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Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG. Augeri DJ, et al. Among authors: kirby ms. J Med Chem. 2005 Jul 28;48(15):5025-37. doi: 10.1021/jm050261p. J Med Chem. 2005. PMID: 16033281
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.
Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG. Zhao G, et al. Among authors: kirby ms. Bioorg Med Chem Lett. 2005 Sep 15;15(18):3992-5. doi: 10.1016/j.bmcl.2005.06.043. Bioorg Med Chem Lett. 2005. PMID: 16046120
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG. Simpkins LM, et al. Among authors: kirby ms. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6476-80. doi: 10.1016/j.bmcl.2007.09.090. Epub 2007 Oct 1. Bioorg Med Chem Lett. 2007. PMID: 17937986
Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation.
Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J. Metzler WJ, et al. Among authors: kirby ms. Protein Sci. 2008 Feb;17(2):240-50. doi: 10.1110/ps.073253208. Protein Sci. 2008. PMID: 18227430 Free PMC article.
61 results