016/j.bmcl.2006.11.014. Epub 2006 Nov 10. Bioorg Med Chem Lett. 2007. PMID: 17126016
Discovery of potent, orally active benzimidazole glucagon receptor antagonists.
Kim RM, Chang J, Lins AR, Brady E, Candelore MR, Dallas-Yang Q, Ding V, Dragovic J, Iliff S, Jiang G, Mock S, Qureshi S, Saperstein R, Szalkowski D, Tamvakopoulos C, Tota L, Wright M, Yang X, Tata JR, Chapman K, Zhang BB, Parmee ER. Kim RM, et al. Among authors: saperstein r. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3701-5. doi: 10.1016/j.bmcl.2008.05.072. Epub 2008 May 22. Bioorg Med Chem Lett. 2008. PMID: 18539028
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.
Shen DM, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Feeney WP, Jiang G, McCann ME, Mock S, Qureshi SA, Saperstein R, Shen X, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER. Shen DM, et al. Among authors: saperstein r. Bioorg Med Chem Lett. 2011 Jan 1;21(1):76-81. doi: 10.1016/j.bmcl.2010.11.074. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21147532
Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists.
Sinz C, Chang J, Lins AR, Brady E, Candelore M, Dallas-Yang Q, Ding V, Jiang G, Lin Z, Mock S, Qureshi S, Salituro G, Saperstein R, Shang J, Szalkowski D, Tota L, Vincent S, Wright M, Xu S, Yang X, Zhang B, Tata J, Kim R, Parmee E. Sinz C, et al. Among authors: saperstein r. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7131-6. doi: 10.1016/j.bmcl.2011.09.085. Epub 2011 Sep 29. Bioorg Med Chem Lett. 2011. PMID: 22001094
A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects.
Qureshi SA, Rios Candelore M, Xie D, Yang X, Tota LM, Ding VD, Li Z, Bansal A, Miller C, Cohen SM, Jiang G, Brady E, Saperstein R, Duffy JL, Tata JR, Chapman KT, Moller DE, Zhang BB. Qureshi SA, et al. Among authors: saperstein r. Diabetes. 2004 Dec;53(12):3267-73. doi: 10.2337/diabetes.53.12.3267. Diabetes. 2004. PMID: 15561959
Activation of insulin signal transduction pathway and anti-diabetic activity of small molecule insulin receptor activators.
Qureshi SA, Ding V, Li Z, Szalkowski D, Biazzo-Ashnault DE, Xie D, Saperstein R, Brady E, Huskey S, Shen X, Liu K, Xu L, Salituro GM, Heck JV, Moller DE, Jones AB, Zhang BB. Qureshi SA, et al. Among authors: saperstein r. J Biol Chem. 2000 Nov 24;275(47):36590-5. doi: 10.1074/jbc.M006287200. J Biol Chem. 2000. PMID: 10967116 Free article.
68 results