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A comparative study of the binding properties, dipeptidyl peptidase-4 (DPP-4) inhibitory activity and glucose-lowering efficacy of the DPP-4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice
Endocrinol Diabetes Metab 1: e00002

Cox JM, Chu HD, Kuethe JT, Gao YD, Scapin G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Sinha-Roy R, Weber AE, Biftu T (2016)
The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors
Bioorganic & Medicinal Chemistry Lett 26: 2622

Pissarnitski DA, Zhao Z, Cole D, Wu WL, Domalski M, Clader JW, Scapin G, Voigt J, Soriano A, Kelly T, Powles MA, Yao Z, Burnett DA (2016)
Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors
Bioorganic & Medicinal Chemistry 24: 5534

Wu WL, Hao J, Domalski M, Burnett DA, Pissarnitski D, Zhao Z, Stamford A, Scapin G, Gao YD, Soriano A, Kelly TM, Yao Z, Powles MA, Chen S, Mei H, Hwa J (2016)
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes
ACS Med Chem Lett 7: 498

Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE (2014)
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes
Journal of Medicinal Chemistry 57: 3205

Edmondson SD, Mastracchio A, Cox JM, Eiermann GJ, He H, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Xu S, Zhu B, Thornberry NA, Roy RS, Weber AE (2009)
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors
Bioorganic & Medicinal Chemistry Lett 19: 4097

Edmondson SD, Wei L, Xu J, Shang J, Xu S, Pang J, Chaudhary A, Dean DC, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Scapin G, Wu JK, Beconi MG, Thornberry NA, Weber AE (2008)
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 18: 2409

Kim D, Kowalchick JE, Brockunier LL, Parmee ER, Eiermann GJ, Fisher MH, He H, Leiting B, Lyons K, Scapin G, Patel SB, Petrov A, Pryor KD, Roy RS, Wu JK, Zhang X, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE (2008)
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines
Journal of Medicinal Chemistry 51: 589

Liang GB, Qian X, Biftu T, Singh S, Gao YD, Scapin G, Patel S, Leiting B, Patel R, Wu J, Zhang X, Thornberry NA, Weber AE (2008)
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design
Bioorganic & Medicinal Chemistry Lett 18: 3706

Biftu T, Feng D, Qian X, Liang GB, Kieczykowski G, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Scapin G, Patel S, Gao YD, Singh S, Wu J, Zhang X, Thornberry NA, Weber AE (2007)
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)- 1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Bioorganic & Medicinal Chemistry Lett 17: 49

Biftu T, Scapin G, Singh S, Feng D, Becker JW, Eiermann G, He H, Lyons K, Patel S, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Doss GA, Thornberry NA, Weber AE (2007)
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin
Bioorganic & Medicinal Chemistry Lett 17: 3384

Duffy JL, Kirk BA, Wang L, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE (2007)
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV
Bioorganic & Medicinal Chemistry Lett 17: 2879

Gao YD, Feng D, Sheridan RP, Scapin G, Patel SB, Wu JK, Zhang X, Sinha-Roy R, Thornberry NA, Weber AE, Biftu T (2007)
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors
Bioorganic & Medicinal Chemistry Lett 17: 3877

Kaelin DE, Smenton AL, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Duffy JL (2007)
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV
Bioorganic & Medicinal Chemistry Lett 17: 5806

Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A, Scapin G, Patel RA, Thornberry NA, Weber AE, Kim D (2007)
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
Bioorganic & Medicinal Chemistry Lett 17: 5934

Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE (2006)
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]tr iazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Journal of Medicinal Chemistry 49: 3614

Xu J, Wei L, Mathvink RJ, Edmondson SD, Eiermann GJ, He H, Leone JF, Leiting B, Lyons KA, Marsilio F, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE (2006)
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 16: 5373

Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE (2005)
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)- yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Journal of Medicinal Chemistry 48: 141