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169. Boccuni P, MacGrogan D, Scandura JM, Nimer SD (2003) The human L(3)MBT polycomb
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170. Trojer P, Li G, Sims 3rd RJ, Vaquero A, Kalakonda N, Boccuni P, Lee D,
Erdjument-Bromage H, Tempst P, Nimer SD, Wang YH, Reinberg D (2007) L3MBTL1,
a histone-methylation-dependent chromatin lock. Cell 129(5):915–928. https://doi.org/10.
1016/j.cell.2007.03.048
171. Herold JM, Ingerman LA, Gao C, Frye SV (2011) Drug discovery toward antagonists of
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172. Northcott PA, Nakahara Y, Wu X, Feuk L, Ellison DW, Croul S, Mack S, Kongkham PN,
Peacock J, Dubuc A, Ra YS, Zilberberg K, McLeod J, Scherer SW, Sunil Rao J, Eberhart CG,
Grajkowska W, Gillespie Y, Lach B, Grundy R, Pollack IF, Hamilton RL, Van Meter T,
Carlotti CG, Boop F, Bigner D, Gilbertson RJ, Rutka JT, Taylor MD (2009) Multiple recurrent
genetic events converge on control of histone lysine methylation in medulloblastoma.
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173. MacGrogan D, Kalakonda N, Alvarez S, Scandura JM, Boccuni P, Johansson B, Nimer SD
(2004) Structural integrity and expression of the L3MBTL gene in normal and malignant
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174. Wigle TJ, Herold JM, Senisterra GA, Vedadi M, Kireev DB, Arrowsmith CH, Frye SV,
Janzen WP (2010) Screening for inhibitors of low-affinity epigenetic peptide-protein
interactions: an AlphaScreen-based assay for antagonists of methyl-lysine binding proteins.
J Biomol Screen 15(1):62–71. https://doi.org/10.1177/1087057109352902
175. Kireev D, Wigle TJ, Norris-Drouin J, Herold JM, Janzen WP, Frye SV (2010) Identification
of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of
commercially available compounds. J Med Chem 53(21):7625–7631. https://doi.org/10.
1021/jm1007374
176. Herold JM, Wigle TJ, Norris JL, Lam R, Korboukh VK, Gao C, Ingerman LA, Kireev DB,
Senisterra G, Vedadi M, Tripathy A, Brown PJ, Arrowsmith CH, Jin J, Janzen WP,
Frye SV (2011) Small-molecule ligands of methyl-lysine binding proteins. J Med Chem
54(7):2504–2511. https://doi.org/10.1021/jm200045v
177. Herold JM, James LI, Korboukh VK, Gao C, Coil KE, Bua DJ, Norris JL, Kireev DB,
Brown PJ, Jin J, Janzen WP, Gozani O, Frye SV (2012) Structure-activity relationships
of methyl-lysine reader antagonists. MedChemComm 3(1):45–51. https://doi.org/10.1039/
C1MD00195G
178. James LI, Barsyte-Lovejoy D, Zhong N, Krichevsky L, Korboukh VK, Herold JM,
MacNevin CJ, Norris JL, Sagum CA, Tempel W, Marcon E, Guo H, Gao C, Huang XP,
Duan S, Emili A, Greenblatt JF, Kireev DB, Jin J, Janzen WP, Brown PJ, Bedford MT,
Arrowsmith CH, Frye SV (2013) Discovery of a chemical probe for the L3MBTL3
methyllysine reader domain. Nat Chem Biol 9(3):184–191. https://doi.org/10.1038/
nchembio.1157
179. James LI, Korboukh VK, Krichevsky L, Baughman BM, Herold JM, Norris JL, Jin J,
Kireev DB, Janzen WP, Arrowsmith CH, Frye SV (2013) Small-molecule ligands of
methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem
56(18):7358–7371. https://doi.org/10.1021/jm400919p
180. Lee YY, Yu YB, Gunawardena HP, Xie L, Chen X (2012) BCLAF1 is a radiation-induced
H2AX-interacting partner involved in γH2AX-mediated regulation of apoptosis and DNA
repair. Cell Death Dis 3:e359. https://doi.org/10.1038/cddis.2012.76
394
G. Sbardella
Polycomb protein SCML2 regulates the cell cycle by binding and modulating CDK/CYCLIN/
p21 complexes. PLoS Biol 11(12):e1001737. https://doi.org/10.1371/journal.pbio.1001737
169. Boccuni P, MacGrogan D, Scandura JM, Nimer SD (2003) The human L(3)MBT polycomb
group protein is a transcriptional repressor and interacts physically and functionally with
TEL (ETV6). J Biol Chem 278(17):15412–15420. https://doi.org/10.1074/jbc.M300592200
170. Trojer P, Li G, Sims 3rd RJ, Vaquero A, Kalakonda N, Boccuni P, Lee D,
Erdjument-Bromage H, Tempst P, Nimer SD, Wang YH, Reinberg D (2007) L3MBTL1,
a histone-methylation-dependent chromatin lock. Cell 129(5):915–928. https://doi.org/10.
1016/j.cell.2007.03.048
171. Herold JM, Ingerman LA, Gao C, Frye SV (2011) Drug discovery toward antagonists of
methyl-lysine binding proteins. Curr Chem Genomics 5:51–61. https://doi.org/10.2174/
1875397301005010051
172. Northcott PA, Nakahara Y, Wu X, Feuk L, Ellison DW, Croul S, Mack S, Kongkham PN,
Peacock J, Dubuc A, Ra YS, Zilberberg K, McLeod J, Scherer SW, Sunil Rao J, Eberhart CG,
Grajkowska W, Gillespie Y, Lach B, Grundy R, Pollack IF, Hamilton RL, Van Meter T,
Carlotti CG, Boop F, Bigner D, Gilbertson RJ, Rutka JT, Taylor MD (2009) Multiple recurrent
genetic events converge on control of histone lysine methylation in medulloblastoma.
Nat Genet 41(4):465–472. https://doi.org/10.1038/ng.336
173. MacGrogan D, Kalakonda N, Alvarez S, Scandura JM, Boccuni P, Johansson B, Nimer SD
(2004) Structural integrity and expression of the L3MBTL gene in normal and malignant
hematopoietic cells. Genes Chromosomes Cancer 41(3):203–213. https://doi.org/10.1002/gcc.
20087
174. Wigle TJ, Herold JM, Senisterra GA, Vedadi M, Kireev DB, Arrowsmith CH, Frye SV,
Janzen WP (2010) Screening for inhibitors of low-affinity epigenetic peptide-protein
interactions: an AlphaScreen-based assay for antagonists of methyl-lysine binding proteins.
J Biomol Screen 15(1):62–71. https://doi.org/10.1177/1087057109352902
175. Kireev D, Wigle TJ, Norris-Drouin J, Herold JM, Janzen WP, Frye SV (2010) Identification
of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of
commercially available compounds. J Med Chem 53(21):7625–7631. https://doi.org/10.
1021/jm1007374
176. Herold JM, Wigle TJ, Norris JL, Lam R, Korboukh VK, Gao C, Ingerman LA, Kireev DB,
Senisterra G, Vedadi M, Tripathy A, Brown PJ, Arrowsmith CH, Jin J, Janzen WP,
Frye SV (2011) Small-molecule ligands of methyl-lysine binding proteins. J Med Chem
54(7):2504–2511. https://doi.org/10.1021/jm200045v
177. Herold JM, James LI, Korboukh VK, Gao C, Coil KE, Bua DJ, Norris JL, Kireev DB,
Brown PJ, Jin J, Janzen WP, Gozani O, Frye SV (2012) Structure-activity relationships
of methyl-lysine reader antagonists. MedChemComm 3(1):45–51. https://doi.org/10.1039/
C1MD00195G
178. James LI, Barsyte-Lovejoy D, Zhong N, Krichevsky L, Korboukh VK, Herold JM,
MacNevin CJ, Norris JL, Sagum CA, Tempel W, Marcon E, Guo H, Gao C, Huang XP,
Duan S, Emili A, Greenblatt JF, Kireev DB, Jin J, Janzen WP, Brown PJ, Bedford MT,
Arrowsmith CH, Frye SV (2013) Discovery of a chemical probe for the L3MBTL3
methyllysine reader domain. Nat Chem Biol 9(3):184–191. https://doi.org/10.1038/
nchembio.1157
179. James LI, Korboukh VK, Krichevsky L, Baughman BM, Herold JM, Norris JL, Jin J,
Kireev DB, Janzen WP, Arrowsmith CH, Frye SV (2013) Small-molecule ligands of
methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem
56(18):7358–7371. https://doi.org/10.1021/jm400919p
180. Lee YY, Yu YB, Gunawardena HP, Xie L, Chen X (2012) BCLAF1 is a radiation-induced
H2AX-interacting partner involved in γH2AX-mediated regulation of apoptosis and DNA
repair. Cell Death Dis 3:e359. https://doi.org/10.1038/cddis.2012.76
394
G. Sbardella