2cn8

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[[Image:2cn8.jpg|left|200px]]
[[Image:2cn8.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2cn8 |SIZE=350|CAPTION= <scene name='initialview01'>2cn8</scene>, resolution 2.70&Aring;
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The line below this paragraph, containing "STRUCTURE_2cn8", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Dbq+Binding+Site+For+Chain+A'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=DBQ:DEBROMOHYMENIALDISINE'>DBQ</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=NO3:NITRATE+ION'>NO3</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2cn8| PDB=2cn8 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2cn8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2cn8 OCA], [http://www.ebi.ac.uk/pdbsum/2cn8 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2cn8 RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE'''
'''CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE'''
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[[Category: Oliver, A W.]]
[[Category: Oliver, A W.]]
[[Category: Pearl, L H.]]
[[Category: Pearl, L H.]]
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[[Category: activation segment]]
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[[Category: Activation segment]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: cancer]]
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[[Category: Cancer]]
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[[Category: cds1]]
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[[Category: Cds1]]
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[[Category: checkpoint]]
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[[Category: Checkpoint]]
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[[Category: chek2]]
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[[Category: Chek2]]
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[[Category: chk2]]
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[[Category: Chk2]]
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[[Category: hypothetical protein]]
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[[Category: Hypothetical protein]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: kinase domain]]
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[[Category: Kinase domain]]
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[[Category: li-fraumeni syndrome]]
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[[Category: Li-fraumeni syndrome]]
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[[Category: nucleotide-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: rad53]]
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[[Category: Rad53]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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[[Category: tumour suppressor]]
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[[Category: Tumour suppressor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 22:34:03 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:23:54 2008''
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Revision as of 19:34, 3 May 2008

Image:2cn8.jpg

Template:STRUCTURE 2cn8

CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE


Overview

The protein kinase Chk2 (checkpoint kinase 2) is a major effector of the replication checkpoint. Chk2 activation is initiated by phosphorylation of Thr68, in the serine-glutamine/threonine-glutamine cluster domain (SCD), by ATM. The phosphorylated SCD-segment binds to the FHA domain of a second Chk2 molecule, promoting dimerisation of the protein and triggering phosphorylation of the activation segment/T-loop in the kinase domain. We have now determined the structure of the kinase domain of human Chk2 in complexes with ADP and a small-molecule inhibitor debromohymenialdisine. The structure reveals a remarkable dimeric arrangement in which T-loops are exchanged between protomers, to form an active kinase conformation in trans. Biochemical data suggest that this dimer is the biologically active state promoted by ATM-phosphorylation, and also suggests a mechanism for dimerisation-driven activation of Chk2 by trans-phosphorylation.

About this Structure

2CN8 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Trans-activation of the DNA-damage signalling protein kinase Chk2 by T-loop exchange., Oliver AW, Paul A, Boxall KJ, Barrie SE, Aherne GW, Garrett MD, Mittnacht S, Pearl LH, EMBO J. 2006 Jul 12;25(13):3179-90. Epub 2006 Jun 22. PMID:16794575 Page seeded by OCA on Sat May 3 22:34:03 2008

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