Rhomboid protease inhibitors: Emerging tools and future therapeutics

0469951 - ÚOCHB 2017 RIV GB eng J - Journal Article
Stříšovský, Kvido
Rhomboid protease inhibitors: Emerging tools and future therapeutics.
Seminars in Cell & Developmental Biology. Roč. 60, Dec (2016), s. 52-62. ISSN 1084-9521. E-ISSN 1096-3634
R&D Projects: GA MŠMT(CZ) LK11206; GA MŠMT LO1302
EU Projects: European Commission(XE) 304154 - Rhomboid substrates
Institutional support: RVO:61388963
Keywords : rhomboid protease * inhibitor * disease * mechanism * substrate specificity
Subject RIV: CE - Biochemistry
Impact factor: 6.614, year: 2016
http://www.sciencedirect.com/science/article/pii/S1084952116302592

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.
Permanent Link: http://hdl.handle.net/11104/0268040