153. Hauser A-T, Roatsch M, Schulz-Fincke J, Robaa D, Sippl W, Jung M (2015) Chapter 18 –
discovery of histone demethylase inhibitors. Epigenetic technological applications. Academic
Press, Boston, pp 397–424. https://doi.org/10.1016/B978-0-12-801080-8.00018-1
154. Chu CH, Wang LY, Hsu KC, Chen CC, Cheng HH, Wang SM, Wu CM, Chen TJ, Li LT, Liu
RW, Hung CL, Yang JM, Kung HJ, Wang WC (2014) KDM4B as a target for prostate cancer:
structural analysis and selective inhibition by a novel inhibitor. J Med Chem 57
(14):5975–5985. https://doi.org/10.1021/jm500249n
155. Roatsch M, Robaa D, Pippel M, Nettleship JE, Reddivari Y, Bird LE, Hoffmann I, Franz H,
Owens RJ, Schule R, Flaig R, Sippl W, Jung M (2016) Substituted 2-(2-aminopyrimidin-4-yl)
pyridine-4-carboxylates as potent inhibitors of JumonjiC domain-containing histone
demethylases. Future Med Chem 8(13):1553–1571. https://doi.org/10.4155/fmc.15.188
156. Franci G, Sarno F, Nebbioso A, Altucci L (2017) Identification and characterization of
PKF118-310 as a KDM4A inhibitor. Epigenetics 12(3):198–205. https://doi.org/10.1080/
15592294.2016.1249089
157. Korczynska M, Le DD, Younger N, Gregori-Puigjane E, Tumber A, Krojer T, Velupillai S,
Gileadi C, Nowak RP, Iwasa E, Pollock SB, Ortiz Torres I, Oppermann U, Shoichet BK,
Fujimori DG (2016) Docking and linking of fragments to discover Jumonji histone
demethylase inhibitors. J Med Chem 59(4):1580–1598. https://doi.org/10.1021/acs.
jmedchem.5b01527
158. Fang Z, Wang TQ, Li H, Zhang G, Wu XA, Yang L, Peng YL, Zou J, Li LL, Xiang R, Yang
SY (2017) Discovery of pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives as a new class of
histone lysine demethylase 4D (KDM4D) inhibitors. Bioorg Med Chem Lett 27
(14):3201–3204. https://doi.org/10.1016/j.bmcl.2017.05.002
159. Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JS, Kales SC, Mott
BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns
MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X (2016) Structural basis for KDM5A
histone lysine demethylase inhibition by diverse compounds. Cell Chem Biol 23(7):769–781.
https://doi.org/10.1016/j.chembiol.2016.06.006
160. Wu XA, Fang Z, Yang B, Zhong L, Yang QY, Zhang CH, Huang SZ, Xiang R, Suzuki T, Li
LL, Yang SY (2016) Discovery of KDM5A inhibitors: homology modeling, virtual screening
and structure-activity relationship analysis. Bioorg Med Chem Lett 26(9):2284–2288. https://
doi.org/10.1016/j.bmcl.2016.03.048
486
D. Robaa et al.
discovery of histone demethylase inhibitors. Epigenetic technological applications. Academic
Press, Boston, pp 397–424. https://doi.org/10.1016/B978-0-12-801080-8.00018-1
154. Chu CH, Wang LY, Hsu KC, Chen CC, Cheng HH, Wang SM, Wu CM, Chen TJ, Li LT, Liu
RW, Hung CL, Yang JM, Kung HJ, Wang WC (2014) KDM4B as a target for prostate cancer:
structural analysis and selective inhibition by a novel inhibitor. J Med Chem 57
(14):5975–5985. https://doi.org/10.1021/jm500249n
155. Roatsch M, Robaa D, Pippel M, Nettleship JE, Reddivari Y, Bird LE, Hoffmann I, Franz H,
Owens RJ, Schule R, Flaig R, Sippl W, Jung M (2016) Substituted 2-(2-aminopyrimidin-4-yl)
pyridine-4-carboxylates as potent inhibitors of JumonjiC domain-containing histone
demethylases. Future Med Chem 8(13):1553–1571. https://doi.org/10.4155/fmc.15.188
156. Franci G, Sarno F, Nebbioso A, Altucci L (2017) Identification and characterization of
PKF118-310 as a KDM4A inhibitor. Epigenetics 12(3):198–205. https://doi.org/10.1080/
15592294.2016.1249089
157. Korczynska M, Le DD, Younger N, Gregori-Puigjane E, Tumber A, Krojer T, Velupillai S,
Gileadi C, Nowak RP, Iwasa E, Pollock SB, Ortiz Torres I, Oppermann U, Shoichet BK,
Fujimori DG (2016) Docking and linking of fragments to discover Jumonji histone
demethylase inhibitors. J Med Chem 59(4):1580–1598. https://doi.org/10.1021/acs.
jmedchem.5b01527
158. Fang Z, Wang TQ, Li H, Zhang G, Wu XA, Yang L, Peng YL, Zou J, Li LL, Xiang R, Yang
SY (2017) Discovery of pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives as a new class of
histone lysine demethylase 4D (KDM4D) inhibitors. Bioorg Med Chem Lett 27
(14):3201–3204. https://doi.org/10.1016/j.bmcl.2017.05.002
159. Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JS, Kales SC, Mott
BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns
MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X (2016) Structural basis for KDM5A
histone lysine demethylase inhibition by diverse compounds. Cell Chem Biol 23(7):769–781.
https://doi.org/10.1016/j.chembiol.2016.06.006
160. Wu XA, Fang Z, Yang B, Zhong L, Yang QY, Zhang CH, Huang SZ, Xiang R, Suzuki T, Li
LL, Yang SY (2016) Discovery of KDM5A inhibitors: homology modeling, virtual screening
and structure-activity relationship analysis. Bioorg Med Chem Lett 26(9):2284–2288. https://
doi.org/10.1016/j.bmcl.2016.03.048
486
D. Robaa et al.