View source for 2oiq

[[Image:2oiq.gif|left|200px]]

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{{STRUCTURE_2oiq|  PDB=2oiq  |  SCENE=  }} 

'''Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib.'''


==Overview==
The cancer drug imatinib inhibits the tyrosine kinases c-Abl, c-Kit, and the PDGF receptor. Imatinib is less effective against c-Src, which is difficult to understand because residues interacting with imatinib in crystal structures of Abl and c-Kit are conserved in c-Src. The crystal structure of the c-Src kinase domain in complex with imatinib closely resembles that of Abl*imatinib and c-Kit*imatinib, and differs significantly from the inactive "Src/CDK" conformation of the Src family kinases. Attempts to increase the affinity of c-Src for imatinib by swapping residues with the corresponding residues in Abl have not been successful, suggesting that the thermodynamic penalty for adoption of the imatinib-binding conformation by c-Src is distributed over a broad region of the structure. Two mutations that are expected to destabilize the inactive Src/CDK conformation increase drug sensitivity 15-fold, suggesting that the free-energy balance between different inactive states is a key to imatinib binding.

==About this Structure==
2OIQ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OIQ OCA]. 

==Reference==
c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty., Seeliger MA, Nagar B, Frank F, Cao X, Henderson MN, Kuriyan J, Structure. 2007 Mar;15(3):299-311. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17355866 17355866]
[[Category: Gallus gallus]]
[[Category: Non-specific protein-tyrosine kinase]]
[[Category: Single protein]]
[[Category: Cao, X.]]
[[Category: Frank, F.]]
[[Category: Henderson, M N.]]
[[Category: Kuriyan, J.]]
[[Category: Nagar, B.]]
[[Category: Seeliger, M A.]]
[[Category: Src,kinase,imatinib,inactive]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 11:00:12 2008''