| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378033 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
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.
Graphical abstractThe structure–activity relationship of various N-acyl-Gly-, N-acyl-Sar-, and N-blocked-boroPro derivatives against three prolyl peptidases (FAP, DPP4, and POP) was explored.Figure optionsDownload full-size imageDownload as PowerPoint slide
