2cn8: Difference between revisions
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:2cn8. | [[Image:2cn8.jpg|left|200px]]<br /><applet load="2cn8" size="450" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2cn8" size="450" color="white" frame="true" align="right" spinBox="true" | |||
caption="2cn8, resolution 2.70Å" /> | caption="2cn8, resolution 2.70Å" /> | ||
'''CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE'''<br /> | '''CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE'''<br /> | ||
| Line 11: | Line 10: | ||
==About this Structure== | ==About this Structure== | ||
2CN8 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 MG, NO3 and DBQ 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] | 2CN8 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 MG, NO3 and DBQ 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:Dbq Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2CN8 OCA]. | ||
==Reference== | ==Reference== | ||
| Line 41: | Line 40: | ||
[[Category: tumour suppressor]] | [[Category: tumour suppressor]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Dec 18 19:29:53 2007'' | ||
Revision as of 20:20, 18 December 2007
|
CRYSTAL STRUCTURE OF HUMAN CHK2 IN COMPLEX WITH DEBROMOHYMENIALDISINE
OverviewOverview
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.
DiseaseDisease
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 StructureAbout this Structure
2CN8 is a Single protein structure of sequence from Homo sapiens with MG, NO3 and DBQ 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.
ReferenceReference
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 Tue Dec 18 19:29:53 2007
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Homo sapiens
- Non-specific serine/threonine protein kinase
- Single protein
- Oliver, A.W.
- Pearl, L.H.
- DBQ
- MG
- NO3
- Activation segment
- Atp-binding
- Cancer
- Cds1
- Checkpoint
- Chek2
- Chk2
- Hypothetical protein
- Kinase
- Kinase domain
- Li-fraumeni syndrome
- Nucleotide-binding
- Phosphorylation
- Rad53
- Serine/threonine-protein kinase
- Transferase
- Tumour suppressor