1zlf: Difference between revisions

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New page: left|200px<br /> <applet load="1zlf" size="450" color="white" frame="true" align="right" spinBox="true" caption="1zlf, resolution 2.30Å" /> '''Crystal structure o...
 
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[[Image:1zlf.gif|left|200px]]<br />
[[Image:1zlf.gif|left|200px]]<br /><applet load="1zlf" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="1zlf" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="1zlf, resolution 2.30&Aring;" />
caption="1zlf, resolution 2.30&Aring;" />
'''Crystal structure of a complex of mutant HIV-1 protease (A71V, V82T, I84V) with a hydroxyethylamine peptidomimetic inhibitor'''<br />
'''Crystal structure of a complex of mutant HIV-1 protease (A71V, V82T, I84V) with a hydroxyethylamine peptidomimetic inhibitor'''<br />


==Overview==
==Overview==
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.
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.


==About this Structure==
==About this Structure==
1ZLF is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_2 Human immunodeficiency virus 2] with NH2 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1ZLF OCA].  
1ZLF is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_2 Human immunodeficiency virus 2] with <scene name='pdbligand=NH2:'>NH2</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1ZLF OCA].  


==Reference==
==Reference==
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[[Category: hiv; protease; inhibitor; peptidomimetic]]
[[Category: hiv; protease; inhibitor; peptidomimetic]]


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