4c52: Difference between revisions
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{{STRUCTURE_4c52| PDB=4c52 | SCENE= }} | |||
===Crystal structure of Bcl-xL in complex with benzoylurea compound (39b)=== | |||
{{ABSTRACT_PUBMED_24456288}} | |||
==Function== | |||
[[http://www.uniprot.org/uniprot/B2CL1_HUMAN B2CL1_HUMAN]] Potent inhibitor of cell death. Inhibits activation of caspases (By similarity). Appears to regulate cell death by blocking the voltage-dependent anion channel (VDAC) by binding to it and preventing the release of the caspase activator, CYC1, from the mitochondrial membrane. Also acts as a regulator of G2 checkpoint and progression to cytokinesis during mitosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> Isoform Bcl-X(S) promotes apoptosis.<ref>PMID:19917720</ref> <ref>PMID:21840391</ref> | |||
==About this Structure== | |||
[[4c52]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4C52 OCA]. | |||
==Reference== | |||
<ref group="xtra">PMID:024456288</ref><references group="xtra"/><references/> | |||
[[Category: Brady, R M.]] | |||
[[Category: Colman, P M.]] | |||
[[Category: Czabotar, P E.]] | |||
[[Category: Lessene, G.]] | |||
[[Category: Roy, M J.]] | |||
[[Category: Apoptosis]] | |||
Revision as of 14:15, 5 February 2014
Crystal structure of Bcl-xL in complex with benzoylurea compound (39b)Crystal structure of Bcl-xL in complex with benzoylurea compound (39b)
Template:ABSTRACT PUBMED 24456288
FunctionFunction
[B2CL1_HUMAN] Potent inhibitor of cell death. Inhibits activation of caspases (By similarity). Appears to regulate cell death by blocking the voltage-dependent anion channel (VDAC) by binding to it and preventing the release of the caspase activator, CYC1, from the mitochondrial membrane. Also acts as a regulator of G2 checkpoint and progression to cytokinesis during mitosis.[1] [2] Isoform Bcl-X(S) promotes apoptosis.[3] [4]
About this StructureAbout this Structure
4c52 is a 2 chain structure. Full crystallographic information is available from OCA.
ReferenceReference
- ↑ Brady RM, Vom A, Roy MJ, Toovey N, Smith BJ, Moss RM, Hazis E, Huang DC, Parisot JP, Yang H, Street IP, Colman PM, Czabotar PE, Baell JB, Lessene G. De-Novo Designed Library of Benzoylureas as Inhibitors of BCL-XL: Synthesis, Structural and Biochemical Characterization. J Med Chem. 2014 Jan 23. PMID:24456288 doi:http://dx.doi.org/10.1021/jm401948b
- ↑ Terrano DT, Upreti M, Chambers TC. Cyclin-dependent kinase 1-mediated Bcl-xL/Bcl-2 phosphorylation acts as a functional link coupling mitotic arrest and apoptosis. Mol Cell Biol. 2010 Feb;30(3):640-56. doi: 10.1128/MCB.00882-09. Epub 2009 Nov, 16. PMID:19917720 doi:10.1128/MCB.00882-09
- ↑ Wang J, Beauchemin M, Bertrand R. Bcl-xL phosphorylation at Ser49 by polo kinase 3 during cell cycle progression and checkpoints. Cell Signal. 2011 Dec;23(12):2030-8. doi: 10.1016/j.cellsig.2011.07.017. Epub, 2011 Aug 5. PMID:21840391 doi:10.1016/j.cellsig.2011.07.017
- ↑ Terrano DT, Upreti M, Chambers TC. Cyclin-dependent kinase 1-mediated Bcl-xL/Bcl-2 phosphorylation acts as a functional link coupling mitotic arrest and apoptosis. Mol Cell Biol. 2010 Feb;30(3):640-56. doi: 10.1128/MCB.00882-09. Epub 2009 Nov, 16. PMID:19917720 doi:10.1128/MCB.00882-09
- ↑ Wang J, Beauchemin M, Bertrand R. Bcl-xL phosphorylation at Ser49 by polo kinase 3 during cell cycle progression and checkpoints. Cell Signal. 2011 Dec;23(12):2030-8. doi: 10.1016/j.cellsig.2011.07.017. Epub, 2011 Aug 5. PMID:21840391 doi:10.1016/j.cellsig.2011.07.017