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Bioorg Med Chem Lett. 2005 Oct 1;15(19):4256-60.

Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.

Author information

1
ActivX Biosciences, 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA. kevins@activx.com

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.

PMID:
16084722
DOI:
10.1016/j.bmcl.2005.06.076
[Indexed for MEDLINE]

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