title: Receptor tyrosine kinase kit and gastrointestinal stromal tumours: an overview.
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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126, Pisa, Italy.
authors.forename: S
authors.initials: S
authors.lastname: Sartini
authors.forename: B
authors.initials: B
authors.lastname: Dario
authors.forename: M
authors.initials: M
authors.lastname: Morelli
authors.forename: F
authors.initials: F
authors.lastname: Da Settimo
authors.forename: C
authors.initials: C
authors.lastname: La Motta
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D046152:Gastrointestinal Stromal Tumors / Q000188:drug therapy* / Q000201:enzymology* / Q000235:genetics; D041981:Gastrointestinal Tract / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D009154:Mutation / Q000187:drug effects; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D019009:Proto-Oncogene Proteins c-kit / Q000737:chemistry / Q000235:genetics* / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D019009:Proto-Oncogene Proteins c-kit