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Kireev DB, Janzen WP, Arrowsmith CH, Frye SV (2013) The structure-activity relationships
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183. Stec I, Nagl SB, van Ommen GJ, den Dunnen JT (2000) The PWWP domain: a potential
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184. Wu H, Zeng H, Lam R, Tempel W, Amaya MF, Xu C, Dombrovski L, Qiu W, Wang Y, Min J
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185. Qin S, Min J (2014) Structure and function of the nucleosome-binding PWWP domain. Trends
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186. Wang Y, Reddy B, Thompson J, Wang H, Noma K, Yates JR 3rd, Jia S (2009) Regulation of
Set9-mediated H4K20 methylation by a PWWP domain protein. Mol Cell 33(4):428–437.
https://doi.org/10.1016/j.molcel.2009.02.002
187. Dhayalan A, Rajavelu A, Rathert P, Tamas R, Jurkowska RZ, Ragozin S, Jeltsch A (2010)
The Dnmt3a PWWP domain reads histone 3 lysine 36 trimethylation and guides DNA
methylation. J Biol Chem 285(34):26114–26120. https://doi.org/10.1074/jbc.M109.089433
188. Vezzoli A, Bonadies N, Allen MD, Freund SM, Santiveri CM, Kvinlaug BT, Huntly BJ,
Gottgens B, Bycroft M (2010) Molecular basis of histone H3K36me3 recognition by the
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189. Huang Z, Wu H, Chuai S, Xu F, Yan F, Englund N, Wang Z, Zhang H, Fang M, Wang Y,
Gu J, Zhang M, Yang T, Zhao K, Yu Y, Dai J, Yi W, Zhou S, Li Q, Wu J, Liu J, Wu X,
Chan H, Lu C, Atadja P, Li E, Wang Y, Hu M (2013) NSD2 is recruited through its PHD
domain to oncogenic gene loci to drive multiple myeloma. Cancer Res 73(20):6277–6288.
https://doi.org/10.1158/0008-5472.CAN-13-1000
190. Hudlebusch HR, Santoni-Rugiu E, Simon R, Ralfkiaer E, Rossing HH, Johansen JV,
Jorgensen M, Sauter G, Helin K (2011) The histone methyltransferase and putative
oncoprotein MMSET is overexpressed in a large variety of human tumors. Clin Cancer Res
17(9):2919–2933. https://doi.org/10.1158/1078-0432.CCR-10-1302
191. Li J, Yin C, Okamoto H, Mushlin H, Balgley BM, Lee CS, Yuan K, Ikejiri B, Glasker S,
Vortmeyer AO, Oldfield EH, Weil RJ, Zhuang Z (2008) Identification of a novel proliferationrelated protein, WHSC1 4a, in human gliomas. Neuro Oncol 10(1):45–51. https://doi.org/10.
1215/15228517-2007-036
192. Kassambara A, Klein B, Moreaux J (2009) MMSET is overexpressed in cancers: link with
tumor aggressiveness. Biochem Biophys Res Commun 379(4):840–845. https://doi.org/10.
1016/j.bbrc.2008.12.093
193. Oyer JA, Huang X, Zheng Y, Shim J, Ezponda T, Carpenter Z, Allegretta M, Okot-Kotber CI,
Patel JP, Melnick A, Levine RL, Ferrando A, Mackerell AD Jr, Kelleher NL, Licht JD,
Popovic R (2014) Point mutation E1099K in MMSET/NSD2 enhances its methyltransferase
activity and leads to altered global chromatin methylation in lymphoid malignancies. Leukemia 28(1):198–201. https://doi.org/10.1038/leu.2013.204
194. Yang ZQ, Liu G, Bollig-Fischer A, Giroux CN, Ethier SP (2010) Transforming properties
of 8p11-12 amplified genes in human breast cancer. Cancer Res 70(21):8487–8497. https://
doi.org/10.1158/0008-5472.CAN-10-1013
195. Morrison MJ, Boriack-Sjodin PA, Swinger KK, Wigle TJ, Sadalge D, Kuntz KW, Scott MP,
Janzen WP, Chesworth R, Duncan KW, Harvey DM, Lampe JW, Mitchell LH, Copeland RA
(2018) Identification of a peptide inhibitor for the histone methyltransferase WHSC1.
PLoS One 13(5):e0197082. https://doi.org/10.1371/journal.pone.0197082
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Biol 33:135–141. https://doi.org/10.1016/j.cbpa.2016.06.004
182. Camerino MA, Zhong N, Dong A, Dickson BM, James LI, Baughman BM, Norris JL,
Kireev DB, Janzen WP, Arrowsmith CH, Frye SV (2013) The structure-activity relationships
of L3MBTL3 inhibitors: flexibility of the dimer interface. MedChemComm 4(11):1501–1507.
https://doi.org/10.1039/C3MD00197K
183. Stec I, Nagl SB, van Ommen GJ, den Dunnen JT (2000) The PWWP domain: a potential
protein-protein interaction domain in nuclear proteins influencing differentiation? FEBS Lett
473(1):1–5. https://doi.org/10.1016/S0014-5793(00)01449-6
184. Wu H, Zeng H, Lam R, Tempel W, Amaya MF, Xu C, Dombrovski L, Qiu W, Wang Y, Min J
(2011) Structural and histone binding ability characterizations of human PWWP domains.
PLoS One 6(6):e18919. https://doi.org/10.1371/journal.pone.0018919
185. Qin S, Min J (2014) Structure and function of the nucleosome-binding PWWP domain. Trends
Biochem Sci 39(11):536–547. https://doi.org/10.1016/j.tibs.2014.09.001
186. Wang Y, Reddy B, Thompson J, Wang H, Noma K, Yates JR 3rd, Jia S (2009) Regulation of
Set9-mediated H4K20 methylation by a PWWP domain protein. Mol Cell 33(4):428–437.
https://doi.org/10.1016/j.molcel.2009.02.002
187. Dhayalan A, Rajavelu A, Rathert P, Tamas R, Jurkowska RZ, Ragozin S, Jeltsch A (2010)
The Dnmt3a PWWP domain reads histone 3 lysine 36 trimethylation and guides DNA
methylation. J Biol Chem 285(34):26114–26120. https://doi.org/10.1074/jbc.M109.089433
188. Vezzoli A, Bonadies N, Allen MD, Freund SM, Santiveri CM, Kvinlaug BT, Huntly BJ,
Gottgens B, Bycroft M (2010) Molecular basis of histone H3K36me3 recognition by the
PWWP domain of Brpf1. Nat Struct Mol Biol 17(5):617–619. https://doi.org/10.1038/nsmb.
1797
189. Huang Z, Wu H, Chuai S, Xu F, Yan F, Englund N, Wang Z, Zhang H, Fang M, Wang Y,
Gu J, Zhang M, Yang T, Zhao K, Yu Y, Dai J, Yi W, Zhou S, Li Q, Wu J, Liu J, Wu X,
Chan H, Lu C, Atadja P, Li E, Wang Y, Hu M (2013) NSD2 is recruited through its PHD
domain to oncogenic gene loci to drive multiple myeloma. Cancer Res 73(20):6277–6288.
https://doi.org/10.1158/0008-5472.CAN-13-1000
190. Hudlebusch HR, Santoni-Rugiu E, Simon R, Ralfkiaer E, Rossing HH, Johansen JV,
Jorgensen M, Sauter G, Helin K (2011) The histone methyltransferase and putative
oncoprotein MMSET is overexpressed in a large variety of human tumors. Clin Cancer Res
17(9):2919–2933. https://doi.org/10.1158/1078-0432.CCR-10-1302
191. Li J, Yin C, Okamoto H, Mushlin H, Balgley BM, Lee CS, Yuan K, Ikejiri B, Glasker S,
Vortmeyer AO, Oldfield EH, Weil RJ, Zhuang Z (2008) Identification of a novel proliferationrelated protein, WHSC1 4a, in human gliomas. Neuro Oncol 10(1):45–51. https://doi.org/10.
1215/15228517-2007-036
192. Kassambara A, Klein B, Moreaux J (2009) MMSET is overexpressed in cancers: link with
tumor aggressiveness. Biochem Biophys Res Commun 379(4):840–845. https://doi.org/10.
1016/j.bbrc.2008.12.093
193. Oyer JA, Huang X, Zheng Y, Shim J, Ezponda T, Carpenter Z, Allegretta M, Okot-Kotber CI,
Patel JP, Melnick A, Levine RL, Ferrando A, Mackerell AD Jr, Kelleher NL, Licht JD,
Popovic R (2014) Point mutation E1099K in MMSET/NSD2 enhances its methyltransferase
activity and leads to altered global chromatin methylation in lymphoid malignancies. Leukemia 28(1):198–201. https://doi.org/10.1038/leu.2013.204
194. Yang ZQ, Liu G, Bollig-Fischer A, Giroux CN, Ethier SP (2010) Transforming properties
of 8p11-12 amplified genes in human breast cancer. Cancer Res 70(21):8487–8497. https://
doi.org/10.1158/0008-5472.CAN-10-1013
195. Morrison MJ, Boriack-Sjodin PA, Swinger KK, Wigle TJ, Sadalge D, Kuntz KW, Scott MP,
Janzen WP, Chesworth R, Duncan KW, Harvey DM, Lampe JW, Mitchell LH, Copeland RA
(2018) Identification of a peptide inhibitor for the histone methyltransferase WHSC1.
PLoS One 13(5):e0197082. https://doi.org/10.1371/journal.pone.0197082
Methyl-Readers and Inhibitors
395