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Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy

文献类型：期刊论文

作者Liu, Feifei; Yang, Xiaotong; Geng, Meiyu; Huang, Min
刊名ACTA PHARMACEUTICA SINICA B
出版日期2018-07
卷号8期号:4页码:552-562
关键词Mitogen-activated protein kinases Extracellular signal-regulated kinase ERK inhibitor ERK kinase Cancer therapy Drug resistance
ISSN号2211-3835
DOI10.1016/j.apsb.2018.01.008
文献子类Review
英文摘要The mitogen-activated protein kinases (MAPK) pathway, often known as the RAS-RAF-MEK-ERK signal cascade, functions to transmit upstream signals to its downstream effectors to regulate physiological process such as cell proliferation, differentiation, survival and death. As the most frequently mutated signaling pathway in human cancer, targeting the MAPK pathway has long been considered a promising strategy for cancer therapy. Substantial efforts in the past decades have led to the clinical success of BRAF and MEK inhibitors. However, the clinical benefits of these inhibitors are compromised by the frequently occurring acquired resistance due to cancer heterogeneity and genomic instability. This review briefly introduces the key protein kinases involved in this pathway as well as their activation mechanisms. We also generalize the correlations between mutations of MAPK members and human cancers, followed by a summarization of progress made on the development of small molecule MAPK kinases inhibitors. In particular, this review highlights the potential advantages of ERK inhibitors in overcoming resistance to upstream targets and proposes that targeting ERK kinase may hold a promising prospect for cancer therapy. (C) 2018 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
WOS关键词INHIBITOR-RESISTANT MELANOMA ; RENAL-CELL CARCINOMA ; ACQUIRED-RESISTANCE ; MEK INHIBITORS ; K-RAS ; FEEDBACK PHOSPHORYLATION ; SIGNALING PATHWAY ; PLASMA-MEMBRANE ; GENE-EXPRESSION ; SMALL MOLECULES
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000439807300008
出版者INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
源URL[http://119.78.100.183/handle/2S10ELR8/279676]  
专题药理学第一研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Huang, Min
作者单位Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Feifei,Yang, Xiaotong,Geng, Meiyu,et al. Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy[J]. ACTA PHARMACEUTICA SINICA B,2018,8(4):552-562.
APA Liu, Feifei,Yang, Xiaotong,Geng, Meiyu,&Huang, Min.(2018).Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy.ACTA PHARMACEUTICA SINICA B,8(4),552-562.
MLA Liu, Feifei,et al."Targeting ERK, an Achilles' Heel of the MAPK pathway, in cancer therapy".ACTA PHARMACEUTICA SINICA B 8.4(2018):552-562.

入库方式： OAI收割

来源：上海药物研究所

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