1hyz

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{{STRUCTURE_1hyz| PDB=1hyz | SCENE= }}
{{STRUCTURE_1hyz| PDB=1hyz | SCENE= }}
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'''HIV INTEGRASE CORE DOMAIN COMPLEXED WITH A DERIVATIVE OF TETRAPHENYL ARSONIUM.'''
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===HIV INTEGRASE CORE DOMAIN COMPLEXED WITH A DERIVATIVE OF TETRAPHENYL ARSONIUM.===
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==Overview==
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Integration of the reverse-transcribed HIV cDNA into the host DNA is a required step in viral replication. The virus-encoded integrase protein catalyzes the initial DNA breaking and joining reactions that mediate cDNA integration. Here, the identification by X-ray crystallography of a small-molecule binding site on the integrase catalytic domain is reported. The small-molecule family studied consists of a core of arsenic or phosphorus surrounded by four aromatic groups. Two arsenic derivatives were visualized bound to integrase. In each case, two molecules bound at symmetry-related sites on the catalytic domain dimer interface. The first compound studied, tetraphenyl arsonium, did not inhibit integrase. However, a synthetic compound substituting a catechol for one of the phenyl rings, dihydroxyphenyltriphenylarsonium, bound to the same site and did inhibit the enzyme. Changes in the vicinity of the catalytic site were seen with the inhibitory compound only, potentially explaining its mechanism of action. Further substituting phosphonium for arsonium yielded a compound with an IC(50) in the low micromolar range. These findings may be useful in designing new inhibitors of integrase, which is at present the only one of the three HIV enzymes for which clinically useful inhibitors are not available.
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The line below this paragraph, {{ABSTRACT_PUBMED_11264582}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 11264582 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11264582}}
==About this Structure==
==About this Structure==
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[[Category: Siegel, J S.]]
[[Category: Siegel, J S.]]
[[Category: Dna integration]]
[[Category: Dna integration]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 19:22:48 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 10:09:17 2008''

Revision as of 07:09, 1 July 2008

Image:1hyz.png

Template:STRUCTURE 1hyz

HIV INTEGRASE CORE DOMAIN COMPLEXED WITH A DERIVATIVE OF TETRAPHENYL ARSONIUM.

Template:ABSTRACT PUBMED 11264582

About this Structure

1HYZ is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Identification of a small-molecule binding site at the dimer interface of the HIV integrase catalytic domain., Molteni V, Greenwald J, Rhodes D, Hwang Y, Kwiatkowski W, Bushman FD, Siegel JS, Choe S, Acta Crystallogr D Biol Crystallogr. 2001 Apr;57(Pt 4):536-44. PMID:11264582

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