Inhibitors of BMP-1/tolloid-like proteinases: efficacy, selectivity and cellular toxicity.

ABSTRACT: BMP-1/tolloid-like proteinases belong to the astacin family of human metalloproteinases, together with meprins and ovastacin. They represent promising targets to treat or prevent a wide range of diseases such as fibrotic disorders or cancer. However, the study of their pathophysiological roles is still impaired by the lack of well-characterized inhibitors and the questions that remain regarding their selectivity and in vivo efficiency. As a first step towards the identification of suitable tools to be used in functional studies, we have undertaken a systematic comparison of seven molecules known to affect the proteolytic activity of human astacins including three hydroxamates (FG-2575, UK383,367, S33A), the protein sizzled, a new phosphinic inhibitor (RXP-1001) and broad-spectrum pr

SUBMITTER: Talantikite M 

PROVIDER: S-EPMC6275283 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature