3tam
From Proteopedia
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| - | [[ | + | ==Crystal structure of HIV-1 reverse transcriptase (K103N mutant) in complex with inhibitor M06== |
| + | <StructureSection load='3tam' size='340' side='right' caption='[[3tam]], [[Resolution|resolution]] 2.51Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3tam]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Hiv-1_m:b_hxb2r Hiv-1 m:b_hxb2r]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3TAM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3TAM FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=M06:3-CHLORO-5-{[4-METHYL-2-OXO-1-(2H-PYRAZOLO[3,4-B]PYRIDIN-3-YLMETHYL)-1,2-DIHYDROPYRIDIN-3-YL]OXY}BENZONITRILE'>M06</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3t19|3t19]], [[3t1a|3t1a]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">gag-pol, HIV-1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11706 HIV-1 M:B_HXB2R])</td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3tam FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3tam OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3tam RCSB], [http://www.ebi.ac.uk/pdbsum/3tam PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constraint to replace the aryl ether core of MK-4965 (1) and the more rigid indazole constraint of MK-6186 (2). The resulting pyridone compounds are potent inhibitors of HIV RT and have antiviral activity in cell culture that is superior to other next generation NNRTI's. | ||
| - | + | Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.,Gomez R, Jolly S, Williams T, Tucker T, Tynebor R, Vacca J, McGaughey G, Lai MT, Felock P, Munshi V, DeStefano D, Touch S, Miller M, Yan Y, Sanchez R, Liang Y, Paton B, Wan BL, Anthony N Bioorg Med Chem Lett. 2011 Dec 15;21(24):7344-50. Epub 2011 Oct 17. PMID:22071300<ref>PMID:22071300</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
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==See Also== | ==See Also== | ||
*[[Reverse transcriptase|Reverse transcriptase]] | *[[Reverse transcriptase|Reverse transcriptase]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Hiv-1 m:b_hxb2r]] | [[Category: Hiv-1 m:b_hxb2r]] | ||
| - | [[Category: Yan, Y | + | [[Category: Yan, Y]] |
[[Category: Hiv-1]] | [[Category: Hiv-1]] | ||
[[Category: Hiv-1 reverse transcriptase]] | [[Category: Hiv-1 reverse transcriptase]] | ||
Revision as of 12:39, 9 December 2014
Crystal structure of HIV-1 reverse transcriptase (K103N mutant) in complex with inhibitor M06
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