PMID: 26881714Feb 18, 2016Paper

Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment

Current Topics in Medicinal Chemistry
Yi C ZhengHong M Liu

Abstract

Due to the increasing costs and time consuming for new drug discovery, a large number of pharmaceutical firms have chosen to modify the existing drug molecules for repositioning candidates with new or improved properties, especially those with severe adverse effects, thereby accelerating the drug discovery process. Such strategy has witnessed its success with several examples reported. As the first identified histone lysine specific demethylase, lysine specific demethylase 1 (LSD1) is classified as a member of monoamine oxidase (MAO) superfamily, and specifically removes mono- and dimethylated histone 3 lysine 4 (H3K4) and H3 lysine 9 (H3K9). It has been reported that LSD1 and its downstream targets are involved in cancer cell growth and metastasis. Meanwhile, it is overexpressed in a variety of tumor cells. Inactivating LSD1 specifically inhibits tumor progression and metastasis. Hence, LSD1 inhibition may represent a new and promising direction in anti-cancer drug discovery. Based on the structure and cofactor of LSD1, some clinical applied MAO inhibitors have been identified as LSD1 inactivators. Among them, tranylcypromine presented the most potency against LSD1 and its derivatives were further developed by medicinal chemis...Continue Reading

Citations

Sep 15, 2016·Science Advances·Valentina SperanziniAndrea Mattevi
Jun 14, 2019·MedChemComm·Steven HolshouserPatrick M Woster
Aug 8, 2019·Current Topics in Medicinal Chemistry·Yuan FangBin Yu
Sep 16, 2020·Chemical Communications : Chem Comm·Xiao SunYan Su
Jul 20, 2017·Future Medicinal Chemistry·Xiaoli FuBin Yu
Jul 11, 2019·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Zhuochao LiuLianfu Deng
Oct 11, 2017·Annual Review of Pharmacology and Toxicology·Richard L Bennett, Jonathan D Licht
Sep 20, 2018·Cell Communication and Signaling : CCS·Keri CallegariVidya Gopalakrishnan
Dec 6, 2019·Journal of Hematology & Oncology·Yuan FangBin Yu
Feb 16, 2019·Nature Reviews. Urology·Sina JostesHubert Schorle
Aug 23, 2019·World Journal of Gastrointestinal Oncology·Hong-Ming PanXiao-Ling Li
Oct 21, 2020·European Journal of Medicinal Chemistry·Amr K A BassGamal El-Din A Abuo-Rahma
Dec 16, 2020·Experimental & Molecular Medicine·Bruno PerilloAntimo Migliaccio
Feb 14, 2021·European Journal of Medicinal Chemistry·Dong-Jun FuBin Yu
Feb 6, 2021·The FEBS Journal·Shengrui Feng, Daniel D De Carvalho
Mar 10, 2017·Trends in Biochemical Sciences·Valentina PianoAndrea Mattevi
Feb 21, 2018·European Journal of Medicinal Chemistry·Isuru R Kumarasinghe, Patrick M Woster
Feb 12, 2017·Pharmacology & Therapeutics·Subhankar Biswas, C Mallikarjuna Rao
Sep 16, 2020·Journal of Medicinal Chemistry·Xing-Jie DaiHong-Min Liu
Jul 2, 2019·Journal of the American Chemical Society·Yongjia ShiSenmiao Xu
Dec 5, 2021·Archiv der Pharmazie·Yixiang SunMaosheng Cheng

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