1m14: Difference between revisions
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{{STRUCTURE_1m14| PDB=1m14 | SCENE= }} | |||
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'''Tyrosine Kinase Domain from Epidermal Growth Factor Receptor''' | '''Tyrosine Kinase Domain from Epidermal Growth Factor Receptor''' | ||
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[[Category: Sliwkowski, M X.]] | [[Category: Sliwkowski, M X.]] | ||
[[Category: Stamos, J.]] | [[Category: Stamos, J.]] | ||
[[Category: | [[Category: Transferase]] | ||
[[Category: | [[Category: Tyrosine kinase domain]] | ||
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Revision as of 00:30, 3 May 2008
Tyrosine Kinase Domain from Epidermal Growth Factor Receptor
OverviewOverview
The crystal structure of the kinase domain from the epidermal growth factor receptor (EGFRK) including forty amino acids from the carboxyl-terminal tail has been determined to 2.6-A resolution, both with and without an EGFRK-specific inhibitor currently in Phase III clinical trials as an anti-cancer agent, erlotinib (OSI-774, CP-358,774, Tarceva(TM)). The EGFR family members are distinguished from all other known receptor tyrosine kinases in possessing constitutive kinase activity without a phosphorylation event within their kinase domains. Despite its lack of phosphorylation, we find that the EGFRK activation loop adopts a conformation similar to that of the phosphorylated active form of the kinase domain from the insulin receptor. Surprisingly, key residues of a putative dimerization motif lying between the EGFRK domain and carboxyl-terminal substrate docking sites are found in close contact with the kinase domain. Significant intermolecular contacts involving the carboxyl-terminal tail are discussed with respect to receptor oligomerization.
About this StructureAbout this Structure
1M14 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor., Stamos J, Sliwkowski MX, Eigenbrot C, J Biol Chem. 2002 Nov 29;277(48):46265-72. Epub 2002 Aug 23. PMID:12196540 Page seeded by OCA on Sat May 3 00:30:17 2008