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''' | ==GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions== | ||
<StructureSection load='4m8x' size='340' side='right' caption='[[4m8x]], [[Resolution|resolution]] 2.05Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[4m8x]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4M8X 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]], [[4m8y|4m8y]]</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=4m8x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4m8x OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4m8x RCSB], [http://www.ebi.ac.uk/pdbsum/4m8x 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. | |||
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> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
== 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: Aspartic protease]] | |||
[[Category: Gs8374]] | |||
[[Category: Hiv protease]] | |||
[[Category: Hydrolase-hydrolase inhibitor complex]] | |||
Revision as of 11:15, 7 May 2014
GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid InsertionsGS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions
Structural highlights
Publication Abstract from PubMedInsertions 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. 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[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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