4aq3

From Proteopedia

(Difference between revisions)

Revision as of 07:52, 4 August 2016

HUMAN BCL-2 WITH PHENYLACYLSULFONAMIDE INHIBITOR

Structural highlights

4aq3 is a 6 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Related:	1bxl, 1g5j, 1g5m, 1gjh, 1lxl, 1maz, 1r2d, 1r2e, 1r2g, 1r2h, 1r2i, 1ysg, 1ysi, 1ysn, 1ysw, 2b48, 2w3l, 2xa0, 2yj1, 4a1u, 4a1w
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Disease

[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

[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).^[1]

Publication Abstract from PubMed

A series of phenylacylsulfonamides has been prepared as antagonists of Bcl-2/Bcl-xL. In addition to potent binding affinities for both Bcl-2 and Bcl-xL, these compounds were shown to induce classical markers of apoptosis in isolated mitochondria. Overall weak cellular potency was improved by the incorporation of polar functionality resulting in compounds with moderate antiproliferative activity.

Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.,Perez HL, Banfi P, Bertrand J, Cai ZW, Grebinski JW, Kim K, Lippy J, Modugno M, Naglich J, Schmidt RJ, Tebben A, Vianello P, Wei DD, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM Bioorg Med Chem Lett. 2012 Jun 15;22(12):3946-50. Epub 2012 May 2. PMID:22608961^[2]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Wei Y, Pattingre S, Sinha S, Bassik M, Levine B. JNK1-mediated phosphorylation of Bcl-2 regulates starvation-induced autophagy. Mol Cell. 2008 Jun 20;30(6):678-88. doi: 10.1016/j.molcel.2008.06.001. PMID:18570871 doi:10.1016/j.molcel.2008.06.001
↑ Perez HL, Banfi P, Bertrand J, Cai ZW, Grebinski JW, Kim K, Lippy J, Modugno M, Naglich J, Schmidt RJ, Tebben A, Vianello P, Wei DD, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM. Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3946-50. Epub 2012 May 2. PMID:22608961 doi:10.1016/j.bmcl.2012.04.103

1 Structural highlights
2 Disease
3 Function
4 Publication Abstract from PubMed
5 See Also
6 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4aq3"

@@ Line 1: / Line 1: @@
 ==HUMAN BCL-2 WITH PHENYLACYLSULFONAMIDE INHIBITOR==
 <StructureSection load='4aq3' size='340' side='right' caption='[[4aq3]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[4aq3]] is a 6 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=4AQ3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AQ3 FirstGlance]. <br>
+<table><tr><td colspan='2'>[[4aq3]] is a 6 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=4AQ3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AQ3 FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=398:N,N-DIBUTYL-4-CHLORANYL-1-[2-(3,4-DIHYDRO-1H-ISOQUINOLIN-2-YLCARBONYL)-4-[(7-IODANYLNAPHTHALEN-2-YL)SULFONYLCARBAMOYL]PHENYL]-5-METHYL-PYRAZOLE-3-CARBOXAMIDE'>398</scene></td></tr>
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1bxl|1bxl]], [[1g5j|1g5j]], [[1g5m|1g5m]], [[1gjh|1gjh]], [[1lxl|1lxl]], [[1maz|1maz]], [[1r2d|1r2d]], [[1r2e|1r2e]], [[1r2g|1r2g]], [[1r2h|1r2h]], [[1r2i|1r2i]], [[1ysg|1ysg]], [[1ysi|1ysi]], [[1ysn|1ysn]], [[1ysw|1ysw]], [[2b48|2b48]], [[2w3l|2w3l]], [[2xa0|2xa0]], [[2yj1|2yj1]], [[4a1u|4a1u]], [[4a1w|4a1w]]</td></tr>
-<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=4aq3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4aq3 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4aq3 RCSB], [http://www.ebi.ac.uk/pdbsum/4aq3 PDBsum]</span></td></tr>
+<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=4aq3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4aq3 OCA], [http://pdbe.org/4aq3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4aq3 RCSB], [http://www.ebi.ac.uk/pdbsum/4aq3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4aq3 ProSAT]</span></td></tr>
 </table>
 == Disease ==
@@ Line 19: / Line 20: @@
 From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 </div>
+<div class="pdbe-citations 4aq3" style="background-color:#fffaf0;"></div>
 ==See Also==
@@ Line 26: / Line 28: @@
 __TOC__
 </StructureSection>
-[[Category: Homo sapiens]]
+[[Category: Human]]
 [[Category: Bertrand, J A]]
 [[Category: Fasolini, M]]

4aq3

From Proteopedia

Revision as of 07:52, 4 August 2016

HUMAN BCL-2 WITH PHENYLACYLSULFONAMIDE INHIBITOR

Structural highlights

Disease

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

Personal tools

Navigation

Search

Toolbox