title: A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells.
abstract: We report herein a novel rhodium(III) complex 1 as a new LSD1 targeting agent and epigenetic modulator. Complex 1 disrupted the interaction of LSD1-H3K4me2 in human prostate carcinoma cells and enhanced the amplification of p21, FOXA2, and BMP2 gene promoters. Complex 1 was selective for LSD1 over other histone demethylases, such as KDM2b, KDM7, and MAO activities, and also showed antiproliferative activity toward human cancer cells. To date, complex 1 is the first metal-based inhibitor of LSD1 activity.
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Macau, China.
authors.forename: Chao
authors.initials: C
authors.lastname: Yang
authors.affiliation: Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong, China.
authors.forename: Wanhe
authors.initials: W
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Macau, China.
authors.forename: Jia-Xin
authors.initials: JX
authors.lastname: Liang
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Macau, China.
authors.forename: Guodong
authors.initials: G
authors.lastname: Li
authors.affiliation: Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong, China.
authors.forename: Kasipandi
authors.initials: K
authors.lastname: Vellaisamy
authors.affiliation: Department of Biology and Chemistry, City University of Hong Kong , Tat Chee Avenue, Kowloon, Hong Kong SAR, China.
authors.forename: Chun-Yuen
authors.identifier: 0000-0003-4780-480X
authors.initials: CY
authors.lastname: Wong
authors.affiliation: Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong, China.
authors.forename: Dik-Lung
authors.identifier: 0000-0002-9515-340X
authors.initials: DL
authors.lastname: Ma
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Macau, China.
authors.forename: Chung-Hang
authors.identifier: 0000-0003-2988-3786
authors.initials: CH
authors.lastname: Leung
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology*; D044127:Epigenesis, Genetic / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008297:Male; D062105:Molecular Docking Simulation; D011467:Prostate / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000473:pathology; D012238:Rhodium / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D012238:Rhodium; D056466:Histone Demethylases; C495195:KDM1A protein, human