2oiq

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[[Image:2oiq.gif|left|200px]]
[[Image:2oiq.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2oiq |SIZE=350|CAPTION= <scene name='initialview01'>2oiq</scene>, resolution 2.07&Aring;
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The line below this paragraph, containing "STRUCTURE_2oiq", creates the "Structure Box" on the page.
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|SITE=
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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=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=STI:4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE'>STI</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_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= SRC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9031 Gallus gallus])
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|DOMAIN=
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{{STRUCTURE_2oiq| PDB=2oiq | 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=2oiq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oiq OCA], [http://www.ebi.ac.uk/pdbsum/2oiq PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oiq RCSB]</span>
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}}
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'''Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib.'''
'''Crystal Structure of chicken c-Src kinase domain in complex with the cancer drug imatinib.'''
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[[Category: Nagar, B.]]
[[Category: Nagar, B.]]
[[Category: Seeliger, M A.]]
[[Category: Seeliger, M A.]]
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[[Category: src,kinase,imatinib,inactive]]
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[[Category: Src,kinase,imatinib,inactive]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:00:12 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:18:27 2008''
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Revision as of 08:00, 4 May 2008

Image:2oiq.gif

Template:STRUCTURE 2oiq

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 Gallus gallus. Full crystallographic information is available from 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:17355866 Page seeded by OCA on Sun May 4 11:00:12 2008

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