The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer

Valentina De Falco, Francesca Carlomagno, Hong yu Li, Massimo Santoro

Research output: Contribution to journalReview article

8 Scopus citations

Abstract

RET receptor tyrosine kinase acts as a mutated oncogenic driver in several human malignancies and it is over-expressed in other cancers. Small molecule compounds with RET tyrosine kinase inhibitory activity are being investigated for the targeted treatment of these malignancies. Multi-targeted compounds with RET inhibitory concentration in the nanomolar range have entered clinical practice. This review summarizes mechanisms of RET oncogenic activity and properties of new compounds that, at the preclinical stage, have demonstrated promising anti-RET activity.

Original languageEnglish (US)
Pages (from-to)307-318
Number of pages12
JournalBest Practice and Research: Clinical Endocrinology and Metabolism
Volume31
Issue number3
DOIs
StatePublished - Jun 2017

Keywords

  • MEN
  • RET
  • TKI
  • targeted therapy
  • thyroid cancer
  • tyrosine kinase

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Endocrinology

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