Title of article :
Synthesis and structure–activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7
Author/Authors :
Yi Hu، نويسنده , , Lifu Ma، نويسنده , , Min Wu، نويسنده , , Melissa S. Wong، نويسنده , , Bei Li Zhang، نويسنده , , Sergio Corral، نويسنده , , Zhizhou Yu، نويسنده , , Tyzoon Nomanbhoy، نويسنده , , Senaiet Alemayehu، نويسنده , , Stacy R. Fuller، نويسنده , , Jonathan S. Rosenblum، نويسنده , , Natasha Rozenkrants، نويسنده , , Lauro C. Minimo، نويسنده , , William C. Ripka، نويسنده , , Anna K. Szardenings، نويسنده , , John W. Kozarich and Adrian Goldman، نويسنده , , Kevin R. Shreder، نويسنده ,
Abstract :
The structure–activity relationship of various N-alkyl Gly-boro-Pro derivatives against three dipeptidyl peptidases (DPPs) was studied. In a series of N-cycloalkyl analogs, DPP4 and fibroblast activation protein-α (FAP) optimally preferred N-cycloheptyl whereas DPP7 tolerated even larger cycloalkyl rings. Gly α-carbon derivatization of N-cyclohexyl or N-(2-adamantyl) Gly-boro-Pro resulted in a significant decrease in potency against all the three DPPs.
Keywords :
DPP4 , Boro-Pro , Dipeptidyl peptidase , FAP , DPP7
