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Page 1
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: marcinkeviciene j. 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: marcinkeviciene j. 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: marcinkeviciene j. 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
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG. Meng W, et al. Among authors: marcinkeviciene j. J Med Chem. 2010 Aug 12;53(15):5620-8. doi: 10.1021/jm100634a. J Med Chem. 2010. PMID: 20684603
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1H-pyrazol-1-yl)methyl)phosphonate (BMS-820132).
Shi Y, Wang Y, Meng W, Brigance RP, Ryono DE, Bolton S, Zhang H, Chen S, Smirk R, Tao S, Tino JA, Williams KN, Sulsky R, Nielsen L, Ellsworth B, Wong MKY, Sun JH, Leith LW, Sun D, Wu DR, Gupta A, Rampulla R, Mathur A, Chen BC, Wang A, Fuentes-Catanio HG, Kunselman L, Cap M, Zalaznick J, Ma X, Liu H, Taylor JR, Zebo R, Jones B, Kalinowski S, Swartz J, Staal A, O'Malley K, Kopcho L, Muckelbauer JK, Krystek SR Jr, Spronk SA, Marcinkeviciene J, Everlof G, Chen XQ, Xu C, Li YX, Langish RA, Yang Y, Wang Q, Behnia K, Fura A, Janovitz EB, Pannacciulli N, Griffen S, Zinker BA, Krupinski J, Kirby M, Whaley J, Zahler R, Barrish JC, Robl JA, Cheng PTW. Shi Y, et al. Among authors: marcinkeviciene j. J Med Chem. 2022 Mar 10;65(5):4291-4317. doi: 10.1021/acs.jmedchem.1c02110. Epub 2022 Feb 18. J Med Chem. 2022. PMID: 35179904
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: marcinkeviciene j. Protein Sci. 2008 Feb;17(2):240-50. doi: 10.1110/ps.073253208. Protein Sci. 2008. PMID: 18227430 Free PMC article.
72 results