5njh

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Current revision (13:01, 15 November 2023) (edit) (undo)
 
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==Triazolopyrimidines stabilize microtubules by binding to the vinca inhibitor site of tubulin==
==Triazolopyrimidines stabilize microtubules by binding to the vinca inhibitor site of tubulin==
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<StructureSection load='5njh' size='340' side='right' caption='[[5njh]], [[Resolution|resolution]] 2.39&Aring;' scene=''>
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<StructureSection load='5njh' size='340' side='right'caption='[[5njh]], [[Resolution|resolution]] 2.39&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5njh]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat] and [http://en.wikipedia.org/wiki/Chick Chick]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NJH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5NJH FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5njh]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [https://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NJH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5NJH FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8Z8:5-chloranyl-7-[(1~{R},5~{S})-3-methoxy-8-azabicyclo[3.2.1]octan-8-yl]-6-[2,4,6-tris(fluoranyl)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine'>8Z8</scene>, <scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.394&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Stmn4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat]), TTL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9031 CHICK])</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8Z8:5-chloranyl-7-[(1~{R},5~{S})-3-methoxy-8-azabicyclo[3.2.1]octan-8-yl]-6-[2,4,6-tris(fluoranyl)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine'>8Z8</scene>, <scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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<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=5njh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5njh OCA], [http://pdbe.org/5njh PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5njh RCSB], [http://www.ebi.ac.uk/pdbsum/5njh PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5njh ProSAT]</span></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=5njh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5njh OCA], [https://pdbe.org/5njh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5njh RCSB], [https://www.ebi.ac.uk/pdbsum/5njh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5njh ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[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).
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[https://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.
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 5njh" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 5njh" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Stathmin-4 3D structures|Stathmin-4 3D structures]]
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*[[Tubulin tyrosine ligase|Tubulin tyrosine ligase]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Bos taurus]]
[[Category: Bos taurus]]
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[[Category: Buffalo rat]]
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[[Category: Gallus gallus]]
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[[Category: Chick]]
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[[Category: Large Structures]]
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[[Category: Calvo, G S]]
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[[Category: Rattus norvegicus]]
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[[Category: Diaz, J F]]
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[[Category: Calvo GS]]
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[[Category: Prota, A E]]
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[[Category: Diaz JF]]
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[[Category: Sharma, A]]
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[[Category: Prota AE]]
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[[Category: Steinmetz, M O]]
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[[Category: Sharma A]]
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[[Category: Antitumoural]]
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[[Category: Steinmetz MO]]
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[[Category: Microtubule targeting agent]]
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[[Category: Microtubule]]
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[[Category: Resistance to chemotherapy]]
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[[Category: Structural protein]]
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[[Category: Tubulin]]
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Current revision

Triazolopyrimidines stabilize microtubules by binding to the vinca inhibitor site of tubulin

PDB ID 5njh

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