Molecular targeting of growth factor receptor-bound 2 (Grb2) as an anti-cancer strategy

Pathirage G. Dharmawardana, Benedetta Peruzzi, Alessio Giubellino, Terrence R. Burke, Donald P. Bottaro

Research output: Contribution to journalArticlepeer-review

53 Scopus citations

Abstract

Growth factor receptor-bound 2 (Grb2) is a ubiquitously expressed adapter protein that provides a critical link between cell surface growth factor receptors and the Ras signaling pathway. As such, it has been implicated in the oncogenesis of several important human malignancies. In addition to this function, research over the last decade has revealed other fundamental roles for Grb2 in cell motility and angiogenesis - processes that also contribute to tumor growth, invasiveness and metastasis. This functional profile makes Grb2 a high priority target for anti-cancer drug development. Knowledge of Grb2 protein structure, its component Src homology domains and their respective structure-function relationships has facilitated the rapid development of sophisticated drug candidates that can penetrate cells, bind Grb2 with high affinity and potently antagonize Grb2 signaling. These novel compounds offer considerable promise in our growing arsenal of rationally designed anti-cancer therapeutics.

Original languageEnglish (US)
Pages (from-to)13-20
Number of pages8
JournalAnti-Cancer Drugs
Volume17
Issue number1
DOIs
StatePublished - Jan 2006

Keywords

  • Angiogenesis
  • Cancer
  • Cell motility
  • Grb2
  • Growth factor receptor-bound 2
  • Metastasis

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