Cancer Molecular Pathology Group, Griffith Health Institute, Griffith University, Gold Coast, Australia.
Cancer Molecular Pathology Group, Griffith Health Institute, Griffith University, Gold Coast, Australia.
Crit Rev Oncol Hematol. 2014 Jun;90(3):220-32. doi: 10.1016/j.critrevonc.2013.12.008. Epub 2013 Dec 16.
BRAF is one of the most commonly mutated proto-oncogenes and plays a significant role in the development of numerous cancers of high clinical impact. Due to the commonality of BRAF mutations, a number of BRAF inhibitors have been developed as tools in the management of patients with cancers dependent on the action of mutant BRAF to drive cellular proliferation. In this review, we examine the current state of clinical trials and laboratory research concerning BRAF inhibitors in development and available for clinical use. We contrast the effectiveness of type-I and type-II BRAF inhibitors, the former typically showing much more restricted inhibitory selectivity and greater patient response rates.
BRAF 是最常见的突变原癌基因之一，在许多具有重大临床影响的癌症的发生发展中发挥着重要作用。由于 BRAF 突变的普遍性，许多 BRAF 抑制剂已被开发为治疗依赖突变 BRAF 驱动细胞增殖的癌症患者的工具。在这篇综述中，我们研究了目前正在进行的临床试验和实验室研究，涉及正在开发和可用于临床使用的 BRAF 抑制剂。我们对比了 I 型和 II 型 BRAF 抑制剂的有效性，前者通常显示出更严格的抑制选择性和更高的患者反应率。
