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Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides
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SYSNO ASEP 0365071 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides Author(s) Mader, Pavel (UMG-J)
Brynda, Jiří (UMG-J) RID
Gitto, R. (IT)
Agnello, S. (IT)
Pachl, Petr (UMG-J)
Supuran, C. T. (IT)
Chimirri, A. (IT)
Řezáčová, Pavlína (UOCHB-X) RID, ORCIDSource Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 54, č. 7 (2011), s. 2522-2526Number of pages 5 s. Language eng - English Country US - United States Keywords carbonic anhydrase ; isoquinolinesulfonamides ; selective inhibition ; crystal structure Subject RIV EB - Genetics ; Molecular Biology R&D Projects GA203/09/0820 GA ČR - Czech Science Foundation (CSF) CEZ AV0Z50520514 - UMG-J (2005-2011) AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000289215700048 DOI 10.1021/jm2000213 Annotation 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. Workplace Institute of Molecular Genetics Contact Nikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217 Year of Publishing 2012
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