4m8y: Difference between revisions

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'''Unreleased structure'''
==GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions==
<StructureSection load='4m8y' size='340' side='right' caption='[[4m8y]], [[Resolution|resolution]] 2.22&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4m8y]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4M8Y OCA]. <br>
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KGQ:DIETHYL+({4-[(2S,3R)-2-({[(3R,3AS,6AR)-HEXAHYDROFURO[2,3-B]FURAN-3-YLOXY]CARBONYL}AMINO)-3-HYDROXY-4-{ISOBUTYL[(4-METHOXYPHENYL)SULFONYL]AMINO}BUTYL]PHENOXY}METHYL)PHOSPHONATE'>KGQ</scene><br>
<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2rkf|2rkf]], [[2rkg|2rkg]], [[4m8x|4m8x]]</td></tr>
<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span></td></tr>
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4m8y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4m8y OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4m8y RCSB], [http://www.ebi.ac.uk/pdbsum/4m8y PDBsum]</span></td></tr>
<table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Insertions in the protease (PR) region of human immunodeficiency virus (HIV) represent an interesting mechanism of antiviral resistance against HIV PR inhibitors (PIs). Here, we demonstrate the improved ability of a phosphonate-containing experimental HIV PI, GS-8374, relative to that of other PIs, to effectively inhibit patient-derived recombinant HIV strains bearing PR insertions and numerous other mutations. We correlate enzyme inhibition with the catalytic activities of corresponding recombinant PRs in vitro and provide a biochemical and structural analysis of the PR-inhibitor complex.


The entry 4m8y is ON HOLD  until Paper Publication
GS-8374, a prototype phosphonate-containing inhibitor of HIV-1 protease, effectively inhibits protease mutants with amino acid insertions.,Grantz Saskova K, Kozisek M, Stray K, de Jong D, Rezaova P, Brynda J, van Maarseveen NM, Nijhuis M, Cihlar T, Konvalinka J J Virol. 2014 Mar;88(6):3586-90. doi: 10.1128/JVI.02688-13. Epub 2013 Dec 26. PMID:24371077<ref>PMID:24371077</ref>


Authors: Grantz saskova, K., Brynda, J., Rezacova, P., Kozisek, M., Konvalinka, J.
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
 
</div>
Description: GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: HIV-1 retropepsin]]
[[Category: Brynda, J.]]
[[Category: Konvalinka, J.]]
[[Category: Kozisek, M.]]
[[Category: Rezacova, P.]]
[[Category: Saskova, K Grantz.]]
[[Category: Amino acid insertion]]
[[Category: Aspartic protease]]
[[Category: Hiv-1 protease]]
[[Category: Hydrolase-hydrolase inhibitor complex]]
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