Počet záznamů: 1

Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides

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    0365071 - UMG-J 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
    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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