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3qtf

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[[Image:3qtf.png|left|200px]]
 
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{{STRUCTURE_3qtf| PDB=3qtf | SCENE= }}
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==Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity==
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<StructureSection load='3qtf' size='340' side='right'caption='[[3qtf]], [[Resolution|resolution]] 1.57&Aring;' scene=''>
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===Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity===
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3qtf]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QTF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QTF FirstGlance]. <br>
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{{ABSTRACT_PUBMED_21420297}}
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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]] 1.5703&#8491;</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=05S:(6S)-6,15,15,18-TETRAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-8,12-(METHENO)[1,4,9]TRIAZACYCLOTETRADECINO[9,8-A]INDOLE-9-CARBOXAMIDE'>05S</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene></td></tr>
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==About this Structure==
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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=3qtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qtf OCA], [https://pdbe.org/3qtf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qtf RCSB], [https://www.ebi.ac.uk/pdbsum/3qtf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qtf ProSAT]</span></td></tr>
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[[3qtf]] is a 1 chain structure of [[Heat Shock Proteins]] with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QTF OCA].
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/HS90A_HUMAN HS90A_HUMAN] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.<ref>PMID:15937123</ref> <ref>PMID:11274138</ref>
==See Also==
==See Also==
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*[[Heat Shock Proteins|Heat Shock Proteins]]
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*[[Heat Shock Protein structures|Heat Shock Protein structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:021420297</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Bloom, J D.]]
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[[Category: Large Structures]]
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[[Category: Boschelli, F.]]
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[[Category: Bloom JD]]
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[[Category: Dushin, R G.]]
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[[Category: Boschelli F]]
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[[Category: Eid, C N.]]
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[[Category: Dushin RG]]
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[[Category: Golas, J.]]
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[[Category: Eid CN]]
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[[Category: Hu, Y.]]
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[[Category: Golas J]]
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[[Category: Ingalls, C.]]
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[[Category: Hu Y]]
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[[Category: Levin, J I.]]
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[[Category: Ingalls C]]
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[[Category: Liu, H.]]
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[[Category: Levin JI]]
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[[Category: McBean, J L.]]
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[[Category: Liu H]]
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[[Category: Nittoli, T.]]
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[[Category: McBean JL]]
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[[Category: Sonye, J P.]]
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[[Category: Nittoli T]]
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[[Category: Sutherland, A G.]]
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[[Category: Sonye JP]]
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[[Category: Vogan, E M.]]
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[[Category: Sutherland AG]]
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[[Category: Zapf, C W.]]
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[[Category: Vogan EM]]
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[[Category: Atp binding domain]]
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[[Category: Zapf CW]]
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[[Category: Atp-binding]]
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[[Category: Chaperone]]
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[[Category: Chaperone-chaperone inhibitor complex]]
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[[Category: Nucleotide-binding]]
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[[Category: Phosphoprotein]]
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[[Category: Stress response]]
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Current revision

Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity

PDB ID 3qtf

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