MEK and the inhibitors: from bench to bedside.
MEK and the inhibitors: from bench to bedside.
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DOI：
10.1186/1756-8722-6-27
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发表时间：
2013-04-12
影响因子：
28.5
通讯作者：
Liu D
中科院分区：
文献类型：
--
作者：
Akinleye A;Furqan M;Mukhi N;Ravella P;Liu D
目前已鉴定出涉及7个MEK酶的4条不同的MAPK信号通路。MEK1和MEK2是MEK家族蛋白的原型成员。几种MEK抑制剂正在进行临床试验。曲美替尼正在接受FDA的评估，用于治疗带有BRAF V600突变的转移性黑色素瘤。赛鲁米替尼与多西紫杉醇联合用于先前治疗的晚期肺癌患者的II期随机试验中进行了研究。赛鲁米替尼组的有效率和无进展生存率较好。本文还综述了临床上应用的新的甲硫氨酸酪氨酸激酶抑制剂，包括匹马司替布、瑞法美替尼、PD-0325901、TAK733、MEK162(ARRY 438162)、RO5126766、WX-554、RO4987655(CH4987655)、GDC0973(XL518)和AZD8330。
Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members of MEK family proteins. Several MEK inhibitors are in clinical trials. Trametinib is being evaluated by FDA for the treatment of metastatic melanoma with BRAF V600 mutation. Selumetinib has been studied in combination with docetaxel in phase II randomized trial in previously treated patients with advanced lung cancer. Selumetinib group had better response rate and progression-free survival. This review also summarized new MEK inhibitors in clinical development, including pimasertib, refametinib, PD-0325901, TAK733, MEK162 (ARRY 438162), RO5126766, WX-554, RO4987655 (CH4987655), GDC-0973 (XL518), and AZD8330.
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