Author/Authors :
Kevin R. Shreder، نويسنده , , Melissa S. Wong، نويسنده , , Sergio Corral، نويسنده , , Zhizhou Yu، نويسنده , , David T. Winn، نويسنده , , Min Wu، نويسنده , , Yi Hu، نويسنده , , Tyzoon Nomanbhoy، نويسنده , , Senaiet Alemayehu، نويسنده , , Stacy R. Fuller، نويسنده , , Jonathan S. Rosenblum، نويسنده , , John W. Kozarich and Adrian Goldman، نويسنده ,
Abstract :
Dipeptide-based inhibitors with C-substituted (alkyl or aminoalkyl) α-amino acids in the P2 position and boro-norleucine (boro-Nle) in the P1 position were synthesized. Relative to boro-proline, boro-Nle as a P1 residue was shown able to significantly dial out DPP4, FAP, DPP8, and DPP9 activity. Dab-boro-Nle (4g) proved to be the most selective and potent DPP7 inhibitor with a DPP7 IC50 value of 480 pM.
Keywords :
DPP4 , FAP , DPP7 , DPP9 , Boro-norleucine , Dipeptidyl peptidase , DPP8
