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Rhomboid protease inhibitors: Emerging tools and future therapeutics

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    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

    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.
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    0469951.pdf42.3 MBPublisher’s postprintopen-access
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