177. Limm K et al (2013) Deregulation of protein methylation in melanoma. Eur J Cancer
49:1305–1313
178. Mitchell LH et al (2015) Aryl Pyrazoles as potent inhibitors of arginine methyltransferases:
identification of the first PRMT6 tool compound. ACS Med Chem Lett 6:655–659
179. Wu H et al (2016) Structural basis of arginine asymmetrical dimethylation by PRMT6.
Biochem J 473:3049–3063
180. Feng Y et al (2013) Mammalian protein arginine methyltransferase 7 (PRMT7) specifically
targets RXR sites in lysine- and arginine-rich regions. J Biol Chem 288:37010–37025
181. Gonsalvez GB et al (2007) Two distinct arginine methyltransferases are required for biogenesis of Sm-class ribonucleoproteins. J Cell Biol 178:733–740
182. Debler EW et al (2016) A glutamate/aspartate switch controls product specificity in a protein
arginine methyltransferase. Proc Natl Acad Sci U S A 113:2068–2073
183. Jain K et al (2016) Protein arginine methyltransferase product specificity is mediated by
distinct active-site architectures. J Biol Chem 291:18299–18308
184. Yao R et al (2014) PRMT7 induces epithelial-to-mesenchymal transition and promotes
metastasis in breast cancer. Cancer Res 74:5656–5667
185. Baldwin RM et al (2015) Protein arginine methyltransferase 7 promotes breast cancer cell
invasion through the induction of MMP9 expression. Oncotarget 6:3013–3032
186. Karkhanis V et al (2012) Protein arginine methyltransferase 7 regulates cellular response to
DNA damage by methylating promoter histones H2A and H4 of the polymerase δ catalytic
subunit gene, POLD1. J Biol Chem 287:29801–29814
187. Ferreira TR et al (2014) Altered expression of an RBP-associated arginine methyltransferase
7 in Leishmania major affects parasite infection. Mol Microbiol 94:1085–1102
188. Gros L et al (2003) Identification of new drug sensitivity genes using genetic suppressor
elements: protein arginine N-methyltransferase mediates cell sensitivity to DNA-damaging
agents. Cancer Res 63:164–171
189. Gros L et al (2006) Characterization of prmt7α and β isozymes from Chinese hamster cells
sensitive and resistant to topoisomerase II inhibitors. Biochim Biophys Acta 1760:1646–1656
190. Verbiest V et al (2008) Protein arginine (N)-methyl transferase 7 (PRMT7) as a potential target
for the sensitization of tumor cells to camptothecins. FEBS Lett 582:1483–1489
191. Smil D et al (2015) Discovery of a dual PRMT5-PRMT7 inhibitor. ACS Med Chem Lett
6:408–412
192. Sayegh J et al (2007) Regulation of protein arginine methyltransferase 8 (PRMT8) activity by
its N-terminal domain. J Biol Chem 282:36444–36453
193. Kousaka A et al (2009) The distribution and characterization of endogenous protein arginine
N-methyltransferase 8 in mouse CNS. Neuroscience 163:1146–1157
194. Hernandez S, Dominko T (2016) Novel protein arginine methyltransferase 8 isoform is
essential for cell proliferation. J Cell Biochem 117:2056–2066
195. Scaramuzzino C et al (2013) Protein arginine methyltransferase 1 and 8 interact with FUS to
modify its sub-cellular distribution and toxicity in vitro and in vivo. PLoS One 8:e61576
196. Hernandez SJ et al (2017) PRMT8 demonstrates variant-specific expression in cancer cells and
correlates with patient survival in breast, ovarian and gastric cancer. Oncol Lett 13:1983–1989
197. Yang Y et al (2015) PRMT9 is a type II methyltransferase that methylates the splicing factor
SAP145. Nat Commun 6:6428
198. Gayatri S et al (2016) Using oriented peptide array libraries to evaluate methylargininespecific antibodies and arginine methyltransferase substrate motifs. Sci Rep 6:28718
199. ClinicalTrials.gov ID: NCT02783300. A phase I, open-label, dose escalation study to investigate the safety, pharmacokinetics, pharmacodynamics and clinical activity of GSK3326595
in subjects with solid tumors and non-Hodgkin’s Lymp. Accessed Jan 2019
196
M. J. van Haren and N. I. Martin
49:1305–1313
178. Mitchell LH et al (2015) Aryl Pyrazoles as potent inhibitors of arginine methyltransferases:
identification of the first PRMT6 tool compound. ACS Med Chem Lett 6:655–659
179. Wu H et al (2016) Structural basis of arginine asymmetrical dimethylation by PRMT6.
Biochem J 473:3049–3063
180. Feng Y et al (2013) Mammalian protein arginine methyltransferase 7 (PRMT7) specifically
targets RXR sites in lysine- and arginine-rich regions. J Biol Chem 288:37010–37025
181. Gonsalvez GB et al (2007) Two distinct arginine methyltransferases are required for biogenesis of Sm-class ribonucleoproteins. J Cell Biol 178:733–740
182. Debler EW et al (2016) A glutamate/aspartate switch controls product specificity in a protein
arginine methyltransferase. Proc Natl Acad Sci U S A 113:2068–2073
183. Jain K et al (2016) Protein arginine methyltransferase product specificity is mediated by
distinct active-site architectures. J Biol Chem 291:18299–18308
184. Yao R et al (2014) PRMT7 induces epithelial-to-mesenchymal transition and promotes
metastasis in breast cancer. Cancer Res 74:5656–5667
185. Baldwin RM et al (2015) Protein arginine methyltransferase 7 promotes breast cancer cell
invasion through the induction of MMP9 expression. Oncotarget 6:3013–3032
186. Karkhanis V et al (2012) Protein arginine methyltransferase 7 regulates cellular response to
DNA damage by methylating promoter histones H2A and H4 of the polymerase δ catalytic
subunit gene, POLD1. J Biol Chem 287:29801–29814
187. Ferreira TR et al (2014) Altered expression of an RBP-associated arginine methyltransferase
7 in Leishmania major affects parasite infection. Mol Microbiol 94:1085–1102
188. Gros L et al (2003) Identification of new drug sensitivity genes using genetic suppressor
elements: protein arginine N-methyltransferase mediates cell sensitivity to DNA-damaging
agents. Cancer Res 63:164–171
189. Gros L et al (2006) Characterization of prmt7α and β isozymes from Chinese hamster cells
sensitive and resistant to topoisomerase II inhibitors. Biochim Biophys Acta 1760:1646–1656
190. Verbiest V et al (2008) Protein arginine (N)-methyl transferase 7 (PRMT7) as a potential target
for the sensitization of tumor cells to camptothecins. FEBS Lett 582:1483–1489
191. Smil D et al (2015) Discovery of a dual PRMT5-PRMT7 inhibitor. ACS Med Chem Lett
6:408–412
192. Sayegh J et al (2007) Regulation of protein arginine methyltransferase 8 (PRMT8) activity by
its N-terminal domain. J Biol Chem 282:36444–36453
193. Kousaka A et al (2009) The distribution and characterization of endogenous protein arginine
N-methyltransferase 8 in mouse CNS. Neuroscience 163:1146–1157
194. Hernandez S, Dominko T (2016) Novel protein arginine methyltransferase 8 isoform is
essential for cell proliferation. J Cell Biochem 117:2056–2066
195. Scaramuzzino C et al (2013) Protein arginine methyltransferase 1 and 8 interact with FUS to
modify its sub-cellular distribution and toxicity in vitro and in vivo. PLoS One 8:e61576
196. Hernandez SJ et al (2017) PRMT8 demonstrates variant-specific expression in cancer cells and
correlates with patient survival in breast, ovarian and gastric cancer. Oncol Lett 13:1983–1989
197. Yang Y et al (2015) PRMT9 is a type II methyltransferase that methylates the splicing factor
SAP145. Nat Commun 6:6428
198. Gayatri S et al (2016) Using oriented peptide array libraries to evaluate methylargininespecific antibodies and arginine methyltransferase substrate motifs. Sci Rep 6:28718
199. ClinicalTrials.gov ID: NCT02783300. A phase I, open-label, dose escalation study to investigate the safety, pharmacokinetics, pharmacodynamics and clinical activity of GSK3326595
in subjects with solid tumors and non-Hodgkin’s Lymp. Accessed Jan 2019
196
M. J. van Haren and N. I. Martin