Targeting Histone Lysine Demethylase LSD1/KDM1A as a New Avenue for Cancer Therapy

Author(s): Yuan Fang, Guochao Liao*, Bin Yu*.

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 11 , 2019

Become EABM
Become Reviewer

[1]
Zheng, Y-C.; Yu, B.; Chen, Z-S.; Liu, Y.; Liu, H-M. TCPs: Privileged scaffolds for identifying potent LSD1 inhibitors for cancer therapy. Epigenomics, 2016, 8, 651-666.
[2]
Zheng Y. Yu B.; Jiang G.; Feng X.; He P.; Chu X.; Zhao W.; M. Liu H. Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment. Curr. Top. Med. Chem., 2016, 16, 2179-2188.
[3]
Fu, X.; Zhang, P.; Yu, B. Advances toward LSD1 inhibitors for cancer therapy. Future Med. Chem., 2017, 9, 1227-1242.
[4]
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. 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., 2017, 125, 940-951.
[5]
Li, Z-R.; Wang, S.; Yang, L.; Yuan, X-H.; Suo, F-Z.; Yu, B.; Liu, H-M. Experience-based discovery (EBD) of aryl hydrazines as new scaffolds for the development of LSD1/KDM1A inhibitors. Eur. J. Med. Chem., 2019, 166, 432-444.
[6]
Wang, S.; Li, Z-R.; Suo, F-Z.; Yuan, X-H.; Yu, B.; Liu, H-M. Synthesis, structure-activity relationship studies and biological characterization of new [1,2,4]triazolo[1,5-a]pyrimidine-based LSD1/KDM1A inhibitors. Eur. J. Med. Chem., 2019, 167, 388-401.
[7]
Kalin, J.H.; Wu, M.; Gomez, A.V.; Song, Y.; Das, J.; Hayward, D.; Adejola, N.; Wu, M.; Panova, I.; Chung, H.J.; Kim, E.; Roberts, H.J.; Roberts, J.M.; Prusevich, P.; Jeliazkov, J.R.; Burman, S.S.; Fairall, L.; Milano, C.; Eroglu, A.; Proby, C.M.; Dinkova-Kostova, A.T.; Hancock, W.W.; Gray, J.J.; Bradner, J.E.; Valente, S.; Mai, A.; Anders, N.M.; Rudek, M.A.; Hu, Y.; Ryu, B.; Schwabe, J.W.R.; Mattevi, A.; Alani, R.M.; Cole, P.A. Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors. Nat. Commun., 2018, 9, 53.
[8]
Li, Z-R.; Suo, F-Z.; Hu, B.; Guo, Y-J.; Fu, D-J.; Yu, B.; Zheng, Y-C.; Liu, H-M. Identification of osimertinib (AZD9291) as a lysine specific demethylase 1 inhibitor. Bioorg. Chem., 2019, 84, 164-169.
[9]
An, S.; Fu, L. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine, 2018, 36, 553-562.
[10]
Sehrawat, A.; Gao, L.; Wang, Y.; Bankhead, A.; McWeeney, S.K.; King, C.J.; Schwartzman, J.; Urrutia, J.; Bisson, W.H.; Coleman, D.J.; Joshi, S.K.; Kim, D.H.; Sampson, D.A.; Weinmann, S.; Kallakury, B.V.S.; Berry, D.L.; Haque, R.; Van Den Eeden, S.K.; Sharma, S.; Bearss, J.; Beer, T.M.; Thomas, G.V.; Heiser, L.M.; Alumkal, J.J. LSD1 activates a lethal prostate cancer gene network independently of its demethylase function. Proc. Natl. Acad. Sci. USA, 2018, 115, E4179-E4188.


Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 19
ISSUE: 11
Year: 2019
Page: [889 - 891]
Pages: 3
DOI: 10.2174/156802661911190725094910

Article Metrics

PDF: 11
HTML: 3