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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.
Berger JP, SinhaRoy R, Pocai A, Kelly TM, Scapin G, Gao YD, Pryor KAD, Wu JK, Eiermann GJ, Xu SS, Zhang X, Tatosian DA, Weber AE, Thornberry NA, Carr RD. Berger JP, et al. Among authors: scapin g. Endocrinol Diabetes Metab. 2017 Nov 24;1(1):e00002. doi: 10.1002/edm2.2. eCollection 2018 Jan. Endocrinol Diabetes Metab. 2017. PMID: 30815539 Free PMC article.
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
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. Xu J, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5373-7. doi: 10.1016/j.bmcl.2006.07.061. Epub 2006 Aug 17. Bioorg Med Chem Lett. 2006. PMID: 16919457
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
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. Biftu T, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3384-7. doi: 10.1016/j.bmcl.2007.03.095. Epub 2007 Apr 2. Bioorg Med Chem Lett. 2007. PMID: 17433672
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
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. Kowalchick JE, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5934-9. doi: 10.1016/j.bmcl.2007.07.100. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17827003
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.
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. Edmondson SD, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4097-101. doi: 10.1016/j.bmcl.2009.06.011. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19539471
(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.
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. Biftu T, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52. doi: 10.1016/j.bmcl.2006.09.099. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2007. PMID: 17055272
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.
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. Duffy JL, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 May 15;17(10):2879-85. doi: 10.1016/j.bmcl.2007.02.066. Epub 2007 Feb 25. Bioorg Med Chem Lett. 2007. PMID: 17350841
111 results