Ontology highlight
ABSTRACT:
SUBMITTER: Colombo E
PROVIDER: S-EPMC4025795 | biostudies-other | 2012 Jul
REPOSITORIES: biostudies-other
Colombo Eloïc E Désilets Antoine A Duchêne Dominic D Chagnon Félix F Najmanovich Rafael R Leduc Richard R Marsault Eric E
ACS medicinal chemistry letters 20120411 7
Matriptase is a member of the type II transmembrane serine protease family. Several studies have reported deregulated matriptase expression in several types of epithelial cancers, suggesting that matriptase constitutes a potential target for cancer therapy. We report herein a new series of slow, tight-binding inhibitors of matriptase, which mimic the P1-P4 substrate recognition sequence of the enzyme. Preliminary structure-activity relationships indicate that this benzothiazole-containing RQAR-p ...[more]