3sfi

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[[Image:3sfi.png|left|200px]]
 
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{{STRUCTURE_3sfi| PDB=3sfi | SCENE= }}
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===Ethionamide Boosters Part 2: Combining Bioisosteric Replacement and Structure-Based Drug Design to Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors.===
===Ethionamide Boosters Part 2: Combining Bioisosteric Replacement and Structure-Based Drug Design to Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors.===
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{{ABSTRACT_PUBMED_22098589}}
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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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{{ABSTRACT_PUBMED_22098589}}
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==About this Structure==
==About this Structure==
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[[3sfi]] 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=3SFI OCA].
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[[3sfi]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Uncultured_bacterium_'eubacterium_sp.' Uncultured bacterium 'eubacterium sp.']. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3SFI OCA].
==Reference==
==Reference==
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<ref group="xtra">PMID:022098589</ref><references group="xtra"/>
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<ref group="xtra">PMID:022098589</ref><references group="xtra"/><references/>
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[[Category: Mycobacterium tuberculosis]]
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[[Category: Uncultured bacterium 'eubacterium sp.']]
[[Category: Baulard, A R.]]
[[Category: Baulard, A R.]]
[[Category: Blondiaux, N.]]
[[Category: Blondiaux, N.]]

Revision as of 04:48, 9 April 2014

Template:STRUCTURE 3sfi

Contents

Ethionamide Boosters Part 2: Combining Bioisosteric Replacement and Structure-Based Drug Design to Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors.

Template:ABSTRACT PUBMED 22098589

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

3sfi is a 1 chain structure with sequence from Uncultured bacterium 'eubacterium sp.'. Full crystallographic information is available from OCA.

Reference

  • Flipo M, Desroses M, Lecat-Guillet N, Villemagne B, Blondiaux N, Leroux F, Piveteau C, Mathys V, Flament MP, Siepmann J, Villeret V, Wohlkonig A, Wintjens R, Soror SH, Christophe T, Jeon HK, Locht C, Brodin P, Deprez BP, Baulard A, Willand N. Ethionamide Boosters Part 2: Combining Bioisosteric Replacement and Structure-Based Drug Design to Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors. J Med Chem. 2011 Nov 20. PMID:22098589 doi:10.1021/jm200825u
  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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