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3lpt

From Proteopedia

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{{Seed}}
 
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[[Image:3lpt.jpg|left|200px]]
 
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<!--
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==HIV integrase==
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The line below this paragraph, containing "STRUCTURE_3lpt", creates the "Structure Box" on the page.
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<StructureSection load='3lpt' size='340' side='right'caption='[[3lpt]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3lpt]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/9hiv1 9hiv1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3LPT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3LPT FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=723:(6-CHLORO-2-OXO-4-PHENYL-1,2-DIHYDROQUINOLIN-3-YL)ACETIC+ACID'>723</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=P03:2-[3-[3-(2-HYDROXYETHOXY)PROPOXY]PROPOXY]ETHANOL'>P03</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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-->
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<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CAF:S-DIMETHYLARSINOYL-CYSTEINE'>CAF</scene></td></tr>
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{{STRUCTURE_3lpt| PDB=3lpt | SCENE= }}
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1hyv|1hyv]], [[3lpu|3lpu]]</div></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3lpt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3lpt OCA], [https://pdbe.org/3lpt PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3lpt RCSB], [https://www.ebi.ac.uk/pdbsum/3lpt PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3lpt ProSAT]</span></td></tr>
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</table>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/lp/3lpt_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3lpt ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Lens epithelium-derived growth factor (LEDGF/p75) is a cellular cofactor of HIV-1 integrase that promotes viral integration by tethering the preintegration complex to the chromatin. By virtue of its crucial role in the early steps of HIV replication, the interaction between LEDGF/p75 and integrase represents an attractive target for antiviral therapy. We have rationally designed a series of 2-(quinolin-3-yl)acetic acid derivatives (LEDGINs) that act as potent inhibitors of the LEDGF/p75-integrase interaction and HIV-1 replication at submicromolar concentration by blocking the integration step. A 1.84-A resolution crystal structure corroborates the binding of the inhibitor in the LEDGF/p75-binding pocket of integrase. Together with the lack of cross-resistance with two clinical integrase inhibitors, these findings define the 2-(quinolin-3-yl)acetic acid derivatives as the first genuine allosteric HIV-1 integrase inhibitors. Our work demonstrates the feasibility of rational design of small molecules inhibiting the protein-protein interaction between a viral protein and a cellular host factor.
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===HIV integrase===
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Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication.,Christ F, Voet A, Marchand A, Nicolet S, Desimmie BA, Marchand D, Bardiot D, Van der Veken NJ, Van Remoortel B, Strelkov SV, De Maeyer M, Chaltin P, Debyser Z Nat Chem Biol. 2010 Jun;6(6):442-8. Epub 2010 May 16. PMID:20473303<ref>PMID:20473303</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3lpt" style="background-color:#fffaf0;"></div>
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==About this Structure==
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==See Also==
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3LPT is a 1 chain structure with sequence from [http://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=3LPT OCA].
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*[[Retroviral integrase 3D structures|Retroviral integrase 3D structures]]
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[[Category: Human immunodeficiency virus 1]]
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== References ==
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[[Category: Chaltin, P.]]
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<references/>
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[[Category: Christ, F.]]
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__TOC__
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[[Category: Debyzer, Z.]]
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</StructureSection>
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[[Category: Maeyer, M de.]]
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[[Category: Large Structures]]
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[[Category: Marchand, A.]]
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[[Category: Chaltin, P]]
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[[Category: Nicolet, S.]]
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[[Category: Christ, F]]
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[[Category: Strelkov, S V.]]
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[[Category: Debyzer, Z]]
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[[Category: Voet, A.]]
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[[Category: Maeyer, M de]]
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[[Category: Marchand, A]]
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[[Category: Nicolet, S]]
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[[Category: Strelkov, S V]]
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[[Category: Voet, A]]
[[Category: Endonuclease]]
[[Category: Endonuclease]]
[[Category: Hiv]]
[[Category: Hiv]]
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[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Viral protein]]
[[Category: Viral protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed May 12 11:19:36 2010''
 

Current revision

HIV integrase

PDB ID 3lpt

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