Tran_2007_Bioorg.Med.Chem.Lett_17_1438

Reference

Title : Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP - Tran_2007_Bioorg.Med.Chem.Lett_17_1438
Author(s) : Tran T , Quan C , Edosada CY , Mayeda M , Wiesmann C , Sutherlin D , Wolf BB
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :1438 , 2007
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.

PubMedSearch : Tran_2007_Bioorg.Med.Chem.Lett_17_1438
PubMedID: 17174090

Related information

Citations formats

Tran T, Quan C, Edosada CY, Mayeda M, Wiesmann C, Sutherlin D, Wolf BB (2007)
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP
Bioorganic & Medicinal Chemistry Lett 17 :1438

Tran T, Quan C, Edosada CY, Mayeda M, Wiesmann C, Sutherlin D, Wolf BB (2007)
Bioorganic & Medicinal Chemistry Lett 17 :1438