Strategies that regulate LSD1 for novel therapeutics
作者机构：School of Pharmaceutical Sciences&Key Laboratory of Advanced Drug Preparation TechnologiesMinistry of EducationZhengzhou UniversityZhengzhou 450001China College of ChemistryZhengzhou UniversityZhengzhou 450001China Tianjian Laboratory of Advanced Biomedical SciencesInstitute of Advanced Biomedical SciencesZhengzhou UniversityZhengzhou 450000China Pingyuan LaboratoryState Key Laboratory of Antiviral DrugsHenan Normal UniversityXinxiang 453007China State Key Laboratory of Pharmaceutical BiotechnologyNanjing UniversityNanjing 210023China
出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)
年 卷 期：2024年第14卷第4期
页 面：1494-1507页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学]
基 金：This work was supported by Natural Science Foundation of China(Nos.81903770,81973177,and 22277110,China) Joint Funds of Technology Research and Development Plan of Henan Province(No.232301420058,China) China Postdoctoral Science Foundation(No.2019M662556,China) Key scientific and technological projects of Henan Province(No.222102310125,China) Natural Science Foundation of Henan Province(No.222300420069,China) Program for Science&Technology Innovation Talents in Universities of Henan Province(No.21HASTIT045,China) Cultivation Project of Zhengzhou University(JC23852097,China) Tianjian Laboratory of Advanced Biomedical Sciences,and the open fund of State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,China(No.KF-202303,China)
主 题：LSD1 regulation Transcription repression Transcription activation the Corepressor complex Post-transcriptional modifications Metabolites
摘 要：Histone methylation plays crucial roles in regulating chromatin structure and gene transcrip-tion in epigenetic ***-specific demethylase 1(LSD1),the first identified histone de-methylase,is universally overexpressed in various ***1 dysregulation is closely associated with cancer,viral infections,and neurodegenerative diseases,etc.,making it a promising therapeutic *** LSD1 inhibitors and two small-molecule degraders(UM171 and BEA-17)have entered the clinical ***1 can remove methyl groups from histone 3 at lysine 4 or lysine 9(H3K4 or H3K9),resulting in either transcription repression or *** the roles of LSD1 in transcrip-tional regulation are well-established,studies have revealed that LSDl can also be dynamically regulated by other *** example,the expression or activity of LSD1 can be regulated by many proteins that form transcriptional corepressor complexes with ***,some post-transcriptional modifica-tions and cellular metabolites can also regulate LSD1 expression or its demethylase ***,in this review,we will systematically summarize how proteins involved in the transcriptional corepressor complex,various post-translational modifications,and metabolites act as regulatory factors for LSD1 ac-tivity.
维普期刊数据库