1m17

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{{STRUCTURE_1m17| PDB=1m17 | SCENE= }}
{{STRUCTURE_1m17| PDB=1m17 | SCENE= }}
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'''Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib'''
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===Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 12196540 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12196540}}
==About this Structure==
==About this Structure==
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[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Tyrosine kinase domain]]
[[Category: Tyrosine kinase domain]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:30:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 22:59:26 2008''

Revision as of 19:59, 2 July 2008

Image:1m17.png

Template:STRUCTURE 1m17

Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib

Template:ABSTRACT PUBMED 12196540

About this Structure

1M17 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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 Wed Jul 2 22:59:26 2008

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