3fzk: Difference between revisions

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-{{Seed}}
-[[Image:3fzk.png|left|200px]]
-<!--
+==Crystal Structures of Hsc70/Bag1 in Complex with Small Molecule Inhibitors==
-The line below this paragraph, containing "STRUCTURE_3fzk", creates the "Structure Box" on the page.
+<StructureSection load='3fzk' size='340' side='right'caption='[[3fzk]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
-You may change the PDB parameter (which sets the PDB file loaded into the applet)
+== Structural highlights ==
-or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
+<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>
-or leave the SCENE parameter empty for the default display.
+</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>
--->
+<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>
-{{STRUCTURE_3fzk|  PDB=3fzk  |  SCENE=  }}
+<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>
+</table>
+== Function ==
+[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 ==
+[[Image:Consurf_key_small.gif|200px|right]]
+Check<jmol>
+  <jmolCheckbox>
+    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fz/3fzk_consurf.spt"</scriptWhenChecked>
+    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
+    <text>to colour the structure by Evolutionary Conservation</text>
+  </jmolCheckbox>
+</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3fzk ConSurf].
+<div style="clear:both"></div>
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+The design and synthesis of novel adenosine-derived inhibitors of HSP70, guided by modeling and X-ray crystallographic structures of these compounds in complex with HSC70/BAG-1, is described. Examples exhibited submicromolar affinity for HSP70, were highly selective over HSP90, and some displayed potency against HCT116 cells. Exposure of compound 12 to HCT116 cells caused significant reduction in cellular levels of Raf-1 and Her2 at concentrations similar to that which caused cell growth arrest.
-===Crystal Structures of Hsc70/Bag1 in Complex with Small Molecule Inhibitors===
+Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.,Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ J Med Chem. 2009 Mar 26;52(6):1510-3. PMID:19256508<ref>PMID:19256508</ref>
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+</div>
+<div class="pdbe-citations 3fzk" style="background-color:#fffaf0;"></div>
-<!--
+==See Also==
-The line below this paragraph, {{ABSTRACT_PUBMED_19256508}}, adds the Publication Abstract to the page
+*[[BAG family proteins 3D structures|BAG family proteins 3D structures]]
-(as it appears on PubMed at http://www.pubmed.gov), where 19256508 is the PubMed ID number.
+*[[Heat Shock Protein structures|Heat Shock Protein structures]]
--->
+== References ==
-{{ABSTRACT_PUBMED_19256508}}
+<references/>
+__TOC__
-==About this Structure==
+</StructureSection>
-FZK is a 2 chains structure of sequences 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=3FZK OCA].
-==Reference==
-<ref group="xtra">PMID:19256508</ref><references group="xtra"/>
 [[Category: Homo sapiens]]
-[[Category: Dokurno, P.]]
+[[Category: Large Structures]]
-[[Category: Murray, J B.]]
+[[Category: Dokurno P]]
-[[Category: Surgenor, A E.]]
+[[Category: Murray JB]]
-[[Category: Williamson, D S.]]
+[[Category: Surgenor AE]]
-[[Category: Adenosine]]
+[[Category: Williamson DS]]
-[[Category: Apoptosis]]
-[[Category: Atp-binding]]
-[[Category: Bag1]]
-[[Category: Chaperone]]
-[[Category: Heat shock]]
-[[Category: Hsc70]]
-[[Category: Hsp70]]
-[[Category: Nucleotide]]
-[[Category: Nucleotide exchange factor]]
-[[Category: Nucleotide-binding]]
-[[Category: Protein folding]]
-[[Category: Small molecule inhibitor]]
-[[Category: Stress response]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Apr  2 16:23:31 2009''