title: An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors.
abstract: Recent crystallographic studies have provided significant new insight into how receptor tyrosine kinases from the EGF receptor or ErbB family are regulated by their growth factor ligands. EGF receptor dimerization is mediated by a unique dimerization arm, which becomes exposed only after a dramatic domain rearrangement is promoted by growth factor binding. ErbB2, a family member that has no ligand, has its dimerization arm constitutively exposed, and this explains several of its unique properties. We outline a mechanistic view of ErbB receptor homo- and heterodimerization, which suggests new approaches for interfering with these processes when they are implicated in human cancers.
authors.affiliation: Cooperative Research Centre for Cellular Growth Factors, P.O. Box 2008, Royal Melbourne Hospital, Parkville, Victoria 3050, Australia.
authors.forename: Antony W
authors.initials: AW
authors.lastname: Burgess
authors.forename: Hyun-Soo
authors.initials: HS
authors.lastname: Cho
authors.forename: Charles
authors.initials: C
authors.lastname: Eigenbrot
authors.forename: Kathryn M
authors.initials: KM
authors.lastname: Ferguson
authors.forename: Thomas P J
authors.initials: TP
authors.lastname: Garrett
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Leahy
authors.forename: Mark A
authors.initials: MA
authors.lastname: Lemmon
authors.forename: Mark X
authors.initials: MX
authors.lastname: Sliwkowski
authors.forename: Colin W
authors.initials: CW
authors.lastname: Ward
authors.forename: Shigeyuki
authors.initials: S
authors.lastname: Yokoyama
mesh_terms: D000818:Animals; D002471:Cell Transformation, Neoplastic / Q000378:metabolism; D066246:ErbB Receptors / Q000378:metabolism*; D005057:Eukaryotic Cells / Q000378:metabolism*; D006133:Growth Substances / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D008968:Molecular Conformation; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D018739:Oncogene Proteins v-erbB / Q000378:metabolism*; D017434:Protein Structure, Tertiary
chemical_list: D006133:Growth Substances; D008024:Ligands; D018739:Oncogene Proteins v-erbB; D066246:ErbB Receptors