4m8y: Difference between revisions
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New page: '''Unreleased structure''' The entry 4m8y is ON HOLD Authors: Grantz Saskova, K., Brynda, J., Rezacova, P., Kozisek, M., Konvalinka, J. Description: GS-8374, a Novel Phosphonate-Contai... |
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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='4m8y' size='340' side='right'caption='[[4m8y]], [[Resolution|resolution]] 2.22Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[4m8y]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4M8Y OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4M8Y FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.22Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4m8y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4m8y OCA], [https://pdbe.org/4m8y PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4m8y RCSB], [https://www.ebi.ac.uk/pdbsum/4m8y PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4m8y ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/Q90JJ9_9HIV1 Q90JJ9_9HIV1] | |||
<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> | |||
<div class="pdbe-citations 4m8y" style="background-color:#fffaf0;"></div> | |||
==See Also== | |||
*[[Immunodeficiency virus protease 3D structures|Immunodeficiency virus protease 3D structures]] | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Human immunodeficiency virus 1]] | |||
[[Category: Large Structures]] | |||
[[Category: Brynda J]] | |||
[[Category: Grantz saskova K]] | |||
[[Category: Konvalinka J]] | |||
[[Category: Kozisek M]] | |||
[[Category: Rezacova P]] | |||
Latest revision as of 16:34, 20 September 2023
GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease, Effectively Inhibits HIV PR Mutants with Amino Acid Insertions
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