0379149 - BFÚ 2013 RIV US eng J - Článek v odborném periodiku
Brabec, Viktor - Griffith, D.M. - Kisová, Anna - Kostrhunová, Hana - Zerzánková, Lenka - Marmion, C.J. - Kašpárková, Jana
Valuable insight into the anticancer activity of the platinum-histone deacetylase inhibitor conjugate, cis-[Pt(NH3)2malSAHA-2H)].
Molecular Pharmaceutics. Roč. 9, č. 7 (2012), s. 1990-1999. ISSN 1543-8384. E-ISSN 1543-8392
Grant CEP: GA ČR(CZ) GAP301/10/0598; GA ČR(CZ) GPP303/11/P047
Výzkumný záměr: CEZ:AV0Z50040702
Klíčová slova: histone deacetylase inhibitor * platinum * DNA
Kód oboru RIV: BO - Biofyzika
Impakt faktor: 4.570, rok: 2012

Cis-[PtII(NH3)2(malSAHA-2H)], a cisplatin adduct conjugated to a potent histone deacetylase inhibitor (HDACi), suberoylanilide hydroxamic acid (SAHA), was developed as a potential anticancer agent. This Pt-HDACi conjugate was demonstrated to have comparable cytotoxicity to cisplatin against A2780 ovarian cancer cells but significantly reduced cytotoxicity against a representative normal cell line, NHDF. The conjugate exhibited no inhibition of HDAC activity in CH1 cells. In light of these results, novel Pt-HDACi conjugates are currently being developed, with particular emphasis, through subtle structural modifications, on enhancing the rate of DNA binding and enhancing HDAC inhibitory activity.
Trvalý link: http://hdl.handle.net/11104/0007105