Kamath Shantaram, Buolamwini John K
Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, USA.
Med Res Rev. 2006 Sep;26(5):569-94. doi: 10.1002/med.20070.
Conventional anticancer therapy using cytotoxic drugs lacks selectivity and is prone to toxicity and drug resistance. Anticancer therapies targeting aberrant growth factor receptor signaling are gaining interest. The erbB receptor family belongs to the type I, the receptor tyrosine kinases class, and comprises EGFR, HER-2, HER-3, and HER-4. It has been targeted for solid tumor therapy, including breast, ovarian, colon, head-and-neck, and non-small-cell lung cancers. This review summarizes structural aspects of this class of growth factor receptors, their oncogenic expression, and various pharmacological interventions including biological products and small molecules that inhibit these enzymes. We have also discussed various mutations that occur in EGFR and their consequences on anticancer therapy.
使用细胞毒性药物的传统抗癌疗法缺乏选择性，且易产生毒性和耐药性。针对异常生长因子受体信号传导的抗癌疗法正受到关注。erbB受体家族属于I型受体酪氨酸激酶类，包括表皮生长因子受体（EGFR）、人表皮生长因子受体2（HER-2）、人表皮生长因子受体3（HER-3）和人表皮生长因子受体4（HER-4）。它已成为实体瘤治疗的靶点，包括乳腺癌、卵巢癌、结肠癌、头颈癌和非小细胞肺癌。本综述总结了这类生长因子受体的结构特征、致癌表达以及包括生物制品和抑制这些酶的小分子在内的各种药理干预措施。我们还讨论了表皮生长因子受体中发生的各种突变及其对抗癌治疗的影响。
