ACS Medicinal Chemistry Letters
Page 12 of 13
1
2
3
4
5
6
7
8
9
1
1
1
1
1
1
1
1
1
1
2
2
2
2
2
2
2
2
2
2
3
3
3
3
3
3
3
3
3
3
4
4
4
4
4
4
4
4
4
4
5
5
5
5
5
5
5
5
5
5
6
1
2
3
4
Bannister, A. J.; Kouzarides, T. Regulation of chromatin by histone modifications. Cell Res. 2011, 23, 381-395.
Kouzarides, T.;Chromatin modifications and their function. Cell. 2007, 128, 693-705.
Suvà, M. L.; Riggi, N.; Bernstein, B. E. Epigenetic reprogramming in cancer. Science. 2013, 339, 1567-1570.
Shi, Y.; Lan, F.; Matson, C.; Mulligan, P.. Whetstine, J. R.; Cole, P. A.; Casero, R. A.; Shi, Y. Histone demethylation
mediated by the nuclear amine oxidase homolog LSD1. Cell. 2004, 119, 941-953.
5
Metzger, E.; Wissman, M.; Yin, N.; Mueller, J. M.; Schneider, R.; Peters, A.; Guenther, T.; Buettner, R.; Schuele, R.
0
1
2
3
4
5
6
7
8
9
0
1
2
3
4
5
6
7
8
9
0
1
2
3
4
5
6
7
8
9
0
1
2
3
4
5
6
7
8
9
0
1
2
3
4
5
6
7
8
9
0
LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription. Nature.
2
005, 437, 436-439.
6
Cho, H. S.; Suzuki, T.; Dohmae, N.; Hayami, S.; Unoki, M.; Yoshimatsu, M.; Toyokawa, G.; Takawa, M.; Chen, T.;
Kurash, J. K.; Field, H. I.; Ponder, B. A.; Nakamura, Y.; Hamamoto, R. Demethylation of RB regulator MYPT1 by histone
demethylase LSD1 promotes cell cycle progression in cancer cells. Cancer Res. 2011, 71, 655-660.
7
Li, Y.; Deng, C.; Hu, X.; Patel, B.; Fu, X.; Qui, Y.; Brand, M.; Zhao, K.; Huang, S. Dynamic interaction between TAL1
oncoprotein and LSD1 regulates TAL1 function in hematopoiesis and leukemogenesis. Oncogene. 2012, 31, 5007-
5
018.
8
Lv, S.; Bu, W.; Jiao, H.; Liu, B.; Zhu, L.; Zhao, H.; Liao, J.; Li, J.; Xu, X. LSD1 is required for chromosome segregation
during mitosis. Eur. J. Cell. Biol. 2010, 89, 557-563.
9
Goodmann, M.; Auger, V.; Ferraroni0Aguiar, V.; Di Sauro, A.; Sette, C.; Behr, R.; Kimmins, S. Dynamic regulation of
histone H3 methylation at lysine 4 in mammalian spermatogenesis. Biol. Reprod. 2007, 77, 754-764.
1
0
Zhou, H.; Li, W.; Zhu, S.; Joo, J. Y.; Do, J. T.; Xiong, W.; Kim, J. B.; Zhang, K.; Schöler, H. R.; Ding, S. Conversion of
mouse epiblast stem cells to an earlier pluripotency state by small molecules. J. Biol. Chem. 2010, 285, 29676-29680.
1
1
Foster, C. T.; Dovey, O. M.; Lezina, L.; Luo, J. L.; Gant, T. W.; Barlev, N.; Bradley, A.; Cowley, S. M. Lysine-specific
demethylase 1 regulates the embryonic transcriptome and CoREST stability. Mol. Cell Biol. 2010, 4851-4863.
1
2
Hayami, S.; Kelly, J. D.; Yoshimatsu, M.; Unoki, M.; Tsunoda, T.; Field, H. I.; Neal, D. E.; Yamaue, H.; Ponder, B. A.;
Nakamura, Y.; Hamamoto, R. Overexpression of LSD1 contributes to human carcinogenesis through chromatin
regulation in various cancers. Int. J. Cancer. 2011, 128, 574-586
1
3
Kosumi, K.; Baba, Y.; Sakamoto, A.; Ishimoto, T.; Harada, K.; Nakamura, K.; Kurashige, J.; Hiyoshi, Y.; Iwatsuki, M.;
Iwagami, S.; Sakamoto, Y.; Miyamoto, Y.; Yoshida, N.; Oki, E.; Watanabe, M.; Hino, S.; Nakao, M.; Baba, H.; Lysine-
specific demethylase-1 contriutes to malignant behavior by regulation of invasive activity and metabolic shift in
esophageal cancer. Int. J. Cancer. 2016, 138, 428-439.
1
4
Sheng, W.; LaFluer, M. W.; Nguyen, T. H.; Chen, S.; Chakravarthy, A.; Li, Y.; Chen, H.; Yang, H.; Hsu, P. H.; Van
Allen, E. M.; Freeman, G. J.; De Carvalho, D. D.; He, H. H.; Sharpe, A. H.; Shi, Y.; LSD1 ablation stimulates anti-tumor
immunity and enables checkpoint blockade. Cell 2018, 174, 549-563.
1
5
Harris, W. J.; Huang, X.; Lynch, J. T.; Spencer, G. J.; Hitchin, J. R.; Li, Y.; Ciceri, F.; Blaser, J. G.; Greystoke, B. F.;
Jordan, A. M.; Miller, C. J.; Ogilivie, D. J.; Somervaille, T. C. P. The histone demethylase KDM1A sustains the oncogenic
potential of MLL-AF9 leukemia stem cells. Cancer Cell 2012, 21, 473-487.
1
6
Mohammad, H. P; Smitheman, K. N.; Kamat, C. D.; Soong, D.; Federowicz, K. E.; Van Aller, G. S.; Schneck, J. L.;
Carson, J. D.; Liu, Y.; Butticello, M.; Bonnette, W. G.; Gorman, S. A.; Degenhardt, Y.; Bai, Y.; McCabe, M. T.; Pappalardi,
M. B.; Kasparec, J.; Tian, X.; McNulty, K.; Rouse, M.; McDevitt, P.; Ho, T.; Crouthamel, M.; Hart, T. K.; Concha, N. O.;
McHugh, C. F.; Miller, W. H.; Dhanak, D.; Tummino, P. J.; Carpenter, C. L.; Johnson, N. W.; Hann, C. L.; Kruger, R. G.
A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell 2015, 28, 57-
69.
patients
with
myelofibrosis.
1
8
Forneris, F.; Binda, C.; Battaglioli, E.; Mattevi, A. LSD1: oxidative chemistry for multifaceted functions in chromatin
regulation. Trends Biochem. Sci. 2008, 33, 6827-6833.
1
9
Binda, C.; Valente, S.; Romanenghi, M.; Pilotto, S.; Cirilli,R.; Karytinos, A.; Ciossani, G.; Botrugno, O. A.; Forneris,
F.; Tardugno, M.; Edmondson, D. E.; Minucci, S.; Mattevi, A.; Mai, A. Biochemical, Structural, and Biological
Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2. J. Am. Chem. Soc.
2
010 132, 6827-6833.
ACS Paragon Plus Environment