1w6f
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(New page: 200px<br /> <applet load="1w6f" size="450" color="white" frame="true" align="right" spinBox="true" caption="1w6f, resolution 2.100Å" /> '''ARYLAMINE N-ACETYL...)
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Revision as of 19:03, 29 October 2007
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ARYLAMINE N-ACETYLTRANSFERASE FROM MYCOBACTERIUM SMEGMATIS WITH THE ANTI-TUBERCULAR DRUG ISONIAZID BOUND IN THE ACTIVE SITE.
Overview
Isoniazid is a frontline drug used in the treatment of tuberculosis (TB)., Isoniazid is a prodrug, requiring activation in the mycobacterial cell by, the catalase/peroxidase activity of the katG gene product. TB kills two, million people every year and the situation is getting worse due to the, increase in prevalence of HIV/AIDS and emergence of multidrug-resistant, strains of TB. Arylamine N-acetyltransferase (NAT) is a drug-metabolizing, enzyme (E.C. 2.1.3.5). NAT can acetylate isoniazid, transferring an acetyl, group from acetyl coenzyme A onto the terminal nitrogen of the drug, which, in its N-acetylated form is therapeutically inactive. The bacterium, responsible for TB, Mycobacterium tuberculosis, contains and expresses the, gene encoding the NAT protein. Isoniazid binds to the NAT ... [(full description)]
About this Structure
1W6F is a [Single protein] structure of sequence from [Mycobacterium smegmatis] with ISZ as [ligand]. Active as [[1]], with EC number [2.3.1.5]. Full crystallographic information is available from [OCA].
Reference
Binding of the anti-tubercular drug isoniazid to the arylamine N-acetyltransferase protein from Mycobacterium smegmatis., Sandy J, Holton S, Fullam E, Sim E, Noble M, Protein Sci. 2005 Mar;14(3):775-82. PMID:15722451
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