Methyllysine reader proteins bind to methylated proteins, such as histones, allowing regulation of gene expression.

* Key recommended reading is highlighted with an asterisk

* Barghout SH, Machado RAC, Barsyte-Lovejoy D. (2022) Chemical biology and pharmacology of histone lysine methylation inhibitors. Biochim Biophys Acta Gene Regul Mech, 1865 (6): 194840. [PMID:35753676]

Daskalaki MG, Tsatsanis C, Kampranis SC. (2018) Histone methylation and acetylation in macrophages as a mechanism for regulation of inflammatory responses. J Cell Physiol, 233 (9): 6495-6507. [PMID:29574768]

* Furuya K, Ikura M, Ikura T. (2019) Epigenetic interplays between DNA demethylation and histone methylation for protecting oncogenesis. J Biochem, 165 (4): 297-299. [PMID:30605533]

* Levy D. (2019) Lysine methylation signaling of non-histone proteins in the nucleus. Cell Mol Life Sci, 76 (15): 2873-2883. [PMID:31123776]

* Li J, Ahn JH, Wang GG. (2019) Understanding histone H3 lysine 36 methylation and its deregulation in disease. Cell Mol Life Sci, 76 (15): 2899-2916. [PMID:31147750]

Liu K, Liu Y, Lau JL, Min J. (2015) Epigenetic targets and drug discovery Part 2: Histone demethylation and DNA methylation. Pharmacol Ther, 151: 121-40. [PMID:25857453]

Milosevich N, Hof F. (2016) Chemical Inhibitors of Epigenetic Methyllysine Reader Proteins. Biochemistry, 55 (11): 1570-83. [PMID:26650180]

Musselman CA, Khorasanizadeh S, Kutateladze TG. (2014) Towards understanding methyllysine readout. Biochim Biophys Acta, 1839 (8): 686-93. [PMID:24727128]

Sadakierska-Chudy A, Kostrzewa RM, Filip M. (2015) A comprehensive view of the epigenetic landscape part I: DNA methylation, passive and active DNA demethylation pathways and histone variants. Neurotox Res, 27 (1): 84-97. [PMID:25362550]

* Shafabakhsh R, Aghadavod E, Ghayour-Mobarhan M, Ferns G, Asemi Z. (2019) Role of histone modification and DNA methylation in signaling pathways involved in diabetic retinopathy. J Cell Physiol, 234 (6): 7839-7846. [PMID:30515789]

Teske KA, Hadden MK. (2017) Methyllysine binding domains: Structural insight and small molecule probe development. Eur J Med Chem, 136: 14-35. [PMID:28478342]

Thinnes CC, England KS, Kawamura A, Chowdhury R, Schofield CJ, Hopkinson RJ. (2014) Targeting histone lysine demethylases - progress, challenges, and the future. Biochim Biophys Acta, 1839 (12): 1416-32. [PMID:24859458]

Zahnow CA, Topper M, Stone M, Murray-Stewart T, Li H, Baylin SB, Casero Jr RA. (2016) Inhibitors of DNA Methylation, Histone Deacetylation, and Histone Demethylation: A Perfect Combination for Cancer Therapy. Adv Cancer Res, 130: 55-111. [PMID:27037751]

1. James LI, Barsyte-Lovejoy D, Zhong N, Krichevsky L, Korboukh VK, Herold JM, MacNevin CJ, Norris JL, Sagum CA, Tempel W et al.. (2013) Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol, 9 (3): 184-91. [PMID:23292653]

2. Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini M, Fagan V, Li F et al.. (2019) Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). J Med Chem, 62 (20): 8996-9007. [PMID:31260300]

3. Xiong Y, Greschik H, Johansson C, Seifert L, Gamble V, Park KS, Fagan V, Li F, Chau I, Vedadi M et al.. (2024) Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor. J Med Chem, 67 (7): 5837-5853. [PMID:38533580]