1u9n

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{{STRUCTURE_1u9n| PDB=1u9n | SCENE= }}
{{STRUCTURE_1u9n| PDB=1u9n | SCENE= }}
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'''Crystal structure of the transcriptional regulator EthR in a ligand bound conformation opens therapeutic perspectives against tuberculosis and leprosy'''
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===Crystal structure of the transcriptional regulator EthR in a ligand bound conformation opens therapeutic perspectives against tuberculosis and leprosy===
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==Overview==
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Mycobacterium tuberculosis EthR is a repressor of ethA, a gene encoding a mono-oxygenase required for the activation of the prodrug ethionamide. Here we describe the X-ray crystal structure of EthR, a homodimer with an entirely helical structure showing similarities to TetR family members. Each monomer contained a fortuitous ligand identified as hexadecyl octanoate. The crystal structure of EthR purified in M. smegmatis revealed the presence of a comparable ligand. The binding of hexadecyl octanoate to EthR induces a conformational state incompatible with repressor function, which should lead to ethA derepression and consequently to an increased sensitivity to ethionamide and other thioamides. A related, more hydrophilic ketone was found to exhibit synergistic antimycobacterial effects when tested together with ethionamide, indicating that this strategy may help reduce the dosage of potent antibacterial compounds that otherwise are too toxic to be used as first-line drugs.
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(as it appears on PubMed at http://www.pubmed.gov), where 15494316 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15494316}}
==About this Structure==
==About this Structure==
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[[Category: Tetr family]]
[[Category: Tetr family]]
[[Category: Transcriptional repressor]]
[[Category: Transcriptional repressor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:56:21 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 17:14:12 2008''

Revision as of 14:14, 27 July 2008

Image:1u9n.png

Template:STRUCTURE 1u9n

Crystal structure of the transcriptional regulator EthR in a ligand bound conformation opens therapeutic perspectives against tuberculosis and leprosy

Template:ABSTRACT PUBMED 15494316

About this Structure

Full crystallographic information is available from OCA.

Reference

Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis., Frenois F, Engohang-Ndong J, Locht C, Baulard AR, Villeret V, Mol Cell. 2004 Oct 22;16(2):301-7. PMID:15494316

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