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Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides
- 1.0365071 - ÚMG 2012 RIV US eng J - Článek v odborném periodiku
Mader, Pavel - Brynda, Jiří - Gitto, R. - Agnello, S. - Pachl, Petr - Supuran, C. T. - Chimirri, A. - Řezáčová, Pavlína
Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides.
Journal of Medicinal Chemistry. Roč. 54, č. 7 (2011), s. 2522-2526. ISSN 0022-2623. E-ISSN 1520-4804
Grant CEP: GA ČR GA203/09/0820
Výzkumný záměr: CEZ:AV0Z50520514; CEZ:AV0Z40550506
Klíčová slova: carbonic anhydrase * isoquinolinesulfonamides * selective inhibition * crystal structure
Kód oboru RIV: EB - Genetika a molekulární biologie
Impakt faktor: 5.248, rok: 2011
lsoquinolinesulfonamides inhibit human carbonic anhydrases (hCAs) and display selectivity toward therapeutically relevant isozymes. The crystal structure of hCA 11 in complex with 6,7-dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamide revealed unusual inhibitor binding. Structural analyses allowed for discerning the fine details of the inhibitor binding mode to the active site, thus providing clues for the future design of even more selective inhibitors for druggable isoforms such as the cancer associated hCA IX and neuronal hCA VII.
Trvalý link: http://hdl.handle.net/11104/0200407
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