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

Publication date: Available online 10 May 2017
Source:Best Practice & Research Clinical Endocrinology & Metabolism
Author(s): Valentina De Falco, Francesca Carlomagno, Hong-yu Li, Massimo Santoro
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.



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