胆固醇及其代谢产物具有重要的生物学功能。胆固醇能够维持细胞膜的物理特性，在细胞信号传导中发挥重要作用，细胞胆固醇水平反映了生物合成、摄取、外流和酯化之间的动态平衡。胆固醇代谢参与了胆汁酸生产和类固醇激素合成。越来越多的证据表明，胆固醇代谢与肿瘤之间存在严格的联系。肿瘤细胞中的胆固醇代谢与正常细胞有着显著的差异，胆固醇平衡的紊乱也会引发肿瘤发生和进展。临床前和临床研究表明，控制胆固醇代谢可抑制肿瘤生长，提示靶向胆固醇代谢可能为肿瘤治疗提供新的可能性。在本综述中，我们总结了正常和肿瘤细胞中胆固醇的代谢途径，并回顾了从实验室到临床的靶向不同阶段胆固醇代谢的药物治疗新策略的临床进展。版权所有©2023夏、王、周、王、薛、曹和宋。

Cholesterol and its metabolites have important biological functions. Cholesterol is able to maintain the physical properties of cell membrane, play an important role in cellular signaling, and cellular cholesterol levels reflect the dynamic balance between biosynthesis, uptake, efflux and esterification. Cholesterol metabolism participates in bile acid production and steroid hormone biosynthesis. Increasing evidence suggests a strict link between cholesterol homeostasis and tumors. Cholesterol metabolism in tumor cells is reprogrammed to differ significantly from normal cells, and disturbances of cholesterol balance also induce tumorigenesis and progression. Preclinical and clinical studies have shown that controlling cholesterol metabolism suppresses tumor growth, suggesting that targeting cholesterol metabolism may provide new possibilities for tumor therapy. In this review, we summarized the metabolic pathways of cholesterol in normal and tumor cells and reviewed the pre-clinical and clinical progression of novel tumor therapeutic strategy with the drugs targeting different stages of cholesterol metabolism from bench to bedside.Copyright © 2023 Xia, Wang, Zhou, Wang, Xue, Cao and Song.