A role for the pseudokinase HER3 in the acquired resistance against EGFR- and HER2-directed targeted therapy
A role for the pseudokinase HER3 in the acquired resistance against EGFR- and HER2-directed targeted therapy
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DOI：
10.1042/bst20140043
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发表时间：
2014-08-01
影响因子：
3.9
通讯作者：
Parker, Peter J.
中科院分区：
文献类型：
--
作者：
Claus, Jeroen;Patel, Gargi;Parker, Peter J.
特异性抑制EGFR（表皮生长因子受体）家族成员，特别是EGFR和HER2（人表皮生长因子受体2），是许多人类癌症的重要治疗策略。与传统的化疗相比，这些靶向治疗具有很强的特异性和最初的有效性，但对这些靶向治疗的获得性耐药是一个反复出现的威胁。最近越来越多的研究表明，EGFR家族中的假激酶HER3及其配体NRG（神经调节蛋白流感）在耐药癌症模型和患者中都很重要。在本文中，我们描述了HER3介导获得性耐药的一些作用，并讨论了目前在癌症中靶向HER3本身的努力。
Specific inhibition of members of the EGFR (epidermal growth factor receptor) family, particularly EGFR and HER2 (human epidermal growth factor receptor 2), are an important therapeutic strategy in many human cancers. Compared with classical chemotherapy, these targeted therapeutics are very specific and initially effective, but acquired resistance against these targeted therapies is a recurring threat. A growing body of recent work has highlighted a pseudokinase in the EGFR family, HER3, and its ligand, NRG (neuregulin flu), to be of importance in models of resistant cancers, as well as in patients. In the present article, we describe some of the roles in which HER3 can mediate acquired resistance and discuss the current efforts to target HER3 itself in cancer.