1yy9

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[[Image:1yy9.gif|left|200px]]
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{{STRUCTURE_1yy9| PDB=1yy9 | SCENE= }}
{{STRUCTURE_1yy9| PDB=1yy9 | SCENE= }}
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'''Structure of the extracellular domain of the epidermal growth factor receptor in complex with the Fab fragment of cetuximab/Erbitux/IMC-C225'''
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===Structure of the extracellular domain of the epidermal growth factor receptor in complex with the Fab fragment of cetuximab/Erbitux/IMC-C225===
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==Overview==
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Recent structural studies of epidermal growth factor receptor (EGFR) family extracellular regions have identified an unexpected mechanism for ligand-induced receptor dimerization that has important implications for activation and inhibition of these receptors. Here we describe the 2.8 angstroms resolution X-ray crystal structure of the antigen binding (Fab) fragment from cetuximab (Erbitux), an inhibitory anti-EGFR antibody, in complex with the soluble extracellular region of EGFR (sEGFR). The sEGFR is in the characteristic "autoinhibited" or "tethered" inactive configuration. Cetuximab interacts exclusively with domain III of sEGFR, partially occluding the ligand binding region on this domain and sterically preventing the receptor from adopting the extended conformation required for dimerization. We suggest that both these effects contribute to potent inhibition of EGFR activation.
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The line below this paragraph, {{ABSTRACT_PUBMED_15837620}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15837620 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15837620}}
==Disease==
==Disease==
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[[Category: Glycoprotein]]
[[Category: Glycoprotein]]
[[Category: Tyrosine kinase]]
[[Category: Tyrosine kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:57:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 23:39:42 2008''

Revision as of 20:39, 27 July 2008

Image:1yy9.png

Template:STRUCTURE 1yy9

Contents

Structure of the extracellular domain of the epidermal growth factor receptor in complex with the Fab fragment of cetuximab/Erbitux/IMC-C225

Template:ABSTRACT PUBMED 15837620

Disease

Known disease associated with this structure: Adenocarcinoma of lung, response to tyrosine kinase inhibitor in OMIM:[131550], Nonsmall cell lung cancer, response to tyrosine kinase inhibitor in OMIM:[131550], Nonsmall cell lung cancer, susceptibility to OMIM:[131550]

About this Structure

1YY9 is a Single protein structure of sequence from Homo sapiens and Mus musculus/homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural basis for inhibition of the epidermal growth factor receptor by cetuximab., Li S, Schmitz KR, Jeffrey PD, Wiltzius JJ, Kussie P, Ferguson KM, Cancer Cell. 2005 Apr;7(4):301-11. PMID:15837620

Page seeded by OCA on Sun Jul 27 23:39:42 2008

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