Ontology highlight
ABSTRACT:
SUBMITTER: Grimshaw CE
PROVIDER: S-EPMC4915685 | biostudies-literature | 2016
REPOSITORIES: biostudies-literature
Grimshaw Charles E CE Jennings Andy A Kamran Ruhi R Ueno Hikaru H Nishigaki Nobuhiro N Kosaka Takuo T Tani Akiyoshi A Sano Hiroki H Kinugawa Yoshinobu Y Koumura Emiko E Shi Lihong L Takeuchi Koji K
PloS one 20160621 6
Trelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor, shows sustained efficacy by once-weekly dosing in type 2 diabetes patients. In this study, we characterized in vitro properties of trelagliptin, which exhibited approximately 4- and 12-fold more potent inhibition against human dipeptidyl peptidase-4 than alogliptin and sitagliptin, respectively, and >10,000-fold selectivity over related proteases including dipeptidyl peptidase-8 and dipeptidyl peptidase-9. Kinetic analysis reveale ...[more]