首页|Strategies that regulate LSD1 for novel therapeutics

Strategies that regulate LSD1 for novel therapeutics

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Histone methylation plays crucial roles in regulating chromatin structure and gene transcrip-tion in epigenetic modifications.Lysine-specific demethylase 1(LSD1),the first identified histone de-methylase,is universally overexpressed in various diseases.LSD1 dysregulation is closely associated with cancer,viral infections,and neurodegenerative diseases,etc.,making it a promising therapeutic target.Several LSD1 inhibitors and two small-molecule degraders(UM171 and BEA-17)have entered the clinical stage.LSD1 can remove methyl groups from histone 3 at lysine 4 or lysine 9(H3K4 or H3K9),resulting in either transcription repression or activation.While the roles of LSD1 in transcrip-tional regulation are well-established,studies have revealed that LSD1 can also be dynamically regulated by other factors.For example,the expression or activity of LSD1 can be regulated by many proteins that form transcriptional corepressor complexes with LSD1.Moreover,some post-transcriptional modifica-tions and cellular metabolites can also regulate LSD1 expression or its demethylase activity.Therefore,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.

LSD1 regulationTranscription repressionTranscription activationthe Corepressor complexPost-transcriptional modificationsMetabolites

Meng Li、Mengge Dai、Bing Cheng、Shaotong Li、Enhui Guo、Junwei Fu、Ting Ma、Bin Yu

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School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies,Ministry of Education,Zhengzhou University,Zhengzhou 450001,China

Pingyuan Laboratory,State Key Laboratory of Antiviral Drugs,Henan Normal University,Xinxiang 453007,China

College of Chemistry,Zhengzhou University,Zhengzhou 450001,China

Tianjian Laboratory of Advanced Biomedical Sciences,Institute of Advanced Biomedical Sciences,Zhengzhou University,Zhengzhou 450000,China

State Key Laboratory of Pharmaceutical Biote

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国家自然科学基金国家自然科学基金国家自然科学基金Joint Funds of Technology Research and Development Plan of Henan Province,China中国博士后科学基金Key scientific and technological projects of Henan Province,China河南省自然科学基金Program for Science and Technology Innovation Talents in Universities of Henan Province,ChinaCultivation Project of Zhengzhou University,ChinaTianjian Laboratory of Advanced Biomedical Sciencesopen fund of State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,China,China

8190377081973177222771102323014200582019M66255622210231012522230042006921HASTIT045JC23852097KF-202303

2024

10.1016/j.apsb.2024.01.005

药学学报(英文版)

药学学报(英文版)

CSTPCD
ISSN：
年,卷(期)：2024.14(4)
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