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Current Topics in Medicinal Chemistry

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ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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Perspectives in Medicinal Chemistry

Targeting KDM5 Demethylases: Inhibition and Degradation

Author(s): Xiaoli Fu, Chao Yang* and Bin Yu*

Volume 20, Issue 4, 2020

Page: [261 - 263] Pages: 3

DOI: 10.2174/156802662004200304124340

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[1]
Fang, Y.; Liao, G.; Yu, B. LSD1/KDM1A inhibitors in clinical trials: Advances and prospects. J. Hema. Onco., 2019, 12, 129.
[2]
Johansson, C.; Velupillai, S.; Tumber, A.; Szykowska, A.; Hookway, E.S.; Nowak, R.P.; Strain-Damerell, C.; Gileadi, C.; Philpott, M.; Burgess-Brown, N.; Wu, N.; Kopec, J.; Nuzzi, A.; Steuber, H.; Egner, U.; Badock, V.; Munro, S.; LaThangue, N.B.; Westaway, S.; Brown, J.; Athanasou, N.; Prinjha, R.; Brennan, P.E.; Oppermann, U. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat. Chem. Biol., 2016, 12, 539-545.
[3]
Longbotham, J.E.; Chio, C.M.; Dharmarajan, V.; Trnka, M.J.; Torres, I.O.; Goswami, D.; Ruiz, K.; Burlingame, A.L.; Griffin, P.R.; Fujimori, D.G. Histone H3 binding to the PHD1 domain of histone demethylase KDM5A enables active site remodeling. Nat. Commun., 2019, 10, 94.
[4]
Johansson, C.; Tumber, A.; Che, K.; Cain, P.; Nowak, R.; Gileadi, C.; Oppermann, U. The roles of Jumonji-type oxygenases in human disease. Epigenomics, 2014, 89-120.
[5]
Wu, L.; Cao, J.; Cai, W.L.; Lang, S.M.; Horton, J.R.; Jansen, D.J.; Liu, Z.Z.; Chen, J.F.; Zhang, M.; Mott, B.T.; Pohida, K.; Rai, G.; Kales, S.C.; Henderson, M.J.; Hu, X.; Jadhav, A.; Maloney, D.J.; Simeonov, A.; Zhu, S.; Iwasaki, A.; Hall, M.D.; Cheng, X.; Shadel, G.S.; Yan, Q. KDM5 histone demethylases repress immune response via suppression of STING. PLOS Bio., 2018, 16 e2006134
[6]
Vinogradova, M.; Gehling, V.S.; Gustafson, A.; Arora, S.; Tindell, C.A.; Wilson, C.; Williamson, K.E.; Guler, G.D.; Gangurde, P.; Manieri, W.; Busby, J.; Flynn, E.M.; Lan, F.; Kim, H-J.; Odate, S.; Cochran, A.G.; Liu, Y.; Wongchenko, M.; Yang, Y.; Cheung, T.K.; Maile, T.M.; Lau, T.; Costa, M.; Hegde, G.V.; Jackson, E.; Pitti, R.; Arnott, D.; Bailey, C.; Bellon, S.; Cummings, R.T.; Albrecht, B.K.; Harmange, J-C.; Kiefer, J.R.; Trojer, P.; Classon, M. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat. Chem. Biol., 2016, 12, 531-538.
[7]
Brier, A-S.B.; Loft, A.; Madsen, J.G.S.; Rosengren, T.; Nielsen, R.; Schmidt, S.F.; Liu, Z.; Yan, Q.; Gronemeyer, H.; Mandrup, S. The KDM5 family is required for activation of pro-proliferative cell cycle genes during adipocyte differentiation. Nucleic Acids Res., 2017, 45, 1743-1759.
[8]
Huang, D.; Qiu, Y.; Li, G.; Liu, C.; She, L.; Zhang, D.; Chen, X.; Zhu, G.; Zhang, X.; Tian, Y.; Liu, Y. KDM5B overexpression predicts a poor prognosis in patients with squamous cell carcinoma of the head and neck. J. Cancer, 2018, 9, 198-204.
[9]
Bachleitner, S.; Sørensen, J.L.; Gacek-Matthews, A.; Sulyok, M.; Studt, L.; Strauss, J. Evidence of a demethylase-independent role for the h3k4-specific histone demethylases in aspergillus nidulans and fusarium graminearum secondary metabolism. Front. Microbiol., 2019, 10, 1759.
[10]
Rasmussen, P.B.; Staller, P. The KDM5 family of histone demethylases as targets in oncology drug discovery. Epigenomics, 2014, 6, 277-286.
[11]
Taylor-Papadimitriou, J.; Burchell, J. JARID1/KDM5 demethylases as cancer targets? Exp. Opin. Therap. Tar., 2017, 21, 5-7.
[12]
Gilmore, S.; Tam, D.; Dick, R.; Appleby, T.; Birkus, G.; Willkom, M.; Delaney, W.E.; Notte, G.T.; Feierbach, B. Antiviral activity of GS-5801, a liver-targeted prodrug of a lysine demethylase 5 inhibitor, in a hepatitis B virus primary human hepatocyte infection model. J. Hepatol., 2017, 66, S690-S691.
[13]
Xu, W.; Zhou, B.; Zhao, X.; Zhu, L.; Xu, J.; Jiang, Z.; Chen, D.; Wei, Q.; Han, M.; Feng, L.; Wang, S.; Wang, X.; Zhou, J.; Jin, H. KDM5B demethylates H3K4 to recruit XRCC1 and promote chemoresistance. Int. J. Biol. Sci., 2018, 14, 1122-1132.
[14]
Bueno, M.T.D.; Richard, S. SUMOylation negatively modulates target gene occupancy of the KDM5B, a histone lysine demethylase. Epigenetics, 2013, 8, 1162-1175.
[15]
Ward, C.C.; Kleinman, J.I.; Brittain, S.M.; Lee, P.S.; Chung, C.Y.S.; Kim, K.; Petri, Y.; Thomas, J.R.; Tallarico, J.A.; McKenna, J.M.; Schirle, M.; Nomura, D.K. Covalent ligand screening uncovers a rnf4 e3 ligase recruiter for targeted protein degradation applications. ACS Chem. Biol., 2019, 14, 2430-2440.

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