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3fzk

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==Crystal Structures of Hsc70/Bag1 in Complex with Small Molecule Inhibitors==
==Crystal Structures of Hsc70/Bag1 in Complex with Small Molecule Inhibitors==
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<StructureSection load='3fzk' size='340' side='right' caption='[[3fzk]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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<StructureSection load='3fzk' size='340' side='right'caption='[[3fzk]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3fzk]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FZK OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3FZK FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3fzk]] is a 2 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=3FZK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FZK 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=3BK:(2R,3R,4S,5R)-2-[6-AMINO-8-[(3,4-DICHLOROPHENYL)METHYLAMINO]PURIN-9-YL]-5-(HYDROXYMETHYL)OXOLANE-3,4-DIOL'>3BK</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=TRS:2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL'>TRS</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]] 2.1&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3fzf|3fzf]], [[3fzh|3fzh]], [[3fzl|3fzl]], [[3fzm|3fzm]]</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=3BK:(2R,3R,4S,5R)-2-[6-AMINO-8-[(3,4-DICHLOROPHENYL)METHYLAMINO]PURIN-9-YL]-5-(HYDROXYMETHYL)OXOLANE-3,4-DIOL'>3BK</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=TRS:2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL'>TRS</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">HSPA8, HSC70, HSP73, HSPA10 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), BAG1, HAP ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3fzk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fzk OCA], [https://pdbe.org/3fzk PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3fzk RCSB], [https://www.ebi.ac.uk/pdbsum/3fzk PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3fzk ProSAT]</span></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=3fzk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fzk OCA], [http://pdbe.org/3fzk PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3fzk RCSB], [http://www.ebi.ac.uk/pdbsum/3fzk PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3fzk ProSAT]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/HSP7C_HUMAN HSP7C_HUMAN]] Acts as a repressor of transcriptional activation. Inhibits the transcriptional coactivator activity of CITED1 on Smad-mediated transcription. Chaperone. Component of the PRP19-CDC5L complex that forms an integral part of the spliceosome and is required for activating pre-mRNA splicing. May have a scaffolding role in the spliceosome assembly as it contacts all other components of the core complex.<ref>PMID:10722728</ref> [[http://www.uniprot.org/uniprot/BAG1_HUMAN BAG1_HUMAN]] Inhibits the chaperone activity of HSP70/HSC70 by promoting substrate release. Inhibits the pro-apoptotic function of PPP1R15A, and has anti-apoptotic activity. Markedly increases the anti-cell death function of BCL2 induced by various stimuli.<ref>PMID:9305631</ref> <ref>PMID:9873016</ref> <ref>PMID:12724406</ref>
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[https://www.uniprot.org/uniprot/HSP7C_HUMAN HSP7C_HUMAN] Acts as a repressor of transcriptional activation. Inhibits the transcriptional coactivator activity of CITED1 on Smad-mediated transcription. Chaperone. Component of the PRP19-CDC5L complex that forms an integral part of the spliceosome and is required for activating pre-mRNA splicing. May have a scaffolding role in the spliceosome assembly as it contacts all other components of the core complex.<ref>PMID:10722728</ref>
== Evolutionary Conservation ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]
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==See Also==
==See Also==
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*[[BAG protein|BAG protein]]
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*[[BAG family proteins 3D structures|BAG family proteins 3D structures]]
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*[[Heat Shock Proteins|Heat Shock Proteins]]
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*[[Heat Shock Protein structures|Heat Shock Protein structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
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[[Category: Dokurno, P]]
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[[Category: Large Structures]]
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[[Category: Murray, J B]]
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[[Category: Dokurno P]]
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[[Category: Surgenor, A E]]
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[[Category: Murray JB]]
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[[Category: Williamson, D S]]
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[[Category: Surgenor AE]]
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[[Category: Adenosine]]
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[[Category: Williamson DS]]
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[[Category: Apoptosis]]
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[[Category: Atp-binding]]
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[[Category: Bag1]]
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[[Category: Chaperone]]
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[[Category: Heat shock]]
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[[Category: Hsc70]]
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[[Category: Hsp70]]
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[[Category: Nucleotide]]
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[[Category: Nucleotide exchange factor]]
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[[Category: Nucleotide-binding]]
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[[Category: Protein folding]]
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[[Category: Small molecule inhibitor]]
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[[Category: Stress response]]
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Current revision

Crystal Structures of Hsc70/Bag1 in Complex with Small Molecule Inhibitors

PDB ID 3fzk

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