充分利用MEK：葡萄膜黑色素瘤中共同靶向Gαq和丝裂原活化蛋白激酶的策略
MEK-ing the Most of It: Strategies to Co-target Gαq and MAPK in Uveal Melanoma.
作者信息
Neelature Sriramareddy Sathya, Smalley Keiran S M
机构信息
Department of Tumor Biology, The Moffitt Cancer Center & Research Institute, Tampa, Florida.
Department of Cutaneous Oncology, The Moffitt Cancer Center & Research Institute, Tampa, Florida.
出版信息
Clin Cancer Res. 2021 Mar 1;27(5):1217-1219. doi: 10.1158/1078-0432.CCR-20-4530. Epub 2020 Dec 22.
Abstract
Most uveal melanomas harbor mutations in Gαq and show constitutive MAPK activation. Although MEK inhibition has some efficacy against uveal melanoma, clinical responses are typically poor. The Gαq inhibitor-MEK inhibitor combination showed prolonged suppression of MAPK signaling in preclinical uveal melanoma models and led to improved therapeutic responses..
摘要
大多数葡萄膜黑色素瘤存在Gαq基因突变，并表现出组成型丝裂原活化蛋白激酶（MAPK）激活。尽管MEK抑制对葡萄膜黑色素瘤有一定疗效，但临床反应通常较差。在临床前葡萄膜黑色素瘤模型中，Gαq抑制剂与MEK抑制剂联合使用可延长对MAPK信号传导的抑制作用，并改善治疗反应。
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