| Literature DB >> 17174090 |
Thuy Tran1, Clifford Quan, Conrad Yap Edosada, Mark Mayeda, Christian Wiesmann, Dan Sutherlin, Beni B Wolf.
Abstract
The structure-activity relationship of various N-acyl-Gly-, N-acyl-Sar-, and N-blocked-boroPro derivatives against three prolyl peptidases was explored. Several N-acyl-Gly- and N-blocked-boroPro compounds showed low nanomolar inhibitory activity against fibroblast activation protein (FAP) and prolyl oligopeptidase (POP) and selectivity against dipeptidyl peptidase-4 (DPP4). N-Acyl-Sar-boroPro analogs retained selectivity against DPP4 and potent POP inhibitory activity but displayed decreased FAP inhibitory activity.Entities:
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Year: 2006 PMID： 17174090 DOI： 10.1016/j.bmcl.2006.11.072
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823