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

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

doi:10.1016/j.beem.2017.04.013

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

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

Pharmacology and Toxicology

Research output: Contribution to journal › Review article › peer-review

29 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 language	English (US)
Pages (from-to)	307-318
Number of pages	12
Journal	Best Practice and Research: Clinical Endocrinology and Metabolism
Volume	31
Issue number	3
DOIs	https://doi.org/10.1016/j.beem.2017.04.013
State	Published - 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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10.1016/j.beem.2017.04.013

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title = "The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer",

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",

author = "{De Falco}, Valentina and Francesca Carlomagno and Li, {Hong yu} and Massimo Santoro",

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AU - De Falco, Valentina

AU - Carlomagno, Francesca

AU - Li, Hong yu

AU - Santoro, Massimo

PY - 2017/6

Y1 - 2017/6

N2 - 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.

AB - 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.

KW - MEN

KW - RET

KW - TKI

KW - targeted therapy

KW - thyroid cancer

KW - tyrosine kinase

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SN - 1521-690X

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ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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