蛋白质与蛋白质相互作用的自然产品调节剂:综合性审查
Emadeldin M Kamel1, Ahmed A Allam2, Hassan A Rudayni2
1Chemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef, Egypt.
Phytochemical analysis : PCA
|February 12, 2026
概括
天然产品有效调节蛋白与蛋白相互作用 (PPI),为癌症等疾病提供各种治疗途径. 本综述详细介绍了针对关键PPI的天然化合物,突出了它们在药物开发中的潜力.
科学领域:
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
- 自然产品 化学 化学
背景情况:
- 天然产品提供多样化的小分子来调节蛋白质与蛋白质相互作用 (PPI).
- 这些分子可以破坏致病性复合体或稳定有益的复合体,扩大治疗策略超越酶抑制.
研究的目的:
- 合成和审查蛋白质与蛋白质相互作用 (PPI) 的天然产品调节剂.
- 强调目标覆盖范围,行动机制,效力,结构证据和功能结果.
主要方法:
- 精心策划的自然产品作为直接或间接的PPI调节器的已发表示例.
- 按功能性PPI类别 (致癌性,信号性,伴侣性,免疫性) 和机械性类别 (例如,竞争性封锁,基调制,共振性修饰,分子) 的有组织化合物.
- 总结了代表性支架,结合亲缘关系 (IC50/Ki) 和结构数据.
主要成果:
- 天然产品表现出多种PPI控制模式,针对关键蛋白质.
- 这些例子包括破坏MDM2-p53的chlorofusin,抑制BCL-xL的 (-) -gossypol,向Hsp90-Cdc37的celasstrol,以及调节免疫蛋白PI的环素A/FK506/拉巴胺素.
- 报告的强度范围从微分子到纳米分子的亲和力.
结论:
- 天然产品调节器证明了蛋白质与蛋白质相互作用 (PPI) 的药用性.
- 这些化合物作为有价值的化学探针和用于治疗开发的支架.
- 潜在的应用范围包括癌症,神经退行,传染病和免疫系统疾病.
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