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黑色素瘤中的RTK/RAS/BRAF/PI3K信号通路:生物学、小分子抑制剂及潜在应用

The RTK/RAS/BRAF/PI3K pathways in melanoma: biology, small molecule inhibitors, and potential applications.

作者信息

Haluska Frank, Pemberton Trevor, Ibrahim Nageatte, Kalinsky Kevin

机构信息

Molecular Oncology Research Institute, Tufts-New England Medical Center, Boston, MA 02111, USA.

出版信息

Semin Oncol. 2007 Dec;34(6):546-54. doi: 10.1053/j.seminoncol.2007.09.011.

Abstract

The discovery of mutations in the BRAF signaling molecule in a large proportion of cutaneous melanomas immediately suggested the prospect of effective therapies for this disease. The most appealing initial target has been BRAF itself, as most mutations involve a single residue in the kinase domain of the protein. But the identification of the high mutation rate in this signaling intermediate also suggests that other molecules up- and downstream of BRAF might be productively targeted. Indeed, several receptor tyrosine kinases, as well as RAS, are mutated in a small number of melanoma cases. Moreover, genetic alterations in the phosphotidylinositol-3-kinase (PI3K) pathway, especially in PTEN, suggest that this route also poses opportunities for therapeutic exploitation. We will review here the genetic evidence suggesting the utility of targets on these pathways. We will also summarize the recent clinical data that have accumulated from initial trials designed to test BRAF inhibition and targeting of other molecules. Finally, we provide an overview of molecules entering the clinic and soon to be tested in clinical studies, as well as strategies for their employment as monotherapy and in combinations.

摘要

在大部分皮肤黑色素瘤中发现BRAF信号分子的突变,这立刻提示了针对该疾病有效治疗方法的前景。最具吸引力的初始靶点一直是BRAF本身,因为大多数突变涉及该蛋白激酶结构域中的单个残基。但在这个信号中间体中高突变率的发现也表明,BRAF上下游的其他分子可能是有效的靶向目标。事实上,在少数黑色素瘤病例中,几种受体酪氨酸激酶以及RAS发生了突变。此外,磷脂酰肌醇-3-激酶(PI3K)途径的基因改变,尤其是PTEN中的改变,表明该途径也为治疗开发提供了机会。我们将在此回顾提示这些途径上靶点有用性的遗传学证据。我们还将总结从旨在测试BRAF抑制和其他分子靶向治疗的初步试验中积累的最新临床数据。最后,我们概述了即将进入临床并很快将在临床研究中进行测试的分子,以及它们作为单一疗法和联合疗法的应用策略。

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