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Rhomboid protease inhibitors: Emerging tools and future therapeutics
K. Strisovsky,
Language English Country Great Britain
Document type Journal Article, Review, Research Support, Non-U.S. Gov't
- MeSH
- Molecular Targeted Therapy * MeSH
- Enzyme Assays MeSH
- Protease Inhibitors chemistry therapeutic use MeSH
- Humans MeSH
- Membrane Proteins antagonists & inhibitors metabolism MeSH
- Substrate Specificity MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Review MeSH
Rhomboid-family intramembrane serine proteases are evolutionarily widespread. Their functions in different organisms are gradually being uncovered and already suggest medical relevance for infectious diseases and cancer. In contrast to these advances, selective inhibitors that could serve as efficient tools for investigation of physiological functions of rhomboids, validation of their disease relevance or as templates for drug development are lacking. In this review I extract what is known about rhomboid protease mechanism and specificity, examine the currently used inhibitors, their mechanism of action and limitations, and conclude by proposing routes for future development of rhomboid protease inhibitors.
References provided by Crossref.org
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