Počet záznamů: 1  

Design of Highly Potent Urea-Based, Exosite-Binding Inhibitors Selective for Glutamate Carboxypeptidase II

  1. 1.
    0445391 - ÚOCHB 2016 RIV US eng J - Článek v odborném periodiku
    Tykvart, Jan - Schimer, Jiří - Jančařík, Andrej - Bařinková, Jitka - Navrátil, Václav - Starková, Jana - Šrámková, Karolína - Konvalinka, Jan - Majer, Pavel - Šácha, Pavel
    Design of Highly Potent Urea-Based, Exosite-Binding Inhibitors Selective for Glutamate Carboxypeptidase II.
    Journal of Medicinal Chemistry. Roč. 58, č. 10 (2015), s. 4357-4363. ISSN 0022-2623
    Grant CEP: GA ČR GBP208/12/G016; GA MŠk LO1302
    Institucionální podpora: RVO:61388963
    Klíčová slova: GCPII selective inhibitors * GCPIII * GCPII
    Kód oboru RIV: CE - Biochemie
    Impakt faktor: 5.589, rok: 2015

    We present here a structure-aided design of inhibitors targeting the active site as well as exosites of glutamate carboxypeptidase II (GCPII), a prostate cancer marker, preparing potent and selective inhibitors that are more than 1000-fold more active toward, GCPII than its closest human homologue, glutamate carboxypeptidase III (GCPIII). Additionally, we demonstrate that the prepared inhibitor conjugate can be used for sensitive and selective imaging of GCPII in mammalian cells.
    Trvalý link: http://hdl.handle.net/11104/0247685