5gon: Difference between revisions
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==Structures of a beta-lactam bridged analogue in complex with tubulin== | |||
<StructureSection load='5gon' size='340' side='right' caption='[[5gon]], [[Resolution|resolution]] 2.48Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5gon]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/ ], [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5GON OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5GON FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6ZR:(3R,4R)-4-(4-METHOXY-3-OXIDANYL-PHENYL)-3-METHYL-1-(3,4,5-TRIMETHOXYPHENYL)AZETIDIN-2-ONE'>6ZR</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4o2b|4o2b]]</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=5gon FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5gon OCA], [http://pdbe.org/5gon PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5gon RCSB], [http://www.ebi.ac.uk/pdbsum/5gon PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5gon ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[[http://www.uniprot.org/uniprot/TBA1B_BOVIN TBA1B_BOVIN]] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain. [[http://www.uniprot.org/uniprot/STMN4_RAT STMN4_RAT]] Exhibits microtubule-destabilizing activity.<ref>PMID:15039434</ref> <ref>PMID:12111843</ref> <ref>PMID:15014504</ref> [[http://www.uniprot.org/uniprot/TBB2B_BOVIN TBB2B_BOVIN]] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity). | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
A series of chiral beta-lactam bridged analogues (3-substituted 1,4-diaryl-2-azetidinones) of combretastatin A-4 (CA-4) were synthesized asymmetrically, and their antitumor activities were evaluated in vitro and in vivo. The cocrystal structure of tubulin in complex with compound 9 was determined by X-ray crystallography, which showed that 9 binds to the same site as colchicine with similar binding mode, and the absolute configuration of its C-4 was first identified and demonstrated to be critically important for their antiproliferative activities. | |||
Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.,Zhou P, Liu Y, Zhou L, Zhu K, Feng K, Zhang H, Liang Y, Jiang H, Luo C, Liu M, Wang Y J Med Chem. 2016 Nov 23;59(22):10329-10334. Epub 2016 Nov 14. PMID:27805821<ref>PMID:27805821</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: | <div class="pdbe-citations 5gon" style="background-color:#fffaf0;"></div> | ||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Bos taurus]] | |||
[[Category: Rattus norvegicus]] | |||
[[Category: Cheng, L]] | [[Category: Cheng, L]] | ||
[[Category: Liu, Y]] | [[Category: Liu, Y]] | ||
[[Category: Wang, Y]] | |||
[[Category: Zhou, L]] | [[Category: Zhou, L]] | ||
[[Category: Beta-lactam bridged analogue tubulin colchicine binding site]] | |||
[[Category: Structural protein]] | |||
Revision as of 16:14, 22 March 2017
Structures of a beta-lactam bridged analogue in complex with tubulin
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