基于ERα的双抑制剂:对于内分泌抵抗性乳腺癌的新型治疗方法
Shuangshuang Xiong1, Ke Song2, Hua Xiang1
1Jiangsu Key Laboratory of Drug Design and Optimization, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
European journal of medicinal chemistry
|April 8, 2024
概括
针对雌激素受体α (ERα) 的向疗法对乳腺癌 (BC) 至关重要,但耐药性很常见. 本综述探讨了新型双向抑制剂,将ERα对抗性与其他抗癌策略结合起来,以克服耐药性.
科学领域:
- 在瘤学瘤学.
- 药用化学 医学化学
- 分子生物学分子生物学
背景情况:
- 雌激素受体α (ERα) 是超过70%的乳腺癌 (BCs) 的关键标.
- 向ERα的内分泌疗法 (SERM,SERD) 是基础的,但在高达30%的患者中面临新出现的耐药性.
- 抵抗的机制涉及异常的信号通路,突出显示了对组合策略的需要.
研究的目的:
- 审查ERα与其他抗癌标之间的协同相互作用.
- 从药物化学的角度来看,总结最近基于ERα的双重向抑制剂的进展.
- 为ERα阳性BC治疗提供未来药物发现的前景.
主要方法:
- 文献综述专注于药物化学和药物发现.
- 对双重向抑制剂的合理设计策略的分析.
- 检查结构-活动关系 (SARs) 和生物活动.
主要成果:
- 确定了ERα与其他致癌信号通路之间的显著交叉.
- 强调了基于ERα的新型双重向剂的开发.
- 剖析了这些抑制剂的设计原理,SAR和有效性.
结论:
- 双向抑制剂为克服ERα阳性乳腺癌内分泌抵抗提供了一个有希望的策略.
- 对合理设计和SAR的进一步研究对于开发有效的组合疗法至关重要.
- 基于ERα的双重向药物发现有可能改善BC治疗结果.
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