title: A Systematic Review of Histone Lysine-Specific Demethylase 1 and Its Inhibitors.
abstract: Histone lysine-specific demethylase 1 (LSD1) is the first discovered and reported histone demethylase by Dr. Shi Yang's group in 2004. It is classified as a member of amine oxidase superfamily, the common feature of which is using the flavin adenine dinucleotide (FAD) as its cofactor. Since it is located in cell nucleus and acts as a histone methylation eraser, LSD1 specifically removes mono- or dimethylated histone H3 lysine 4 (H3K4) and H3 lysine 9 (H3K9) through formaldehyde-generating oxidation. It has been indicated that LSD1 and its downstream targets are involved in a wide range of biological courses, including embryonic development and tumor-cell growth and metastasis. LSD1 has been reported to be overexpressed in variety of tumors. Inactivating LSD1 or downregulating its expression inhibits cancer-cell development. LSD1 targeting inhibitors may represent a new insight in anticancer drug discovery. This review summarizes recent studies about LSD1 and mainly focuses on the basic physiological function of LSD1 and its involved mechanisms in pathophysiologic conditions, as well as the development of LSD1 inhibitors as potential anticancer therapeutic agents.
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Yi-Chao
authors.initials: YC
authors.lastname: Zheng
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Jinlian
authors.initials: J
authors.lastname: Ma
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Zhiru
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Li
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Bailing
authors.initials: B
authors.lastname: Jiang
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Wenjuan
authors.initials: W
authors.lastname: Zhou
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Xiaojing
authors.initials: X
authors.lastname: Shi
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Xixin
authors.initials: X
authors.lastname: Wang
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Wen
authors.initials: W
authors.lastname: Zhao
authors.affiliation: Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan, 450001, P. R. China.
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000378:metabolism; D002384:Catalysis; D002467:Cell Nucleus / Q000378:metabolism; D044127:Epigenesis, Genetic; D058750:Epithelial-Mesenchymal Transition; D005260:Female; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D006657:Histones / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D056004:Molecular Dynamics Simulation; D009362:Neoplasm Metastasis; D009369:Neoplasms / Q000378:metabolism; D010100:Oxygen / Q000737:chemistry; D010455:Peptides / Q000737:chemistry; D025941:Protein Interaction Mapping; D017434:Protein Structure, Tertiary; D011960:Receptors, Estrogen / Q000378:metabolism; D013234:Stem Cells / Q000378:metabolism; D014158:Transcription, Genetic
chemical_list: D000970:Antineoplastic Agents; D006657:Histones; D010455:Peptides; D011960:Receptors, Estrogen; D056466:Histone Demethylases; C495195:KDM1A protein, human; D010100:Oxygen
keywords: LSD1; cancer; histone modification; inhibitors