| Title : Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778) - Devasthale_2013_J.Med.Chem_56_7343 |
| Author(s) : Devasthale P , Wang Y , Wang W , Fevig J , Feng J , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Moulin F , Li YX , Zahler R , Kirby MS , Hamann LG |
| Ref : Journal of Medicinal Chemistry , 56 :7343 , 2013 |
| Abstract : |
| PubMedSearch : Devasthale_2013_J.Med.Chem_56_7343 |
| PubMedID: 23964740 |
| Gene_locus related to this paper: human-DPP4 |
| Title : Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors - Zhao_2013_Bioorg.Med.Chem.Lett_23_1622 |
| Author(s) : Zhao G , Kwon C , Wang A , Robertson JG , Marcinkeviciene J , Parker RA , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 23 :1622 , 2013 |
| Abstract : |
| PubMedSearch : Zhao_2013_Bioorg.Med.Chem.Lett_23_1622 |
| PubMedID: 23416006 |
| Title : DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues - Harstad_2013_Regul.Pept_186C_26 |
| Author(s) : Harstad EB , Rosenblum JS , Gorrell MD , Achanzar WE , Minimo L , Wu J , Rosini-Marthaler L , Gullo R , Ordway ND , Kirby MS , Chadwick KD , Cosma GN , Moyer CF |
| Ref : Regul Pept , 186C :26 , 2013 |
| Abstract : |
| PubMedSearch : Harstad_2013_Regul.Pept_186C_26 |
| PubMedID: 23850796 |
| Gene_locus related to this paper: rat-dpp9 |
| Title : Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor - Wang_2012_BMC.Pharmacol_12_2 |
| Author(s) : Wang A , Dorso C , Kopcho L , Locke G , Langish R , Harstad E , Shipkova P , Marcinkeviciene J , Hamann L , Kirby MS |
| Ref : BMC Pharmacol , 12 :2 , 2012 |
| Abstract : |
| PubMedSearch : Wang_2012_BMC.Pharmacol_12_2 |
| PubMedID: 22475049 |
| Title : 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site - Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| Author(s) : Wang W , Devasthale P , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Li YX , Zahler R , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :6646 , 2011 |
| Abstract : |
| PubMedSearch : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
| PubMedID: 21996520 |
| Gene_locus related to this paper: human-DPP4 |
| Title : Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes - Brigance_2010_Bioorg.Med.Chem.Lett_20_4395 |
| Author(s) : Brigance RP , Meng W , Fura A , Harrity T , Wang A , Zahler R , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 20 :4395 , 2010 |
| Abstract : |
| PubMedSearch : Brigance_2010_Bioorg.Med.Chem.Lett_20_4395 |
| PubMedID: 20598534 |
| Title : Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors - O'Connor_2010_Bioorg.Med.Chem.Lett_20_6273 |
| Author(s) : O'Connor SP , Wang Y , Simpkins LM , Brigance RP , Meng W , Wang A , Kirby MS , Weigelt CA , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 20 :6273 , 2010 |
| Abstract : |
| PubMedSearch : O'Connor_2010_Bioorg.Med.Chem.Lett_20_6273 |
| PubMedID: 20833042 |
| Title : Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxa mides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors - Meng_2010_J.Med.Chem_53_5620 |
| Author(s) : 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 |
| Ref : Journal of Medicinal Chemistry , 53 :5620 , 2010 |
| Abstract : |
| PubMedSearch : Meng_2010_J.Med.Chem_53_5620 |
| PubMedID: 20684603 |
| Gene_locus related to this paper: human-DPP4 |
| Title : Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation - Metzler_2008_Protein.Sci_17_240 |
| Author(s) : 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 |
| Ref : Protein Science , 17 :240 , 2008 |
| Abstract : |
| PubMedSearch : Metzler_2008_Protein.Sci_17_240 |
| PubMedID: 18227430 |
| Gene_locus related to this paper: human-DPP4 |
| Title : Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors - Simpkins_2007_Bioorg.Med.Chem.Lett_17_6476 |
| Author(s) : 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 |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :6476 , 2007 |
| Abstract : |
| PubMedSearch : Simpkins_2007_Bioorg.Med.Chem.Lett_17_6476 |
| PubMedID: 17937986 |
| Title : Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1 - Magnin_2006_Bioorg.Med.Chem.Lett_16_1731 |
| Author(s) : Magnin DR , Taunk PC , Robertson JG , Wang A , Marcinkeviciene J , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 16 :1731 , 2006 |
| Abstract : |
| PubMedSearch : Magnin_2006_Bioorg.Med.Chem.Lett_16_1731 |
| PubMedID: 16376077 |
| Title : Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach - Kopcho_2005_Arch.Biochem.Biophys_436_367 |
| Author(s) : Kopcho LM , Kim YB , Wang A , Liu MA , Kirby MS , Marcinkeviciene J |
| Ref : Archives of Biochemistry & Biophysics , 436 :367 , 2005 |
| Abstract : |
| PubMedSearch : Kopcho_2005_Arch.Biochem.Biophys_436_367 |
| PubMedID: 15797249 |
| Title : Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors - Zhao_2005_Bioorg.Med.Chem.Lett_15_3992 |
| Author(s) : Zhao G , Taunk PC , Magnin DR , Simpkins LM , Robl JA , Wang A , Robertson JG , Marcinkeviciene J , Sitkoff DF , Parker RA , Kirby MS , Hamann LG |
| Ref : Bioorganic & Medicinal Chemistry Lett , 15 :3992 , 2005 |
| Abstract : |
| PubMedSearch : Zhao_2005_Bioorg.Med.Chem.Lett_15_3992 |
| PubMedID: 16046120 |
| Title : 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_2005_J.Med.Chem_48_5025 |
| Author(s) : 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 |
| Ref : Journal of Medicinal Chemistry , 48 :5025 , 2005 |
| Abstract : |
| PubMedSearch : Augeri_2005_J.Med.Chem_48_5025 |
| PubMedID: 16033281 |