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Cole PA, Yu H (2007) Structural basis of histone demethylation by LSD1 revealed by suicide
inactivation. Nat Struct Mol Biol 14(6):535–539. https://doi.org/10.1038/nsmb1255
128. Forneris F, Battaglioli E, Mattevi A, Binda C (2009) New roles of flavoproteins in molecular
cell biology: histone demethylase LSD1 and chromatin. FEBS J 276(16):4304–4312. https://
doi.org/10.1111/j.1742-4658.2009.07142.x
129. Hojfeldt JW, Agger K, Helin K (2013) Histone lysine demethylases as targets for anticancer
therapy. Nat Rev Drug Discov 12(12):917–930. https://doi.org/10.1038/nrd4154
130. Schmitt ML, Hauser AT, Carlino L, Pippel M, Schulz-Fincke J, Metzger E, Willmann D,
Yiu T, Barton M, Schule R, Sippl W, Jung M (2013) Nonpeptidic propargylamines as
inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity. J Med Chem 56
(18):7334–7342. https://doi.org/10.1021/jm400792m
131. Sorna V, Theisen ER, Stephens B, Warner SL, Bearss DJ, Vankayalapati H, Sharma S (2013)
High-throughput virtual screening identifies novel N
0 -(1-phenylethylidene)-benzohydrazides
as potent, specific, and reversible LSD1 inhibitors. J Med Chem 56(23):9496–9508. https://
doi.org/10.1021/jm400870h
132. Zhou C, Kang D, Xu YG, Zhang LY, Zha XM (2015) Identification of novel selective lysinespecific demethylase 1 (LSD1) inhibitors using a pharmacophore-based virtual screening
combined with docking. Chem Biol Drug Des 85(6):659–671. https://doi.org/10.1111/cbdd.
12461
133. Zhou C, Wu F, Lu L, Wei L, Pai E, Yao Y, Song Y (2017) Structure activity relationship and
modeling studies of inhibitors of lysine specific demethylase 1. Plos One 12(2):e0170301.
https://doi.org/10.1371/journal.pone.0170301
134. Pieroni M, Annunziato G, Azzali E, Dessanti P, Mercurio C, Meroni G, Trifiró P, Vianello P,
Villa M, Beato C, Varasi M, Costantino G (2015) Further insights into the SAR of
α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A.
Eur J Med Chem 92:377–386. https://doi.org/10.1016/j.ejmech.2014.12.032
135. Mould DP, Bremberg U, Jordan AM, Geitmann M, McGonagle AE, Somervaille TCP,
Spencer GJ, Ogilvie DJ (2017) Development and evaluation of 4-(pyrrolidin-3-yl)benzonitrile
derivatives as inhibitors of lysine specific demethylase 1. Bioorg Med Chem Lett 27
(20):4755–4759. https://doi.org/10.1016/j.bmcl.2017.08.052
136. Xi J, Xu S, Wu L, Ma T, Liu R, Liu Y-C, Deng D, Gu Y, Zhou J, Lan F, Zha X (2017) Design,
synthesis and biological activity of 3-oxoamino-benzenesulfonamides as selective and reversible LSD1 inhibitors. Bioorg Chem 72:182–189. https://doi.org/10.1016/j.bioorg.2017.04.006
137. Han C, Li Z, Hou J, Wang Z, Xu D, Xue G, Kong L (2018) Bioactivity evaluation of natural
product α-mangostin as a novel xanthone-based lysine-specific demethylase 1 inhibitor to
against tumor metastasis. Bioorg Chem 76:415–419. https://doi.org/10.1016/j.bioorg.2017.12.
004
138. Wang S, Zhao L-J, Zheng Y-C, Shen D-D, Miao E-F, Qiao X-P, Zhao L-J, Liu Y, Huang R,
Yu B, Liu H-M (2017) Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]
pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors. Eur J Med
Chem 125:940–951. https://doi.org/10.1016/j.ejmech.2016.10.021
139. Duan Y-C, Guan Y-Y, Zhai X-Y, Ding L-N, Qin W-P, Shen D-D, Liu X-Q, Sun X-D, Zheng
Y-C, Liu H-M (2017) Discovery of resveratrol derivatives as novel LSD1 inhibitors: design,
synthesis and their biological evaluation. Eur J Med Chem 126:246–258. https://doi.org/10.
1016/j.ejmech.2016.11.035
140. Duan Y-C, Ma Y-C, Qin W-P, Ding L-N, Zheng Y-C, Zhu Y-L, Zhai X-Y, Yang J, Ma C-Y,
Guan Y-Y (2017) Design and synthesis of tranylcypromine derivatives as novel LSD1/
484
D. Robaa et al.