1zj7

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{{STRUCTURE_1zj7| PDB=1zj7 | SCENE= }}
{{STRUCTURE_1zj7| PDB=1zj7 | SCENE= }}
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'''Crystal structure of a complex of mutant HIV-1 protease (A71V, V82T, I84V) with a hydroxyethylamine peptidomimetic inhibitor BOC-PHE-PSI[S-CH(OH)CH2NH]-PHE-GLU-PHE-NH2'''
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===Crystal structure of a complex of mutant HIV-1 protease (A71V, V82T, I84V) with a hydroxyethylamine peptidomimetic inhibitor BOC-PHE-PSI[S-CH(OH)CH2NH]-PHE-GLU-PHE-NH2===
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==Overview==
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Two new X-ray structures of an HIV-1 protease mutant (A71V, V82T, I84V) in complex with inhibitors SE and SQ, pseudotetrapeptide inhibitors with an acyclic S-hydroxyethylamine isostere, were determined. Comparison of eight structures exploring the binding of four similar inhibitors--SE, SQ (S-hydroxyethylamine isostere), OE (ethyleneamine), and QF34 (hydroxyethylene)--to wild-type and A71V/V82T/I84V HIV-1 protease elucidates the principles of altered interaction with changing conditions. The A71V mutation, which is distant from the active site, causes changes in the structure of the enzyme detectable by the means of X-ray structure analysis, and a route of propagation of the effect toward the active site is proposed.
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(as it appears on PubMed at http://www.pubmed.gov), where 16970402 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16970402}}
==About this Structure==
==About this Structure==
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[[Category: Peptidomimetic]]
[[Category: Peptidomimetic]]
[[Category: Protease]]
[[Category: Protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:41:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:40:54 2008''

Revision as of 09:40, 28 July 2008

Image:1zj7.png

Template:STRUCTURE 1zj7

Crystal structure of a complex of mutant HIV-1 protease (A71V, V82T, I84V) with a hydroxyethylamine peptidomimetic inhibitor BOC-PHE-PSI[S-CH(OH)CH2NH]-PHE-GLU-PHE-NH2

Template:ABSTRACT PUBMED 16970402

About this Structure

1ZJ7 is a Single protein structure of sequence from Human immunodeficiency virus. Full crystallographic information is available from OCA.

Reference

HIV-1 protease mutations and inhibitor modifications monitored on a series of complexes. Structural basis for the effect of the A71V mutation on the active site., Skalova T, Dohnalek J, Duskova J, Petrokova H, Hradilek M, Soucek M, Konvalinka J, Hasek J, J Med Chem. 2006 Sep 21;49(19):5777-84. PMID:16970402

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