Knudsen Beatrice S, Vande Woude George
Division of Public Health Sciences, Fred Hutchinson Cancer Research Center, 1100 Fairview Avenue, Seattle, WA 98109, United States.
Curr Opin Genet Dev. 2008 Feb;18(1):87-96. doi: 10.1016/j.gde.2008.02.001. Epub 2008 Apr 9.
The receptor tyrosine kinase, c-MET and its ligand hepatocyte growth factor/scatter factor (HGF/SF) have become leading candidates for targeted cancer therapies. Inappropriate c-MET signaling through autocrine, paracrine, amplification, and mutational activation occurs in virtually all types of solid tumors (http://www.vai.org/met), contributing to one or a combination of proliferative, invasive, survival, or angiogenic cancer phenotypes. c-MET and HGF/SF participate in all stages of malignant progression and represent promising drug targets in a variety of cancer types, including carcinomas, sarcomas, and brain tumors. While many are in pre-clinical testing, a few inhibitors have entered clinical trials. With hundreds of thousands of potential responding cancers that express c-MET, the interest in this molecule as a drug target is not surprising. However, the cognate c-MET diagnostic tests lag behind. In addition, despite the great enthusiasm based on response rates in phase I trials, there is a need for caution. It is almost without question that combination therapies with c-MET-HGF/SF inhibitors will be required for most cancers to achieve a cytotoxic tumor response.
受体酪氨酸激酶c-MET及其配体肝细胞生长因子/分散因子(HGF/SF)已成为靶向癌症治疗的主要候选对象。在几乎所有类型的实体瘤中(http://www.vai.org/met),都会通过自分泌、旁分泌、扩增和突变激活发生不适当的c-MET信号传导,导致增殖、侵袭、存活或血管生成性癌症表型中的一种或多种。c-MET和HGF/SF参与恶性进展的所有阶段,在包括癌、肉瘤和脑肿瘤在内的多种癌症类型中均代表有前景的药物靶点。虽然许多药物正处于临床前测试阶段,但已有少数抑制剂进入了临床试验。鉴于有数十万潜在的表达c-MET的应答性癌症,将该分子作为药物靶点受到关注也就不足为奇了。然而,相关的c-MET诊断测试却滞后了。此外,尽管基于I期试验的缓解率人们热情高涨,但仍需谨慎。几乎毫无疑问,大多数癌症需要使用c-MET-HGF/SF抑制剂联合疗法才能实现细胞毒性肿瘤应答。