3r92: Difference between revisions
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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.== | |||
<StructureSection load='3r92' size='340' side='right'caption='[[3r92]], [[Resolution|resolution]] 1.58Å' scene=''> | |||
== Structural highlights == | |||
<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> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.5801Å</td></tr> | |||
<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> | |||
== | <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> | ||
[[3r92]] is a 1 chain structure | </table> | ||
== Function == | |||
[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== | ||
*[[Heat Shock | *[[Heat Shock Protein structures|Heat Shock Protein structures]] | ||
== References == | |||
== | <references/> | ||
< | __TOC__ | ||
</StructureSection> | |||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Bloom | [[Category: Large Structures]] | ||
[[Category: Boschelli | [[Category: Bloom JD]] | ||
[[Category: Dushin | [[Category: Boschelli F]] | ||
[[Category: Golas | [[Category: Dushin RG]] | ||
[[Category: Levin | [[Category: Golas JM]] | ||
[[Category: Liu | [[Category: Levin JI]] | ||
[[Category: Lucas | [[Category: Liu H]] | ||
[[Category: McBean | [[Category: Lucas J]] | ||
[[Category: Vogan | [[Category: McBean JL]] | ||
[[Category: Zapf | [[Category: Vogan EM]] | ||
[[Category: Zapf CW]] | |||
Latest revision as of 10:53, 21 February 2024
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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