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.
MeSH terms
-
Adenosine Deaminase Inhibitors
-
Antigens, Neoplasm
-
Biomarkers, Tumor / antagonists & inhibitors
-
Boron Compounds / chemical synthesis*
-
Boron Compounds / pharmacology
-
Dipeptidyl Peptidase 4
-
Dipeptidyl-Peptidase IV Inhibitors
-
Endopeptidases
-
Gelatinases
-
Glycoproteins / antagonists & inhibitors
-
Membrane Proteins
-
Proline / chemistry*
-
Proline / pharmacology
-
Prolyl Oligopeptidases
-
Serine Endopeptidases / drug effects
-
Serine Proteinase Inhibitors / chemical synthesis*
-
Serine Proteinase Inhibitors / chemistry
-
Serine Proteinase Inhibitors / pharmacology*
-
Structure-Activity Relationship
Substances
-
Adenosine Deaminase Inhibitors
-
Antigens, Neoplasm
-
Biomarkers, Tumor
-
Boron Compounds
-
Dipeptidyl-Peptidase IV Inhibitors
-
Glycoproteins
-
Membrane Proteins
-
Serine Proteinase Inhibitors
-
Proline
-
Endopeptidases
-
DPP4 protein, human
-
Dipeptidyl Peptidase 4
-
Serine Endopeptidases
-
fibroblast activation protein alpha
-
PREPL protein, human
-
Prolyl Oligopeptidases
-
Gelatinases