Covalent modifications of histone tails have fundamental roles in chromatin structure and function. One such modification, lysine methylation, has important functions in many biological processes that include heterochromatin formation, X-chromosome inactivation and transcriptional regulation. The DNA within our cells exists in the form of chromatin. The basic building block of chromatin is the nucleosome, a structure consisting of an octamer of four core histone proteins around which 147 base pairs of DNA is wrapped. Core histones are subject to a large number of covalent modifications (PTMs: Post Translational Modifications) including acetylation, methylation, phosphorylation and ubiquitination. Histone methylation occurs on arginine and lysine residues and is catalyzed by enzymes belonging to three distinct families of proteins: the protein arginine specific methyl transferase (PRMT1) family, the SET-domain-containing protein family, and the non-SET-domain proteins DOT1/DOT1L. Unlike acetylation, which generally correlates with transcriptional activation, histone lysine methylation can signal either activation or repression, depending on the sites of methylation. Similar to the discovery that bromodomains can recognize acetylated lysines, studies on histone methylation identified at least three protein motifs (the Chromo-, the Tudor-, and the WD40-repeat domain) that are capable of forming specific interactions with methylated lysine residues of histone[1],[2].

Histone methyltransferases listed: HMTasePRMT

[1] C. Martin, Y. Zhang. The diverse functions of histone lysine methylation. Nat. Rev. Mol. Cell Biol. 2005, 6, 838-849.
[2] E.L. Greer, Y. Shi . Histone methylation: a dynamic mark in health, disease and inheritance. Nat. Rev. Genetics 2012,  13, 343-357

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Axon ID Name Description From price
2863 AMI-1 Inhibitor of PRMT €99.00
2210 C 7280948 Sulfone inhibitor of PRMT1 €85.00
2709 CMP5 Inhibitor of PRMT5 €95.00
2831 EPZ 015666 Potent, selective and orally available inhibitor of PRMT5 €125.00
2710 HLCL65 hydrochloride Inhibitor of PRMT5 €105.00
3681 MS023 dihydrochloride Potent, cell-active, and Type I selective PRMT inhibitor €90.00
3692 PF-06939999 dihydrochloride SAM competitive PRMT5 inhibitor Inquire
2211 PRMT3 inhibitor 1 Allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) €105.00
2625 SGC2085 Potent and selective CARM1 inhibitor (aka PRMT4) €120.00
2945 SGC707 First-in-class, potent, selective and cell-active allosteric inhibitor of PRMT3 €90.00

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