摘要
C-Met是一种具有二转膜的受体络氨酸激酶,又以作为肝细胞生长因子受体(HGFR)的表面受体而广为人知。c-Met涉及了许多信号通路的激活,大部分c-Met都与侵略性肿瘤表型有关。在各种各样的人体恶性肿瘤中,c-Met/HGF信号发射被发现存在异常,在许多实例中,c-Met/HGF信号发射与晚期疾病分型和不良预后有关。因此,c-Met被确定为化学癌症疗法的一个新兴的和有趣的靶点。这篇综述简要的总结了c-Met的信号通路,讨论了典型c-Met的晶体结构和配体结合模式。这篇文章还提出了从2014年至今最新的c-Met抑制剂的设计、合成和构效关系分析。最后,我们总结了临床发展中的c-Met抑制剂,并提出了展望。
关键词: c-Met抑制剂,肝细胞生长因子受体(HGFR),ATP-竞争性抑制剂,抗癌药物,构效关系分析,结合模式
Current Medicinal Chemistry
Title:Recent Advances in the Design and Synthesis of c-Met Inhibitors as Anticancer Agents (2014-Present)
Volume: 24 Issue: 1
Author(s): Peng-Cheng Lv, Zhong-Chang Wang, Hai-Liang Zhu.
Affiliation:
关键词: c-Met抑制剂,肝细胞生长因子受体(HGFR),ATP-竞争性抑制剂,抗癌药物,构效关系分析,结合模式
摘要: c-Met, also known as the surface receptor of hepatocyte growth factor receptor (HGFR), is a receptor tyrosine kinase with heterodimer transmembrane. c-Met involves in the activation of several signaling pathways, most of them are implicated in aggressive cancer phenotypes. In a variety of human malignances, c-Met/HGF signaling has been found aberrant, and in many instances, has been correlated with advanced disease stage and poor prognosis. Thus, the c-Met has identified as an emerging and interesting target for cancer chemotherapy. In this review, we briefly summarize signaling pathways of c-Met, and discuss the crystal structures of representative c-Met and the binding modes with their ligands. We also present updates on the design, synthesis and structure-activity relationship analysis of c-Met inhibitors developed from 2014 till now. At last, we review the c-Met inhibitors that are in clinical development and highlight the future prospects.
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Cite this article as:
Peng-Cheng Lv, Zhong-Chang Wang, Hai-Liang Zhu. , Recent Advances in the Design and Synthesis of c-Met Inhibitors as Anticancer Agents (2014-Present), Current Medicinal Chemistry 2017; 24 (1) . https://dx.doi.org/10.2174/0929867323666161028161441
DOI https://dx.doi.org/10.2174/0929867323666161028161441 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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