迈向 RAF 抑制剂耐药性的统一模型。
Towards a unified model of RAF inhibitor resistance.
机构信息
1Department of Medicine, 2Human Oncology and Pathogenesis Program, and 3Program in Molecular Pharmacology, Memorial Sloan-Kettering Cancer Center, New York, New York.
出版信息
Cancer Discov. 2014 Jan;4(1):27-30. doi: 10.1158/2159-8290.CD-13-0961.
Abstract
ATP-competitive RAF inhibitors elicit profound but often temporary antitumor responses in patients with BRAF-mutant melanoma. Analysis of tumor samples collected at the time of disease progression indicates that alterations within the extracellular signal-regulated kinase (ERK) pathway that result in reactivation of ERK signaling are present in most patients. Mutations in the phosphoinositide 3-kinase/AKT pathway that enhance the adaptive response to RAF inhibitors also contribute to RAF inhibitor resistance in a subset of patients.
摘要
三磷酸腺苷（ATP）竞争型 RAF 抑制剂在 BRAF 突变型黑色素瘤患者中引发显著但往往是短暂的抗肿瘤反应。对疾病进展时采集的肿瘤样本的分析表明，大多数患者存在导致 ERK 信号重新激活的细胞外信号调节激酶（ERK）通路改变。磷酸肌醇 3-激酶/AKT 通路中的突变增强了对 RAF 抑制剂的适应性反应，也导致了一部分患者对 RAF 抑制剂产生耐药性。
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