固醇调节元件结合蛋白抑制剂的研究进展

Recearch progress on sterol regulatory element-binding proteins inhibitors

固醇调节元件结合蛋白(SREBP)是脂类合成的重要调节转录因子,基本参与了脂肪酸和胆固醇的全部合成过程,调控多种脂质合成关键酶的基因表达。SREBP抑制剂通过抑制SREBP的合成、剪切、转运等过程来抑制其活性,从而降低脂质合成水平来阻止肿瘤生长。主要介绍的SREBP抑制剂包括合成小分子结构(PF-429242、法图他汀等)和天然小分子结构(白桦脂醇、灵芝酸、大黄素等),通过作用于不同靶点而对SREBP产生抑制作用,从而抑制脂质合成。

Sterol regulatory element-binding proteins(SREBP) is an important regulator of lipid biosynthesis, which participates in the synthesis of fatty acids and cholesterol, and regulates the gene expression of several key lipid synthesis enzymes. SREBP inhibitors inhibit the activity of SREBP by inhibiting the synthesis, shearing, and transport of SREBP, thus reducing the level of lipid synthesis to prevent the growth of tumors. SREBP inhibitors mainly include synthetic drugs of small molecular structures(PF-429242, fatustatin,etc.) and natural medicine of small molecular structures(betulinol, ganoderic acid, emodin, etc.), which inhibit SREBP by acting on different targets and inhibit lipid synthesis.