2bow

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{{STRUCTURE_2bow| PDB=2bow | SCENE= }}
{{STRUCTURE_2bow| PDB=2bow | SCENE= }}
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'''MULTIDRUG-BINDING DOMAIN OF TRANSCRIPTION ACTIVATOR BMRR IN COMPLEX WITH A LIGAND, TETRAPHENYLPHOSPHONIUM'''
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===MULTIDRUG-BINDING DOMAIN OF TRANSCRIPTION ACTIVATOR BMRR IN COMPLEX WITH A LIGAND, TETRAPHENYLPHOSPHONIUM===
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==Overview==
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Multidrug-efflux transporters demonstrate an unusual ability to recognize multiple structurally dissimilar toxins. A comparable ability to bind diverse hydrophobic cationic drugs is characteristic of the Bacillus subtilis transcription regulator BmrR, which upon drug binding activates expression of the multidrug transporter Bmr. Crystal structures of the multidrug-binding domain of BmrR (2.7 A resolution) and of its complex with the drug tetraphenylphosphonium (2.8 A resolution) revealed a drug-induced unfolding and relocation of an alpha helix, which exposes an internal drug-binding pocket. Tetraphenylphosphonium binding is mediated by stacking and van der Waals contacts with multiple hydrophobic residues of the pocket and by an electrostatic interaction between the positively charged drug and a buried glutamate residue, which is the key to cation selectivity. Similar binding principles may be used by other multidrug-binding proteins.
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(as it appears on PubMed at http://www.pubmed.gov), where 10025401 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10025401}}
==About this Structure==
==About this Structure==
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[[Category: Multidrug binding]]
[[Category: Multidrug binding]]
[[Category: Transcription activator]]
[[Category: Transcription activator]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:35:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 05:15:27 2008''

Revision as of 02:15, 29 July 2008

Template:STRUCTURE 2bow

MULTIDRUG-BINDING DOMAIN OF TRANSCRIPTION ACTIVATOR BMRR IN COMPLEX WITH A LIGAND, TETRAPHENYLPHOSPHONIUM

Template:ABSTRACT PUBMED 10025401

About this Structure

2BOW is a Single protein structure of sequence from Bacillus subtilis. Full crystallographic information is available from OCA.

Reference

Structural basis of multidrug recognition by BmrR, a transcription activator of a multidrug transporter., Zheleznova EE, Markham PN, Neyfakh AA, Brennan RG, Cell. 1999 Feb 5;96(3):353-62. PMID:10025401

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