60. Mathioudaki K et al (2008) The PRMT1 gene expression pattern in colon cancer. Br J Cancer
99:2094–2099
61. Papadokostopoulou A et al (2009) Colon cancer and protein arginine methyltransferase 1 gene
expression. Anticancer Res 29:1361–1366
62. Chuang C et al (2017) PRMT1 expression is elevated in head and neck cancer and inhibition of
protein arginine methylation by adenosine dialdehyde or PRMT1 knockdown downregulates
proliferation and migration of oral cancer cells. Oncol Rep 38:1115–1123
63. Yoshimatsu M et al (2011) Dysregulation of PRMT1 and PRMT6, type I arginine
methyltransferases, is involved in various types of human cancers. Int J Cancer 128:562–573
64. Cheung N et al (2007) Protein arginine-methyltransferase-dependent oncogenesis. Nat Cell
Biol 9:1208–1215
65. Shia W-J et al (2012) PRMT1 interacts with AML1-ETO to promote its transcriptional
activation and progenitor cell proliferative potential. Blood 119:4953–4962
66. Sun Q et al (2015) PRMT1 upregulated by epithelial Proinflammatory cytokines participates in
COX2 expression in fibroblasts and chronic antigen-induced pulmonary inflammation.
J Immunol 195:298–306
67. Iwasaki H (2009) Impaired PRMT1 activity in the liver and pancreas of type 2 diabetic GotoKakizaki rats. Life Sci 85:161–166
68. Li Y et al (2015) Arginine methyltransferase 1 in the nucleus Accumbens regulates behavioral
effects of cocaine. J Neurosci 35:12890–12902
69. Ragno R et al (2007) Small molecule inhibitors of histone arginine methyltransferases:
homology modeling, molecular docking, binding mode analysis, and biological evaluations.
J Med Chem 50:1241–1253
70. Mai A et al (2008) Epigenetic multiple ligands: mixed histone/protein methyltransferase,
acetyltransferase, and class III deacetylase (Sirtuin) inhibitors. J Med Chem 51:2279–2290
71. Feng Y et al (2010) Discovery and mechanistic study of a class of protein arginine methylation
inhibitors. J Med Chem 53:6028–6039
72. Wang J et al (2012) Pharmacophore-based virtual screening and biological evaluation of small
molecule inhibitors for protein arginine methylation. J Med Chem 55:7978–7987
73. Bonham K et al (2010) Effects of a novel arginine methyltransferase inhibitor on T-helper cell
cytokine production. FEBS J 277:2096–2108
74. Spannhoff A et al (2007) Target-based approach to inhibitors of histone arginine
methyltransferases. J Med Chem 50:2319–2325
75. Bissinger E-M et al (2011) Acyl derivatives of p-aminosulfonamides and dapsone as new
inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem 19:3717–3731
76. Spannhoff A et al (2007) A novel arginine methyltransferase inhibitor with cellular activity.
Bioorg Med Chem Lett 17:4150–4153
77. Heinke R et al (2009) Virtual screening and biological characterization of novel histone
arginine methyltransferase PRMT1 inhibitors. ChemMedChem 4:69–77
78. Xie Y et al (2014) Virtual screening and biological evaluation of novel small molecular
inhibitors against protein arginine methyltransferase 1 (PRMT1). Org Biomol Chem
12:9665–9673
79. Dowden J et al (2010) Toward the development of potent and selective bisubstrate inhibitors of
protein arginine methyltransferases. Bioorg Med Chem Lett 20:2103–2105
80. Dowden J et al (2011) Small molecule inhibitors that discriminate between protein arginine
N-methyltransferases PRMT1 and CARM1. Org Biomol Chem 9:7814
81. Lakowski TM et al (2010) Nη-substituted Arginyl peptide inhibitors of protein arginine
N-methyltransferases. ACS Chem Biol 5:1053–1063
82. ’t Hart P et al (2011) Peptidic partial bisubstrates as inhibitors of the protein arginine
N-methyltransferases. Chembiochem 12:1427–1432
83. ’t Hart P et al (2012) Analogues of the HIV-Tat peptide containing Nη-modified arginines as
potent inhibitors of protein arginine N-methyltransferases. Med Chem Commun 3:1235–1244
PRMT Inhibitors
191
99:2094–2099
61. Papadokostopoulou A et al (2009) Colon cancer and protein arginine methyltransferase 1 gene
expression. Anticancer Res 29:1361–1366
62. Chuang C et al (2017) PRMT1 expression is elevated in head and neck cancer and inhibition of
protein arginine methylation by adenosine dialdehyde or PRMT1 knockdown downregulates
proliferation and migration of oral cancer cells. Oncol Rep 38:1115–1123
63. Yoshimatsu M et al (2011) Dysregulation of PRMT1 and PRMT6, type I arginine
methyltransferases, is involved in various types of human cancers. Int J Cancer 128:562–573
64. Cheung N et al (2007) Protein arginine-methyltransferase-dependent oncogenesis. Nat Cell
Biol 9:1208–1215
65. Shia W-J et al (2012) PRMT1 interacts with AML1-ETO to promote its transcriptional
activation and progenitor cell proliferative potential. Blood 119:4953–4962
66. Sun Q et al (2015) PRMT1 upregulated by epithelial Proinflammatory cytokines participates in
COX2 expression in fibroblasts and chronic antigen-induced pulmonary inflammation.
J Immunol 195:298–306
67. Iwasaki H (2009) Impaired PRMT1 activity in the liver and pancreas of type 2 diabetic GotoKakizaki rats. Life Sci 85:161–166
68. Li Y et al (2015) Arginine methyltransferase 1 in the nucleus Accumbens regulates behavioral
effects of cocaine. J Neurosci 35:12890–12902
69. Ragno R et al (2007) Small molecule inhibitors of histone arginine methyltransferases:
homology modeling, molecular docking, binding mode analysis, and biological evaluations.
J Med Chem 50:1241–1253
70. Mai A et al (2008) Epigenetic multiple ligands: mixed histone/protein methyltransferase,
acetyltransferase, and class III deacetylase (Sirtuin) inhibitors. J Med Chem 51:2279–2290
71. Feng Y et al (2010) Discovery and mechanistic study of a class of protein arginine methylation
inhibitors. J Med Chem 53:6028–6039
72. Wang J et al (2012) Pharmacophore-based virtual screening and biological evaluation of small
molecule inhibitors for protein arginine methylation. J Med Chem 55:7978–7987
73. Bonham K et al (2010) Effects of a novel arginine methyltransferase inhibitor on T-helper cell
cytokine production. FEBS J 277:2096–2108
74. Spannhoff A et al (2007) Target-based approach to inhibitors of histone arginine
methyltransferases. J Med Chem 50:2319–2325
75. Bissinger E-M et al (2011) Acyl derivatives of p-aminosulfonamides and dapsone as new
inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem 19:3717–3731
76. Spannhoff A et al (2007) A novel arginine methyltransferase inhibitor with cellular activity.
Bioorg Med Chem Lett 17:4150–4153
77. Heinke R et al (2009) Virtual screening and biological characterization of novel histone
arginine methyltransferase PRMT1 inhibitors. ChemMedChem 4:69–77
78. Xie Y et al (2014) Virtual screening and biological evaluation of novel small molecular
inhibitors against protein arginine methyltransferase 1 (PRMT1). Org Biomol Chem
12:9665–9673
79. Dowden J et al (2010) Toward the development of potent and selective bisubstrate inhibitors of
protein arginine methyltransferases. Bioorg Med Chem Lett 20:2103–2105
80. Dowden J et al (2011) Small molecule inhibitors that discriminate between protein arginine
N-methyltransferases PRMT1 and CARM1. Org Biomol Chem 9:7814
81. Lakowski TM et al (2010) Nη-substituted Arginyl peptide inhibitors of protein arginine
N-methyltransferases. ACS Chem Biol 5:1053–1063
82. ’t Hart P et al (2011) Peptidic partial bisubstrates as inhibitors of the protein arginine
N-methyltransferases. Chembiochem 12:1427–1432
83. ’t Hart P et al (2012) Analogues of the HIV-Tat peptide containing Nη-modified arginines as
potent inhibitors of protein arginine N-methyltransferases. Med Chem Commun 3:1235–1244
PRMT Inhibitors
191