Title of article
Synthesis and structure–activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP
Author/Authors
Thuy Tran، نويسنده , , Clifford Quan، نويسنده , , Conrad Yap Edosada، نويسنده , , Mark Mayeda، نويسنده , , Christian Wiesmann، نويسنده , , Dan Sutherlin، نويسنده , , Beni B. Wolf، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
1438
To page
1442
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.
Keywords
Prolyl peptidase , dipeptidyl peptidase , BoroPro , FAP , DPP4 , POP
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797865
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