3r92

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[[Image:3r92.png|left|200px]]
 
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{{STRUCTURE_3r92| PDB=3r92 | SCENE= }}
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==Discovery of a macrocyclic o-aminobenzamide Hsp90 inhibitor with heterocyclic tether that shows extended biomarker activity and in vivo efficacy in a mouse xenograft model.==
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<StructureSection load='3r92' size='340' side='right'caption='[[3r92]], [[Resolution|resolution]] 1.58&Aring;' scene=''>
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===Discovery of a macrocyclic o-aminobenzamide Hsp90 inhibitor with heterocyclic tether that shows extended biomarker activity and in vivo efficacy in a mouse xenograft model.===
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3r92]] 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=3R92 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3R92 FirstGlance]. <br>
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{{ABSTRACT_PUBMED_21605975}}
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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]] 1.5801&#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=06J:(3AR)-13,13,16-TRIMETHYL-15-OXO-1,2,3,3A,4,5,12,14,15,17,18,19-DODECAHYDRO-13H-10,6-(METHENO)PYRROLO[2,1 3,4][1,4,9]TRIAZACYCLOTETRADECINO[9,8-A]INDOLE-7-CARBOXAMIDE'>06J</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=3r92 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3r92 OCA], [https://pdbe.org/3r92 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3r92 RCSB], [https://www.ebi.ac.uk/pdbsum/3r92 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3r92 ProSAT]</span></td></tr>
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[[3r92]] is a 1 chain structure 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=3R92 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:021605975</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: Golas, J M.]]
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[[Category: Dushin RG]]
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[[Category: Levin, J I.]]
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[[Category: Golas JM]]
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[[Category: Liu, H.]]
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[[Category: Levin JI]]
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[[Category: Lucas, J.]]
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[[Category: Liu H]]
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[[Category: McBean, J L.]]
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[[Category: Lucas J]]
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[[Category: Vogan, E M.]]
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[[Category: McBean JL]]
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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

Discovery of a macrocyclic o-aminobenzamide Hsp90 inhibitor with heterocyclic tether that shows extended biomarker activity and in vivo efficacy in a mouse xenograft model.

PDB ID 3r92

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