4dw6

From Proteopedia

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'''Unreleased structure'''
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{{STRUCTURE_4dw6| PDB=4dw6 | SCENE= }}
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===Novel N-phenyl-phenoxyacetamide derivatives as potential EthR inhibitors and ethionamide boosters. Discovery and optimization using High-Throughput Synthesis.===
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{{ABSTRACT_PUBMED_022738293}}
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The entry 4dw6 is ON HOLD until Mar 27 2014
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==Function==
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[[http://www.uniprot.org/uniprot/ETHR_MYCTU ETHR_MYCTU]] Involved in the repression of the monooxygenase EthA which is responsible of the formation of the active metabolite of ethionamide (ETH).<ref>PMID:10869356</ref><ref>PMID:10944230</ref>
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Authors: Flipo, M., Willand, N., Lecat-Guillet, N., Hounsou, C., Desroses, M., Leroux, F., Lens, Z., Villeret, V., Wohlkonig, A., Wintjens, R., Christophe, T., Jeon, H.K., Locht, C., Brodin, P., Baulard, A.R., Deprez, B.
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==About this Structure==
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[[4dw6]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mycobacterium_tuberculosis Mycobacterium tuberculosis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4DW6 OCA].
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Description: Novel N-phenyl-phenoxyacetamide derivatives as potential EthR inhibitors and ethionamide boosters. Discovery and optimization using High-Throughput Synthesis.
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==Reference==
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<references group="xtra"/><references/>
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[[Category: Mycobacterium tuberculosis]]
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[[Category: Baulard, A R.]]
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[[Category: Brodin, P.]]
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[[Category: Christophe, T.]]
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[[Category: Deprez, B.]]
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[[Category: Desroses, M.]]
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[[Category: Flipo, M.]]
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[[Category: Hounsou, C.]]
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[[Category: Jeon, H K.]]
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[[Category: Lecat-Guillet, N.]]
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[[Category: Lens, Z.]]
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[[Category: Leroux, F.]]
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[[Category: Locht, C.]]
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[[Category: Villeret, V.]]
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[[Category: Willand, N.]]
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[[Category: Wintjens, R.]]
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[[Category: Wohlkonig, A.]]
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[[Category: Dna binding protein]]
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[[Category: Inhibitor]]
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[[Category: Tetr-family]]
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[[Category: Transcription repressor-inhibitor complex]]
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[[Category: Transcription-inhibitor complex]]
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[[Category: Transcritptional regulatory repressor]]

Revision as of 08:56, 27 March 2013

Template:STRUCTURE 4dw6

Contents

Novel N-phenyl-phenoxyacetamide derivatives as potential EthR inhibitors and ethionamide boosters. Discovery and optimization using High-Throughput Synthesis.

Template:ABSTRACT PUBMED 022738293

Function

[ETHR_MYCTU] Involved in the repression of the monooxygenase EthA which is responsible of the formation of the active metabolite of ethionamide (ETH).[1][2]

About this Structure

4dw6 is a 1 chain structure with sequence from Mycobacterium tuberculosis. Full crystallographic information is available from OCA.

Reference

  1. ↑ Baulard AR, Betts JC, Engohang-Ndong J, Quan S, McAdam RA, Brennan PJ, Locht C, Besra GS. Activation of the pro-drug ethionamide is regulated in mycobacteria. J Biol Chem. 2000 Sep 8;275(36):28326-31. PMID:10869356 doi:10.1074/jbc.M003744200
  2. ↑ DeBarber AE, Mdluli K, Bosman M, Bekker LG, Barry CE 3rd. Ethionamide activation and sensitivity in multidrug-resistant Mycobacterium tuberculosis. Proc Natl Acad Sci U S A. 2000 Aug 15;97(17):9677-82. PMID:10944230

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OCA

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