Receptor tyrosine kinases as targets for anticancer therapeutics.
Oncogenic conversion of receptor protein tyrosine kinases (RTK) is a frequent feature of malignant cells. This knowledge has fostered efforts to develop target-specific low molecular weight therapeutics able to obstruct RTK signalling. The clinical efficacy of the ABL- and KIT-inhibitors are paradigmatic of the power of this approach. Here, we focus on small-molecule inhibitors for RTKs involved in human cancer. In particular, we examine the KIT, MET and RET receptors that are targeted by genetic alterations in both sporadic and familial human tumours.
Carlomagno
Francesca
F
Istituto di Endocrinologia ed Oncologia Sperimentale del CNR/Dipartimento di Biologia e Patologia Cellulare e Molecolare, Universita' di Napoli Federico II, via S. Pansini 5, 80131 Napoli, Italy.
Santoro
Massimo
M
D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D020794:Receptor Protein-Tyrosine Kinases / Q000187:drug effects*
D000970:Antineoplastic Agents; D020794:Receptor Protein-Tyrosine Kinases