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ID: ALA1141052
Journal: Bioorg Med Chem Lett
Title: Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.
Authors: Shreder KR, Wong MS, Corral S, Yu Z, Winn DT, Wu M, Hu Y, Nomanbhoy T, Alemayehu S, Fuller SR, Rosenblum JS, Kozarich JW.
Abstract: Dipeptide-based inhibitors with C-substituted (alkyl or aminoalkyl) alpha-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.
CiteXplore: 16084722