2cn5
From Proteopedia
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| - | [[Image:2cn5.gif|left|200px]]<br /><applet load="2cn5" size=" | + | [[Image:2cn5.gif|left|200px]]<br /><applet load="2cn5" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2cn5, resolution 2.25Å" /> | caption="2cn5, resolution 2.25Å" /> | ||
'''CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH ADP'''<br /> | '''CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH ADP'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2CN5 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CL, MG, NO3 and ADP as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Known structural/functional Site: <scene name='pdbsite=AC1:Adp Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | + | 2CN5 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CL:'>CL</scene>, <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=NO3:'>NO3</scene> and <scene name='pdbligand=ADP:'>ADP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Known structural/functional Site: <scene name='pdbsite=AC1:Adp+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2CN5 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: tumour suppressor]] | [[Category: tumour suppressor]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:37:10 2008'' |
Revision as of 08:37, 3 February 2008
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CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH ADP
Contents |
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.
Disease
Known diseases associated with this structure: Breast and colorectal cancer, susceptibility to OMIM:[604373], Breast cancer, susceptibility to OMIM:[604373], Li-Fraumeni syndrome OMIM:[604373], Osteosarcoma, somatic OMIM:[604373], Prostate cancer, familial OMIM:[604373]
About this Structure
2CN5 is a Single protein structure of sequence from Homo sapiens with , , and as ligands. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Known structural/functional Site: . 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
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Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Oliver, A.W. | Pearl, L.H. | ADP | CL | MG | NO3 | Activation segment | Alternative splicing | Atp-binding | Cancer | Cds1 | Cell cycle | Checkpoint | Chek2 | Chk2 | Disease mutation | Kinase | Kinase domain | Li-fraumeni syndrome | Magnesium | Metal-binding | Nuclear protein | Nucleotide-binding | Phosphorylation | Proto-oncogene | Rad53 | Serine/threonine-protein kinase | Transferase | Tumour suppressor
