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2cig
From Proteopedia
(New page: 200px<br /> <applet load="2cig" size="450" color="white" frame="true" align="right" spinBox="true" caption="2cig, resolution 1.90Å" /> '''DIHYDROFOLATE REDUC...) |
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==About this Structure== | ==About this Structure== | ||
| - | 2CIG is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Mycobacterium_tuberculosis Mycobacterium tuberculosis]] with SO4, 1DG and GOL as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.5.1.3 1.5.1.3]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2CIG OCA]]. | + | 2CIG is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Mycobacterium_tuberculosis Mycobacterium tuberculosis]] with SO4, 1DG and GOL as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/Dihydrofolate_reductase Dihydrofolate reductase]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.5.1.3 1.5.1.3]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2CIG OCA]]. |
==Reference== | ==Reference== | ||
Mycobacterium tuberculosis dihydrofolate reductase is a target for isoniazid., Argyrou A, Vetting MW, Aladegbami B, Blanchard JS, Nat Struct Mol Biol. 2006 May;13(5):408-13. Epub 2006 Apr 30. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16648861 16648861] | Mycobacterium tuberculosis dihydrofolate reductase is a target for isoniazid., Argyrou A, Vetting MW, Aladegbami B, Blanchard JS, Nat Struct Mol Biol. 2006 May;13(5):408-13. Epub 2006 Apr 30. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16648861 16648861] | ||
| + | [[Category: Dihydrofolate reductase]] | ||
[[Category: Mycobacterium tuberculosis]] | [[Category: Mycobacterium tuberculosis]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: tuberculosis]] | [[Category: tuberculosis]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 14:10:25 2007'' |
Revision as of 12:05, 30 October 2007
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DIHYDROFOLATE REDUCTASE FROM MYCOBACTERIUM TUBERCULOSIS INHIBITED BY THE ACYCLIC 4R ISOMER OF INH-NADP A DERIVATIVE OF THE PRODRUG ISONIAZID.
Overview
Isoniazid is a key drug used in the treatment of tuberculosis. Isoniazid, is a pro-drug, which, after activation by the katG-encoded catalase, peroxidase, reacts nonenzymatically with NAD(+) and NADP(+) to generate, several isonicotinoyl adducts of these pyridine nucleotides. One of these, the acyclic 4S isomer of isoniazid-NAD, targets the inhA-encoded enoyl-ACP, reductase, an enzyme essential for mycolic acid biosynthesis in, Mycobacterium tuberculosis. Here we show that the acyclic 4R isomer of, isoniazid-NADP inhibits the M. tuberculosis dihydrofolate reductase, (DHFR), an enzyme essential for nucleic acid synthesis. This biologically, relevant form of the isoniazid adduct is a subnanomolar bisubstrate, inhibitor of M. tuberculosis DHFR. Expression of M. tuberculosis DHFR in, ... [(full description)]
About this Structure
2CIG is a [Single protein] structure of sequence from [Mycobacterium tuberculosis] with SO4, 1DG and GOL as [ligands]. Active as [Dihydrofolate reductase], with EC number [1.5.1.3]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
Mycobacterium tuberculosis dihydrofolate reductase is a target for isoniazid., Argyrou A, Vetting MW, Aladegbami B, Blanchard JS, Nat Struct Mol Biol. 2006 May;13(5):408-13. Epub 2006 Apr 30. PMID:16648861
Page seeded by OCA on Tue Oct 30 14:10:25 2007
