中国药科大学学报2026,Vol.57Issue(2):133-143,11.DOI:10.11665/j.issn.1000-5048.2025051301
细胞氧感受器FIH抑制剂的研究进展
Research progress of cellular oxygen sensor FIH inhibitors
摘要
Abstract
The cellular oxygen sensor factor inhibiting HIF(FIH)is a JmjC domain-containing 2-oxoglutarate and Fe(II)-dependent oxygenase that catalyzes the hydroxylation of specific asparagine residues in the C-terminal transcriptional activation domain of hypoxia-inducible factor(HIF)-α.This modification inhibits HIF transcriptional activity by suppressing its interaction with the transcriptional coactivator p300/CBP.FIH inhibitors have attracted considerable attention due to their potential metabolic regulatory capabilities,particularly their significant therapeutic potential in improving lipid metabolic disorders.This review provides a detailed discussion of the catalytic mechanism of FIH and its biological functions in regulating the HIF pathway.In addition,it highlights recent advances in the development of FIH inhibitors and further explores their potential applications in the treatment of lipid metabolic diseases,offering new insights for the development of drugs targeting lipid metabolism disorders.关键词
细胞氧感知通路/FIH抑制剂/脂质代谢性疾病/2OG加氧酶Key words
cellular oxygen pathway/FIH inhibitor/lipid metabolic disorders/2OG oxygenases分类
医药卫生引用本文复制引用
伍悦,张晓进..细胞氧感受器FIH抑制剂的研究进展[J].中国药科大学学报,2026,57(2):133-143,11.基金项目
国家自然科学青年基金项目(No.82504579) (No.82504579)
江苏省基础研究计划(BK20251577) (BK20251577)
中国博士后创新人才支持项目(BX20250210) (BX20250210)
国家自然科学基金优秀青年基金项目(No.82322062)This work was supported by the Young Scientists Fund of National Natural Science Foundation of China(No.82504579) (No.82322062)
Basic Research Program of Jiangsu Province(BK20251577) (BK20251577)
China Postdoctoral Science Foundation(BX20250210) (BX20250210)
the Excellent Young Scientists Fund of National Natural Science Foundation of China(No.82322062) (No.82322062)