79. Pallante P, Federico A, Berlingieri MT, Bianco M, Ferraro A, Forzati F, Iaccarino A, Russo M,
Pierantoni GM, Leone V, Sacchetti S, Troncone G, Santoro M, Fusco A (2008) Loss of the
CBX7 gene expression correlates with a highly malignant phenotype in thyroid cancer. Cancer
Res 68(16):6770–6778. https://doi.org/10.1158/0008-5472.CAN-08-0695
80. Federico A, Pallante P, Bianco M, Ferraro A, Esposito F, Monti M, Cozzolino M, Keller S,
Fedele M, Leone V, Troncone G, Chiariotti L, Pucci P, Fusco A (2009) Chromobox protein
homologue 7 protein, with decreased expression in human carcinomas, positively regulates
E-cadherin expression by interacting with the histone deacetylase 2 protein. Cancer Res
69(17):7079–7087. https://doi.org/10.1158/0008-5472.CAN-09-1542
81. Traore M, Gignac M, Doan ND, Hof F, Lubell WD (2017) Aza-amino acid scanning
of chromobox homolog 7 (CBX7) ligands. J Pept Sci 23(4):266–271. https://doi.org/10.
1002/psc.2982
82. Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S,
Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G,
Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV
(2016) A cellular chemical probe targeting the chromodomains of Polycomb repressive
complex 1. Nat Chem Biol 12(3):180–187. https://doi.org/10.1038/nchembio.2007
83. Fischle W, Franz H, Jacobs SA, Allis CD, Khorasanizadeh S (2008) Specificity of the
chromodomain Y chromosome family of chromodomains for lysine-methylated ARK(S/T)
motifs. J Biol Chem 283(28):19626–19635. https://doi.org/10.1074/jbc.M802655200
84. Stuckey JI, Simpson C, Norris-Drouin JL, Cholensky SH, Lee J, Pasca R, Cheng N,
Dickson BM, Pearce KH, Frye SV, James LI (2016) Structure-activity relationships and
kinetic studies of peptidic antagonists of CBX chromodomains. J Med Chem 59
(19):8913–8923. https://doi.org/10.1021/acs.jmedchem.6b00801
85. Bernard D, Martinez-Leal JF, Rizzo S, Martinez D, Hudson D, Visakorpi T, Peters G,
Carnero A, Beach D, Gil J (2005) CBX7 controls the growth of normal and tumor-derived
prostate cells by repressing the Ink4a/Arf locus. Oncogene 24(36):5543–5551. https://doi.org/
10.1038/sj.onc.1208735
86. Barnash KD, Lamb KN, Stuckey JI, Norris JL, Cholensky SH, Kireev DB, Frye SV, James LI
(2016) Chromodomain ligand optimization via target-class directed combinatorial
repurposing. ACS Chem Biol 11(9):2475–2483. https://doi.org/10.1021/acschembio.6b00415
87. Astle JM, Simpson LS, Huang Y, Reddy MM, Wilson R, Connell S, Wilson J, Kodadek T
(2010) Seamless bead to microarray screening: rapid identification of the highest affinity
protein ligands from large combinatorial libraries. Chem Biol 17(1):38–45. https://doi.org/
10.1016/j.chembiol.2009.12.015
88. Mendes K, Ndungu JM, Clark LF, Kodadek T (2015) Optimization of the magnetic recovery
of hits from one-bead-one-compound library screens. ACS Comb Sci 17(9):506–517. https://
doi.org/10.1021/acscombsci.5b00090
89. Ren C, Morohashi K, Plotnikov AN, Jakoncic J, Smith SG, Li J, Zeng L, Rodriguez Y,
Stojanoff V, Walsh M, Zhou MM (2015) Small-molecule modulators of methyl-lysine binding
for the CBX7 chromodomain. Chem Biol 22(2):161–168. https://doi.org/10.1016/j.chembiol.
2014.11.021
90. Li H, Li H, Qu H, Zhao M, Yuan B, Cao M, Cui J (2015) Suramin inhibits cell proliferation in
ovarian and cervical cancer by downregulating heparanase expression. Cancer Cell Int 15
(1):52. https://doi.org/10.1186/s12935-015-0196-y
91. Morgan HP, McNae IW, Nowicki MW, Zhong W, Michels PA, Auld DS, Fothergill-Gilmore
LA, Walkinshaw MD (2011) The trypanocidal drug suramin and other trypan blue
mimetics are inhibitors of pyruvate kinases and bind to the adenosine site. J Biol Chem
286(36):31232–31240. https://doi.org/10.1074/jbc.M110.212613
92. Ragno R, Simeoni S, Castellano S, Vicidomini C, Mai A, Caroli A, Tramontano A,
Bonaccini C, Trojer P, Bauer I, Brosch G, Sbardella G (2007) Small molecule inhibitors of
histone arginine methyltransferases: homology modeling, molecular docking, binding mode
388
G. Sbardella
Pierantoni GM, Leone V, Sacchetti S, Troncone G, Santoro M, Fusco A (2008) Loss of the
CBX7 gene expression correlates with a highly malignant phenotype in thyroid cancer. Cancer
Res 68(16):6770–6778. https://doi.org/10.1158/0008-5472.CAN-08-0695
80. Federico A, Pallante P, Bianco M, Ferraro A, Esposito F, Monti M, Cozzolino M, Keller S,
Fedele M, Leone V, Troncone G, Chiariotti L, Pucci P, Fusco A (2009) Chromobox protein
homologue 7 protein, with decreased expression in human carcinomas, positively regulates
E-cadherin expression by interacting with the histone deacetylase 2 protein. Cancer Res
69(17):7079–7087. https://doi.org/10.1158/0008-5472.CAN-09-1542
81. Traore M, Gignac M, Doan ND, Hof F, Lubell WD (2017) Aza-amino acid scanning
of chromobox homolog 7 (CBX7) ligands. J Pept Sci 23(4):266–271. https://doi.org/10.
1002/psc.2982
82. Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S,
Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G,
Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV
(2016) A cellular chemical probe targeting the chromodomains of Polycomb repressive
complex 1. Nat Chem Biol 12(3):180–187. https://doi.org/10.1038/nchembio.2007
83. Fischle W, Franz H, Jacobs SA, Allis CD, Khorasanizadeh S (2008) Specificity of the
chromodomain Y chromosome family of chromodomains for lysine-methylated ARK(S/T)
motifs. J Biol Chem 283(28):19626–19635. https://doi.org/10.1074/jbc.M802655200
84. Stuckey JI, Simpson C, Norris-Drouin JL, Cholensky SH, Lee J, Pasca R, Cheng N,
Dickson BM, Pearce KH, Frye SV, James LI (2016) Structure-activity relationships and
kinetic studies of peptidic antagonists of CBX chromodomains. J Med Chem 59
(19):8913–8923. https://doi.org/10.1021/acs.jmedchem.6b00801
85. Bernard D, Martinez-Leal JF, Rizzo S, Martinez D, Hudson D, Visakorpi T, Peters G,
Carnero A, Beach D, Gil J (2005) CBX7 controls the growth of normal and tumor-derived
prostate cells by repressing the Ink4a/Arf locus. Oncogene 24(36):5543–5551. https://doi.org/
10.1038/sj.onc.1208735
86. Barnash KD, Lamb KN, Stuckey JI, Norris JL, Cholensky SH, Kireev DB, Frye SV, James LI
(2016) Chromodomain ligand optimization via target-class directed combinatorial
repurposing. ACS Chem Biol 11(9):2475–2483. https://doi.org/10.1021/acschembio.6b00415
87. Astle JM, Simpson LS, Huang Y, Reddy MM, Wilson R, Connell S, Wilson J, Kodadek T
(2010) Seamless bead to microarray screening: rapid identification of the highest affinity
protein ligands from large combinatorial libraries. Chem Biol 17(1):38–45. https://doi.org/
10.1016/j.chembiol.2009.12.015
88. Mendes K, Ndungu JM, Clark LF, Kodadek T (2015) Optimization of the magnetic recovery
of hits from one-bead-one-compound library screens. ACS Comb Sci 17(9):506–517. https://
doi.org/10.1021/acscombsci.5b00090
89. Ren C, Morohashi K, Plotnikov AN, Jakoncic J, Smith SG, Li J, Zeng L, Rodriguez Y,
Stojanoff V, Walsh M, Zhou MM (2015) Small-molecule modulators of methyl-lysine binding
for the CBX7 chromodomain. Chem Biol 22(2):161–168. https://doi.org/10.1016/j.chembiol.
2014.11.021
90. Li H, Li H, Qu H, Zhao M, Yuan B, Cao M, Cui J (2015) Suramin inhibits cell proliferation in
ovarian and cervical cancer by downregulating heparanase expression. Cancer Cell Int 15
(1):52. https://doi.org/10.1186/s12935-015-0196-y
91. Morgan HP, McNae IW, Nowicki MW, Zhong W, Michels PA, Auld DS, Fothergill-Gilmore
LA, Walkinshaw MD (2011) The trypanocidal drug suramin and other trypan blue
mimetics are inhibitors of pyruvate kinases and bind to the adenosine site. J Biol Chem
286(36):31232–31240. https://doi.org/10.1074/jbc.M110.212613
92. Ragno R, Simeoni S, Castellano S, Vicidomini C, Mai A, Caroli A, Tramontano A,
Bonaccini C, Trojer P, Bauer I, Brosch G, Sbardella G (2007) Small molecule inhibitors of
histone arginine methyltransferases: homology modeling, molecular docking, binding mode
388
G. Sbardella