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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: candelore m. 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 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: candelore m. 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
Chronic treatment with a glucagon receptor antagonist lowers glucose and moderately raises circulating glucagon and glucagon-like peptide 1 without severe alpha cell hypertrophy in diet-induced obese mice.
Mu J, Jiang G, Brady E, Dallas-Yang Q, Liu F, Woods J, Zycband E, Wright M, Li Z, Lu K, Zhu L, Shen X, Sinharoy R, Candelore ML, Qureshi SA, Shen DM, Zhang F, Parmee ER, Zhang BB. Mu J, et al. Among authors: candelore ml. Diabetologia. 2011 Sep;54(9):2381-91. doi: 10.1007/s00125-011-2217-2. Epub 2011 Jun 22. Diabetologia. 2011. PMID: 21695571
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.
Xiong Y, Guo J, Candelore MR, Liang R, Miller C, Dallas-Yang Q, Jiang G, McCann PE, Qureshi SA, Tong X, Xu SS, Shang J, Vincent SH, Tota LM, Wright MJ, Yang X, Zhang BB, Tata JR, Parmee ER. Xiong Y, et al. Among authors: candelore mr. J Med Chem. 2012 Jul 12;55(13):6137-48. doi: 10.1021/jm300579z. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22708876
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: candelore mr. 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 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: candelore mr. 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
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: candelore mr. 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
54 results