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A Third Shot at EGFR: New Opportunities in Cancer Therapy.
Trends in Pharmacological Sciences ( IF 13.8 ) Pub Date : 2019-11-06 , DOI: 10.1016/j.tips.2019.10.004
Salvador Guardiola 1 , Monica Varese 1 , Macarena Sánchez-Navarro 1 , Ernest Giralt 2
Affiliation  

Epidermal growth factor receptor (EGFR) inhibitors were among the first type of targeted agents discovered in cancer and currently constitute the standard of care for a wide range of lung and colon malignancies. However, the therapeutic progress achieved with these drugs has been accompanied by the identification of an ever-increasing number of acquired resistance mechanisms that inevitably appear in nearly all patients. Increased knowledge on EGFR biochemistry, cellular crosstalk, and resistance pathways provides an opportunity to establish effective combination therapies and discover novel-acting inhibitors that prevent or overcome therapeutic resistance. One such strategy is the selective blockade of circulating growth factors such as EGF. In this review, we address the uses and limitations of approved EGFR inhibitors and explore the potential of drug combinations and new third avenues to block the activation of the EGFR.

中文翻译:

EGFR的第三枪:癌症治疗的新机会。

表皮生长因子受体(EGFR)抑制剂是在癌症中发现的第一类靶向药物,目前构成广泛的肺和结肠恶性肿瘤的治疗标准。然而,随着这些药物的治疗进展,伴随着越来越多的获得性耐药机制的鉴定,这种耐药机制不可避免地出现在几乎所有患者中。对EGFR生物化学,细胞串扰和抗药性途径的了解增加,为建立有效的联合疗法和发现预防或克服治疗性抗药性的新型抑制剂提供了机会。一种这样的策略是对诸如EGF的循环生长因子的选择性阻断。在这篇评论中,
更新日期:2019-11-07
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