ErbB receptors: from oncogenes to targeted cancer therapies.
Understanding the genetic origin of cancer at the molecular level has facilitated the development of novel targeted therapies. Aberrant activation of the ErbB family of receptors is implicated in many human cancers and is already the target of several anticancer therapeutics. The use of mAbs specific for the extracellular domain of ErbB receptors was the first implementation of rational targeted therapy. The cytoplasmic tyrosine kinase domain is also a preferred target for small compounds that inhibit the kinase activity of these receptors. However, current therapy has not yet been optimized, allowing for opportunities for optimization of the next generation of targeted therapy, particularly with regards to inhibiting heteromeric ErbB family receptor complexes.
Zhang
Hongtao
H
Department of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104-6082, USA.
Berezov
Alan
A
Wang
Qiang
Q
Zhang
Geng
G
Drebin
Jeffrey
J
Murali
Ramachandran
R
Greene
Mark I
MI
D000818:Animals; D000911:Antibodies, Monoclonal / Q000627:therapeutic use*; D016503:Drug Delivery Systems; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000627:therapeutic use*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology* / Q000235:genetics; D017434:Protein Structure, Tertiary
D000911:Antibodies, Monoclonal; D004791:Enzyme Inhibitors; C512478:EGFR protein, human; D066246:ErbB Receptors