2. Academic Validation
  3. The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer

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

  • Best Pract Res Clin Endocrinol Metab. 2017 Jun;31(3):307-318. doi: 10.1016/j.beem.2017.04.013.
Valentina De Falco 1,  Francesca Carlomagno 2,  Hong-Yu Li 3,  Massimo Santoro 4
Affiliations

Affiliations

  • 1 Istituto di Endocrinologia e Oncologia Sperimentale, CNR, Via S Pansini 5, 80131 Naples, Italy. Electronic address: vdefalco@unina.it.
  • 2 Istituto di Endocrinologia e Oncologia Sperimentale, CNR, Via S Pansini 5, 80131 Naples, Italy; Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università Federico II, Via S Pansini 5, 80131 Naples, Italy. Electronic address: francesca.carlomagno@unina.it.
  • 3 University of Arkansas for Medical Sciences, College of Pharmacy, Division of Pharmaceutical Science, 200 South Cedar, Little Rock AR 72202, USA. Electronic address: HLi2@uams.edu.
  • 4 Istituto di Endocrinologia e Oncologia Sperimentale, CNR, Via S Pansini 5, 80131 Naples, Italy; Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Università Federico II, Via S Pansini 5, 80131 Naples, Italy. Electronic address: masantor@unina.it.
PMID: 28911727 DOI: 10.1016/j.beem.2017.04.013
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.

Keywords

MEN; RET; TKI; targeted therapy; thyroid cancer; tyrosine kinase.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-164482
    RET Inhibitor
    RET