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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: szalkowski d. 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 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: szalkowski d. 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 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: szalkowski d. 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
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: szalkowski d. 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
The basal SAR of a novel insulin receptor activator.
Wood HB Jr, Black R, Salituro G, Szalkowski D, Li Z, Zhang Y, Moller DE, Zhang B, Jones AB. Wood HB Jr, et al. Among authors: szalkowski d. Bioorg Med Chem Lett. 2000 Jun 5;10(11):1189-92. doi: 10.1016/s0960-894x(00)00206-7. Bioorg Med Chem Lett. 2000. PMID: 10866378
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: szalkowski d. J Biol Chem. 2000 Nov 24;275(47):36590-5. doi: 10.1074/jbc.M006287200. J Biol Chem. 2000. PMID: 10967116 Free article.
We recently described the identification of a non-peptidyl fungal metabolite (l-783,281, compound 1), which induced activation of human insulin receptor (IR) tyrosine kinase and mediated insulin-like effects in cells, as well as decreased blood glucose levels in murine models of …
We recently described the identification of a non-peptidyl fungal metabolite (l-783,281, compound 1), which induced activation of human insu …
23 results