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Inhibitors of JmjC-Containing Histone Demethylases
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KDM5 inhibitors. Bioorg Med Chem Lett 28:1490–1494. https://doi.org/10.1016/j.bmcl.2018.
03.083
69. Liang J, Zhang B, Labadie S et al (2016) Lead optimization of a pyrazolo[1,5-a]pyrimidin-7
(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable
for in vivo biological studies. Bioorg Med Chem Lett 26:4036–4041. https://doi.org/10.1016/j.
bmcl.2016.06.078
70. Labadie SS, Dragovich PS, Cummings RT et al (2016) Design and evaluation of
1,7-naphthyridones as novel KDM5 inhibitors. Bioorg Med Chem Lett 26:4492–4496.
https://doi.org/10.1016/j.bmcl.2016.07.070
71. Liang J, Labadie S, Zhang B et al (2017) From a novel HTS hit to potent, selective, and orally
bioavailable KDM5 inhibitors. Bioorg Med Chem Lett 27:2974–2981. https://doi.org/10.1016/
j.bmcl.2017.05.016
72. Heinemann B, Nielsen JM, Hudlebusch HR et al (2014) Inhibition of demethylases by GSK-J1/
J4. Nature 514:E1
73. Woon ECY, Tumber A, Kawamura A et al (2012) Linking of 2-oxoglutarate and substrate
binding sites enables potent and highly selective inhibition of JmjC histone demethylases.
Angew Chem Int Ed Engl 51:1631–1634. https://doi.org/10.1002/anie.201107833
74. Hillringhaus L, Yue WW, Rose NR et al (2011) Structural and evolutionary basis for the dual
substrate selectivity of human KDM4 histone demethylase family. J Biol Chem
286:41616–41625. https://doi.org/10.1074/jbc.M111.283689
75. Lohse B, Nielsen AL, Kristensen JBL et al (2011) Targeting histone lysine demethylases by
truncating the histone 3 tail to obtain selective substrate-based inhibitors. Angew Chem Int Ed
Engl 50:9100–9103. https://doi.org/10.1002/anie.201101849
76. Kawamura A, Münzel M, Kojima T et al (2017) Highly selective inhibition of histone
demethylases by de novo macrocyclic peptides. Nat Commun 8:14773. https://doi.org/10.
1038/ncomms14773
77. Chang Y, Zhang X, Horton JR et al (2009) Structural basis for G9a-like protein lysine
methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol 16:312–317. https://doi.org/
10.1038/nsmb.1560
78. Upadhyay AK, Rotili D, Han JW et al (2012) An analog of BIX-01294 selectively inhibits a
family of histone H3 lysine 9 Jumonji demethylases. J Mol Biol 416:319–327. https://doi.org/
10.1016/j.jmb.2011.12.036
79. Gerken PA, Wolstenhulme JR, Tumber A et al (2017) Discovery of a highly selective cellactive inhibitor of the histone lysine demethylases KDM2/7. Angew Chem Int Ed
56:15555–15559. https://doi.org/10.1002/anie.201706788
Inhibitors of JmjC-Containing Histone Demethylases
253