Source:http://linkedlifedata.com/resource/pubmed/id/19186056
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2009-2-23
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pubmed:abstractText |
A sulfonamide derivative of the antihelmintic drug thiabendazole was prepared and investigated for inhibition of the zinc enzyme carbonic anhydrase CA (EC 4.2.1.1). Mammalian isoforms CA I-XIV and the nematode enzyme of Caenorhabditis elegans CAH-4b were included in this study. Thiabendazole-5-sulfonamide was a very effective inhibitor of CAH-4b and CA IX (K(I)s of 6.4-9.5nm) and also inhibited effectively isozymes CA I, II, IV-VII, and XII, with K(I)s in the range of 17.8-73.2nM. The high resolution X-ray crystal structure of its adduct with isozyme II evidenced the structural elements responsible for this potent inhibitory activity.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Caenorhabditis elegans Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrases,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/Thiabendazole
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1371-5
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pubmed:meshHeading |
pubmed-meshheading:19186056-Animals,
pubmed-meshheading:19186056-Caenorhabditis elegans,
pubmed-meshheading:19186056-Caenorhabditis elegans Proteins,
pubmed-meshheading:19186056-Carbonic Anhydrase Inhibitors,
pubmed-meshheading:19186056-Carbonic Anhydrases,
pubmed-meshheading:19186056-Crystallography, X-Ray,
pubmed-meshheading:19186056-Mammals,
pubmed-meshheading:19186056-Sulfonamides,
pubmed-meshheading:19186056-Thiabendazole
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pubmed:year |
2009
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pubmed:articleTitle |
A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases.
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pubmed:affiliation |
Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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