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ErbB receptors: from oncogenes to targeted cancer therapies
Hongtao Zhang, … , Ramachandran Murali, Mark I. Greene
Hongtao Zhang, … , Ramachandran Murali, Mark I. Greene
Published August 1, 2007
Citation Information: J Clin Invest. 2007;117(8):2051-2058. https://doi.org/10.1172/JCI32278.
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Review

ErbB receptors: from oncogenes to targeted cancer therapies

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Abstract

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.

Authors

Hongtao Zhang, Alan Berezov, Qiang Wang, Geng Zhang, Jeffrey Drebin, Ramachandran Murali, Mark I. Greene

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Figure 1

ErbB receptors and their ligands.

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ErbB receptors and their ligands.
All four members of the ErbB receptor ...
All four members of the ErbB receptor family share high homology in the extracellular domain and the kinase domain. However, ErbB3 is not kinase active. So far no ligand has been found for p185her2/neu, which has been found to be the preferred dimerization partner for other receptors. Only a few examples of receptor dimers are shown here. Ectodomain-truncated receptors also exist in some cancer cells. NRG1, neuregulin 1.

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ISSN: 0021-9738 (print), 1558-8238 (online)

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