2cn8: Difference between revisions

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[[Image:2cn8.~~jpg~~|left|200px]]

[[Image:2cn8.png|left|200px]]

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~~'''~~CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE~~'''~~

===CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE===

~~==Overview==~~

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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.~~

The line below this paragraph, {{ABSTRACT_PUBMED_16794575}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 16794575 is the PubMed ID number.

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==About this Structure==

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[[Category: Transferase]]

[[Category: Tumour suppressor]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sat May 3 22~~:34:03 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 01:57:09 2008''

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-[[Image:2cn8.jpg|left|200px]]
+{{Seed}}
+[[Image:2cn8.png|left|200px]]
 <!--
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 {{STRUCTURE_2cn8|  PDB=2cn8  |  SCENE=  }}
-'''CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE'''
+===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.
+The line below this paragraph, {{ABSTRACT_PUBMED_16794575}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 16794575 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_16794575}}
 ==About this Structure==
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 [[Category: Transferase]]
 [[Category: Tumour suppressor]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 22:34:03 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 01:57:09 2008''