Moon Aree
College of Pharmacy, Duksung Women's University, Seoul, South Korea.
Adv Exp Med Biol. 2021;1187:81-101. doi: 10.1007/978-981-32-9620-6_4.
Ras proteins mediate extracellular and cytoplasmic signaling networks via receptor tyrosine kinase. The Ras pathway induces activation of signaling molecules involved in cell proliferation and growth, cell survival and apoptosis, metabolism, and motility. Although Ras mutations in breast cancer are not frequently reported, hyperactivation of Ras signaling plays an important role in breast cancer growth and progression. Oncogenic Ras activation occurs via loss of Ras GTPase-activating proteins, overexpression of growth factor receptor, and stimulation by various cytokines. Effective control of oncogenic Ras is one of the therapeutic strategies in breast cancer. The mechanisms of intracellular localization, activation, and signaling pathway of Ras in cancer have been used to develop therapeutic candidates. Recent studies have reported an effective therapy for breast cancer by inhibition of enzymes involved in the posttranslational modification of Ras, such as farnesyltransferase and geranylgeranyltransferase 1, and anti-cancer therapies targeting the epidermal growth factor receptor (EGFR). Emerging targets involved in EGF-mediated Ras activity in breast cancer have shed new insight into Ras activation in breast cancer progression. These alternative mechanisms for Ras signaling pathway may suggest novel therapeutic approaches for targeting Ras in breast cancer. In spite of the difficulties in targeting Ras protein, important discoveries highlight the direct inhibition of Ras activity. Further studies may elucidate the effects of targeting Ras protein and the clinical relevance thereof.
Ras蛋白通过受体酪氨酸激酶介导细胞外和细胞质信号网络。Ras途径诱导参与细胞增殖与生长、细胞存活与凋亡、代谢及运动的信号分子活化。尽管乳腺癌中Ras突变的报道并不常见,但Ras信号的过度激活在乳腺癌的生长和进展中起重要作用。致癌性Ras激活通过Ras GTP酶激活蛋白的缺失、生长因子受体的过表达以及各种细胞因子的刺激而发生。有效控制致癌性Ras是乳腺癌的治疗策略之一。Ras在癌症中的细胞内定位、激活及信号通路机制已被用于开发治疗候选物。最近的研究报道了通过抑制参与Ras翻译后修饰的酶(如法尼基转移酶和香叶基香叶基转移酶1)以及靶向表皮生长因子受体(EGFR)的抗癌疗法对乳腺癌进行有效治疗。乳腺癌中涉及表皮生长因子(EGF)介导的Ras活性的新靶点为乳腺癌进展中的Ras激活提供了新的见解。Ras信号通路的这些替代机制可能提示针对乳腺癌中Ras的新型治疗方法。尽管靶向Ras蛋白存在困难,但重要发现突出了对Ras活性的直接抑制。进一步的研究可能阐明靶向Ras蛋白的作用及其临床相关性。