1yy8
From Proteopedia
| Line 7: | Line 7: | ||
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1yy9|1YY9]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yy8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yy8 OCA], [http://www.ebi.ac.uk/pdbsum/1yy8 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yy8 RCSB]</span> | ||
}} | }} | ||
| Line 28: | Line 31: | ||
[[Category: Schmitz, K R.]] | [[Category: Schmitz, K R.]] | ||
[[Category: Wiltzius, J J.W.]] | [[Category: Wiltzius, J J.W.]] | ||
| - | [[Category: | + | [[Category: antibody drug]] |
| + | [[Category: cancer]] | ||
| + | [[Category: fab fragment]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:26:21 2008'' |
Revision as of 22:26, 30 March 2008
| |||||||
| , resolution 2.00Å | |||||||
|---|---|---|---|---|---|---|---|
| Related: | 1YY9
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal structure of the Fab fragment from the monoclonal antibody cetuximab/Erbitux/IMC-C225
Overview
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.
About this Structure
1YY8 is a Protein complex structure of sequences from 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 Mon Mar 31 01:26:21 2008
