1t56

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{{STRUCTURE_1t56| PDB=1t56 | SCENE= }}
{{STRUCTURE_1t56| PDB=1t56 | SCENE= }}
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'''Crystal structure of TetR family repressor M. tuberculosis EthR'''
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===Crystal structure of TetR family repressor M. tuberculosis EthR===
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==Overview==
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Ethionamide has been used for more than 30 years as a second-line chemotherapeutic to treat tuberculosis patients who have developed resistance to first-line drugs, such as isoniazid (INH) and rifampicin. Activation of the pro-drug ethionamide is regulated by the Baeyer-Villiger monooxygenase EthA and the TetR/CamR family repressor EthR, whose open reading frames are separated by 75 bp on the Mycobacterium tuberculosis genome. EthR has been shown to repress transcription of the activator gene ethA by binding to this intergenic region, thus contributing to ethionamide resistance. We have determined the crystal structure of EthR, to 1.7A resolution, revealing a dimeric two-domain molecule with an overall architecture typical for TetR/CamR repressor proteins. A 20A long hydrophobic tunnel-like cavity in the "drug-binding" domain of EthR is occupied by two 1,4-dioxane molecules, a component of the crystallisation buffer. Comparing the present structure to those of the homologues Staphylococcus aureus QacR and Escherichia coli TetR leads to the hypothesis that the hydrophobic cavity constitutes a binding site for an as yet unknown ligand that might regulate DNA-binding of EthR.
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(as it appears on PubMed at http://www.pubmed.gov), where 15236969 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15236969}}
==About this Structure==
==About this Structure==
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[[Category: Helix-turn-helix]]
[[Category: Helix-turn-helix]]
[[Category: Tetr family]]
[[Category: Tetr family]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:32:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:55:04 2008''

Revision as of 16:55, 27 July 2008

Image:1t56.png

Template:STRUCTURE 1t56

Crystal structure of TetR family repressor M. tuberculosis EthR

Template:ABSTRACT PUBMED 15236969

About this Structure

1T56 is a Single protein structure of sequence from Mycobacterium tuberculosis h37rv. Full crystallographic information is available from OCA.

Reference

Crystal structure of the TetR/CamR family repressor Mycobacterium tuberculosis EthR implicated in ethionamide resistance., Dover LG, Corsino PE, Daniels IR, Cocklin SL, Tatituri V, Besra GS, Futterer K, J Mol Biol. 2004 Jul 23;340(5):1095-105. PMID:15236969

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