2w3l

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (10:07, 9 May 2024) (edit) (undo)
 
(7 intermediate revisions not shown.)
Line 1: Line 1:
-
{{STRUCTURE_2w3l| PDB=2w3l | SCENE= }}
 
-
===CRYSTAL STRUCTURE OF CHIMAERIC BCL2-XL AND PHENYL TETRAHYDROISOQUINOLINE AMIDE COMPLEX===
 
-
{{ABSTRACT_PUBMED_19027294}}
 
-
==Disease==
+
==Crystal Structure of Chimaeric Bcl2-xL and Phenyl Tetrahydroisoquinoline Amide Complex==
-
[[http://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.
+
<StructureSection load='2w3l' size='340' side='right'caption='[[2w3l]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
 +
== Structural highlights ==
 +
<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>
 +
</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=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>
 +
<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>
 +
</table>
 +
== Disease ==
 +
[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.
 +
== Function ==
 +
[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>
 +
== 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/w3/2w3l_consurf.spt"</scriptWhenChecked>
 +
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.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=2w3l ConSurf].
 +
<div style="clear:both"></div>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
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.
-
==Function==
+
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>
-
[[http://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>
+
-
==About this Structure==
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-
[[2w3l]] is a 2 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=2W3L OCA].
+
</div>
 +
<div class="pdbe-citations 2w3l" style="background-color:#fffaf0;"></div>
==See Also==
==See Also==
-
*[[Bcl-2|Bcl-2]]
+
*[[B-cell lymphoma proteins 3D structures|B-cell lymphoma proteins 3D structures]]
-
 
+
== References ==
-
==Reference==
+
<references/>
-
<ref group="xtra">PMID:019027294</ref><references group="xtra"/><references/>
+
__TOC__
 +
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
-
[[Category: Candole, B De.]]
+
[[Category: Large Structures]]
-
[[Category: Davis, J.]]
+
[[Category: Davis J]]
-
[[Category: Edwards, C.]]
+
[[Category: Edwards C]]
-
[[Category: Fisher, M.]]
+
[[Category: Fisher M]]
-
[[Category: Ford, D.]]
+
[[Category: Ford D]]
-
[[Category: Hutchinson, B.]]
+
[[Category: Hutchinson B]]
-
[[Category: Lamers, M.]]
+
[[Category: Lamers M]]
-
[[Category: Payne, A.]]
+
[[Category: Payne A]]
-
[[Category: Porter, J.]]
+
[[Category: Porter J]]
-
[[Category: Stubberfield, C.]]
+
[[Category: Stubberfield C]]
-
[[Category: Trevitt, G.]]
+
[[Category: Trevitt G]]
-
[[Category: Turner, J.]]
+
[[Category: Turner J]]
-
[[Category: Watkins, C.]]
+
[[Category: Watkins C]]
-
[[Category: Whitcombe, I.]]
+
[[Category: Whitcombe I]]
-
[[Category: Apoptosis]]
+
[[Category: De Candole B]]

Current revision

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

PDB ID 2w3l

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2w3l"
Personal tools