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2fum

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[[Image:2fum.gif|left|200px]]
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{{STRUCTURE_2fum| PDB=2fum | SCENE= }}
{{STRUCTURE_2fum| PDB=2fum | SCENE= }}
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'''Catalytic domain of protein kinase PknB from Mycobacterium tuberculosis in complex with mitoxantrone'''
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===Catalytic domain of protein kinase PknB from Mycobacterium tuberculosis in complex with mitoxantrone===
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==Overview==
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Mycobacterium tuberculosis PknB is an essential receptor-like protein kinase involved in cell growth control. Here, we demonstrate that mitoxantrone, an anthraquinone derivative used in cancer therapy, is a PknB inhibitor capable of preventing mycobacterial growth. The structure of the complex reveals that mitoxantrone partially occupies the adenine-binding pocket in PknB, providing a framework for the design of compounds with potential therapeutic applications. PknB crystallizes as a 'back-to-back' homodimer identical to those observed in other structures of PknB in complex with ATP analogs. This organization resembles that of the RNA-dependent protein kinase PKR, suggesting a mechanism for kinase activation in mycobacteria.
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The line below this paragraph, {{ABSTRACT_PUBMED_16674948}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16674948 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16674948}}
==About this Structure==
==About this Structure==
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[[Category: Wehenkel, A.]]
[[Category: Wehenkel, A.]]
[[Category: Protein kinase-inhibitor complex]]
[[Category: Protein kinase-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:19:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 13:30:58 2008''

Revision as of 10:31, 29 July 2008

Template:STRUCTURE 2fum

Catalytic domain of protein kinase PknB from Mycobacterium tuberculosis in complex with mitoxantrone

Template:ABSTRACT PUBMED 16674948

About this Structure

2FUM is a Single protein structure of sequence from Mycobacterium tuberculosis. Full crystallographic information is available from OCA.

Reference

The structure of PknB in complex with mitoxantrone, an ATP-competitive inhibitor, suggests a mode of protein kinase regulation in mycobacteria., Wehenkel A, Fernandez P, Bellinzoni M, Catherinot V, Barilone N, Labesse G, Jackson M, Alzari PM, FEBS Lett. 2006 May 29;580(13):3018-22. Epub 2006 Apr 27. PMID:16674948

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