Carborane-based carbonic anhydrase inhibitors

0422652 - ÚMG 2014 RIV DE eng J - Journal Article
Brynda, Jiří - Mader, Pavel - Šícha, Václav - Fábry, Milan - Poncová, Kristýna - Bakardjiev, Mario - Grüner, Bohumír - Cígler, Petr - Řezáčová, Pavlína
Carborane-based carbonic anhydrase inhibitors.
Angewandte Chemie - International Edition. Roč. 52, č. 51 (2013), s. 13760-13763. ISSN 1433-7851. E-ISSN 1521-3773
R&D Projects: GA TA ČR(CZ) TE01020028; GA AV ČR IAAX00320901
Institutional support: RVO:68378050 ; RVO:61388963 ; RVO:61388980
Keywords : carbonic anhydrases * carboranes * drug discovery * inhibitors * structure elucidation
Subject RIV: EB - Genetics ; Molecular Biology
Impact factor: 11.336, year: 2013

CA inhibitors: Human carbonic anhydrases (CAs) are diagnostic and therapeutic targets. Various carborane cages are shown to act as active-site-directed inhibitors, and substitution with a sulfamide group and other substituents leads to compounds with high selectivity towards the cancer-specific isozyme IX. Crystal structures of the carboranes in the active site provide information that can be applied to the structure-based design of specific inhibitors.
Permanent Link: http://hdl.handle.net/11104/0228887