2hkj

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[[Image:2hkj.gif|left|200px]]
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{{Seed}}
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[[Image:2hkj.png|left|200px]]
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{{STRUCTURE_2hkj| PDB=2hkj | SCENE= }}
{{STRUCTURE_2hkj| PDB=2hkj | SCENE= }}
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'''Topoisomerase VI-B bound to radicicol'''
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===Topoisomerase VI-B bound to radicicol===
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==Overview==
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Members of the GHL ATPase superfamily, including type II topoisomerases, Hsp90-class chaperones, and MutL, all share a common GHKL-type ATP-binding fold and act as nucleotide-controlled 'molecular clamps'. These enzymes' ATP-binding sites have proven to be rich drug targets, and certain inhibitors of type II topoisomerases and Hsp90 bind to this region and competitively inhibit these enzymes. Recently, it was found that radicicol, a drug known to block Hsp90 function, also inhibits the archaeal type IIB topoisomerase topo VI. Here, we use X-ray crystallography to show that despite low sequence identity ( approximately 10-12%) between topo VI and Hsp90, radicicol binds to the ATPase sites of these two enzymes in an equivalent manner. We further demonstrate that radicicol inhibits both the dimerization of the topo VI ATPase domains and ATP hydrolysis, two critical steps in the enzyme's strand passage reaction. This work contributes to a growing set of structures detailing the interactions between GHL-family proteins and various drugs, and reveals radicicol as a versatile scaffold for targeting distantly related GHL enzymes.
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The line below this paragraph, {{ABSTRACT_PUBMED_16920739}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16920739 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16920739}}
==About this Structure==
==About this Structure==
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[[Category: Radicicol]]
[[Category: Radicicol]]
[[Category: Topoisomerase]]
[[Category: Topoisomerase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:23:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:44:34 2008''

Revision as of 00:44, 28 July 2008

Image:2hkj.png

Template:STRUCTURE 2hkj

Topoisomerase VI-B bound to radicicol

Template:ABSTRACT PUBMED 16920739

About this Structure

2HKJ is a Single protein structure of sequence from Sulfolobus shibatae. Full crystallographic information is available from OCA.

Reference

Structural basis for topoisomerase VI inhibition by the anti-Hsp90 drug radicicol., Corbett KD, Berger JM, Nucleic Acids Res. 2006;34(15):4269-77. Epub 2006 Aug 18. PMID:16920739

Page seeded by OCA on Mon Jul 28 03:44:34 2008

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