Current Medicinal Chemistry

Author(s): S. Sartini, B. Dario, M. Morelli, F. Da Settimo and C. La Motta

DOI: 10.2174/092986711796150504

Receptor Tyrosine Kinase Kit and Gastrointestinal Stromal Tumours: An Overview

Page: [2893 - 2903] Pages: 11

  • * (Excluding Mailing and Handling)

Abstract

Kit is a growth factor receptor of the type III tyrosine kinase family, whose gain-of-function mutations have been identified as driving causes of different kinds of tumours. It thus represents a viable drug target, and the development of Kit inhibitors has been shown to be a promising therapeutic concept.

This review will focus on structural and signalling properties of both wild-type and mutant Kit, as well as its role in the development of human cancers. Special attention will be dedicated to gastrointestinal stromal tumours, GISTs. Progress in research on the aetiopathogenesis of GISTs and their therapeutic approaches will be fully discussed, focusing on the latest tendencies for the treatment of these kinds of tumours.

Keywords: GISTs, Kit, tyrosine kinase inhibitors