RET酪氨酸激酶抑制剂在甲状腺癌中的分子基础。
The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer.
作者信息
De Falco Valentina, Carlomagno Francesca, Li Hong-Yu, Santoro Massimo
机构信息
Istituto di Endocrinologia e Oncologia Sperimentale, CNR, Via S Pansini 5, 80131 Naples, Italy.
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.
出版信息
Best Pract Res Clin Endocrinol Metab. 2017 Jun;31(3):307-318. doi: 10.1016/j.beem.2017.04.013. Epub 2017 May 10.
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.
摘要
RET受体酪氨酸激酶在多种人类恶性肿瘤中作为一种突变的致癌驱动因子发挥作用，并且在其他癌症中过度表达。具有RET酪氨酸激酶抑制活性的小分子化合物正在被研究用于这些恶性肿瘤的靶向治疗。RET抑制浓度在纳摩尔范围内的多靶点化合物已进入临床应用。本综述总结了RET致癌活性的机制以及在临床前阶段已显示出有前景的抗RET活性的新化合物的特性。
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