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2w3l

From Proteopedia

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{{Seed}}
 
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[[Image:2w3l.png|left|200px]]
 
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==Crystal Structure of Chimaeric Bcl2-xL and Phenyl Tetrahydroisoquinoline Amide Complex==
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The line below this paragraph, containing "STRUCTURE_2w3l", creates the "Structure Box" on the page.
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<StructureSection load='2w3l' size='340' side='right'caption='[[2w3l]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2w3l]] 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=2W3L OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2W3L FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DRO:1-(2-{[(3S)-3-(AMINOMETHYL)-3,4-DIHYDROISOQUINOLIN-2(1H)-YL]CARBONYL}PHENYL)-4-CHLORO-5-METHYL-N,N-DIPHENYL-1H-PYRAZOLE-3-CARBOXAMIDE'>DRO</scene></td></tr>
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{{STRUCTURE_2w3l| PDB=2w3l | SCENE= }}
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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=2w3l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2w3l OCA], [https://pdbe.org/2w3l PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2w3l RCSB], [https://www.ebi.ac.uk/pdbsum/2w3l PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2w3l ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN] Note=A chromosomal aberration involving BCL2 has been found in chronic lymphatic leukemia. Translocation t(14;18)(q32;q21) with immunoglobulin gene regions. BCL2 mutations found in non-Hodgkin lymphomas carrying the chromosomal translocation could be attributed to the Ig somatic hypermutation mechanism resulting in nucleotide transitions.
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== Function ==
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[https://www.uniprot.org/uniprot/BCL2_HUMAN BCL2_HUMAN] Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating factor (APAF-1).<ref>PMID:18570871</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/w3/2w3l_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</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=2w3l ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Anti-apoptotic Bcl-2 protects cells from apoptosis by binding to pro-apoptotic members of the Bcl-2 family thereby playing a role in tumour survival in response to chemo- or radiation therapy. We describe a series of phenyl pyrazoles that have high affinity for Bcl-2 and rationalise the observed SAR by means of an X-ray crystal structure.
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===CRYSTAL STRUCTURE OF CHIMAERIC BCL2-XL AND PHENYL TETRAHYDROISOQUINOLINE AMIDE COMPLEX===
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Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors.,Porter J, Payne A, de Candole B, Ford D, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Whitcombe I, Davis J, Stubberfield C Bioorg Med Chem Lett. 2008 Oct 31. PMID:19027294<ref>PMID:19027294</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 2w3l" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_19027294}}, adds the Publication Abstract to the page
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*[[B-cell lymphoma proteins 3D structures|B-cell lymphoma proteins 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 19027294 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_19027294}}
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__TOC__
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</StructureSection>
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==About this Structure==
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2W3L 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=2W3L OCA].
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==Reference==
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Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors., Porter J, Payne A, de Candole B, Ford D, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Whitcombe I, Davis J, Stubberfield C, Bioorg Med Chem Lett. 2008 Oct 31. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/19027294 19027294]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Candole, B De.]]
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[[Category: Large Structures]]
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[[Category: Davis, J.]]
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[[Category: Davis J]]
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[[Category: Edwards, C.]]
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[[Category: Edwards C]]
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[[Category: Fisher, M.]]
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[[Category: Fisher M]]
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[[Category: Ford, D.]]
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[[Category: Ford D]]
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[[Category: Hutchinson, B.]]
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[[Category: Hutchinson B]]
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[[Category: Lamers, M.]]
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[[Category: Lamers M]]
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[[Category: Payne, A.]]
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[[Category: Payne A]]
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[[Category: Porter, J.]]
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[[Category: Porter J]]
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[[Category: Stubberfield, C.]]
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[[Category: Stubberfield C]]
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[[Category: Trevitt, G.]]
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[[Category: Trevitt G]]
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[[Category: Turner, J.]]
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[[Category: Turner J]]
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[[Category: Watkins, C.]]
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[[Category: Watkins C]]
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[[Category: Whitcombe, I.]]
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[[Category: Whitcombe I]]
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[[Category: Apoptosis]]
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[[Category: De Candole B]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Dec 24 11:08:46 2008''
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Current revision

Crystal Structure of Chimaeric Bcl2-xL and Phenyl Tetrahydroisoquinoline Amide Complex

PDB ID 2w3l

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