Target type: molecularfunction
Catalysis of the reaction: L-lysyl79-[histone H3] + 3 S-adenosyl-L-methionine = 3 H+ + N6,N6,N6-trimethyl-L-lysyl79-[histone H3] + 3 S-adenosyl-L-homocysteine. This reaction is the successive addition of up to three methyl group to the lysine residue at position 79 of the histone H3 protein, producing H3K79me3. [PMID:15371351, RHEA:60328]
Histone H3K79 trimethyltransferase activity is a molecular function that refers to the enzymatic activity of proteins that catalyze the transfer of three methyl groups to lysine 79 (K79) of histone H3. This process is known as trimethylation and is a critical epigenetic modification that plays a vital role in various cellular processes, including gene regulation, DNA replication, and DNA repair.
Histone H3K79 trimethylation is typically associated with active transcription, although its precise role can vary depending on the specific gene and cellular context. It is often found at promoters and enhancers of actively transcribed genes, where it contributes to the recruitment of transcription factors and the formation of euchromatin, a less condensed state of chromatin that allows for efficient gene expression.
The enzymes responsible for histone H3K79 trimethylation are known as histone H3K79 methyltransferases (DOT1L in humans). DOT1L is a highly conserved protein that specifically recognizes and methylates histone H3 at lysine 79. It possesses a unique catalytic domain that differs from other histone methyltransferases and requires S-adenosyl-L-methionine (SAM) as a methyl donor.
Disruptions in histone H3K79 trimethylation have been implicated in various human diseases, including cancer. For example, DOT1L is often overexpressed in leukemia, and its inhibition has been shown to have therapeutic potential.
Overall, histone H3K79 trimethyltransferase activity is an essential epigenetic mark that regulates gene expression and other cellular processes. Its deregulation can contribute to disease development, highlighting its significance in maintaining cellular homeostasis.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Histone-lysine N-methyltransferase, H3 lysine-79 specific | A histone-lysine N-methyltransferase, H3 lysine-79 specific that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8TEK3] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| toyocamycin | toyocamycin : An N-glycosylpyrrolopyrimidine that is tubercidin in which the hydrogen at position 5 of the pyrrolopyrimidine moiety has been replaced by a cyano group. Toyocamycin: 4-Amino-5-cyano-7-(D-ribofuranosyl)-7H- pyrrolo(2,3-d)pyrimidine. Antibiotic antimetabolite isolated from Streptomyces toyocaensis cultures. It is an analog of adenosine, blocks RNA synthesis and ribosome function, and is used mainly as a tool in biochemistry. | antibiotic antifungal agent; N-glycosylpyrrolopyrimidine; nitrile; ribonucleoside | antimetabolite; antineoplastic agent; apoptosis inducer; bacterial metabolite |
| nsc 65346 | sangivamycin : A nucleoside analogue that is adenosine in which the nitrogen at position 7 is replaced by a carbamoyl-substituted carbon. It is a potent inhibitor of protein kinase C. sangivamycin: RN given refers to parent cpd | nucleoside analogue | protein kinase inhibitor |
| adenosine | quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| sinefungin | adenosines; non-proteinogenic alpha-amino acid | antifungal agent; antimicrobial agent | |
| 5-iodotubercidin | 7-iodotubercidin: inhibits Toxoplasma gondii adenosine kinase | organoiodine compound | |
| s-adenosyl-3-thiopropylamine | S-adenosyl-3-thiopropylamine : A thioadenosine that is adenosine in which the hydroxy group at C-5' is replaced by a 3-aminopropyl group. S-adenosyl-3-thiopropylamine: decarboxylated S-adenosylhomocysteine; RN given refers to parent cpd | organic sulfide; primary amino compound; thioadenosine | |
| s-adenosylhomocysteine | S-adenosyl-L-homocysteine : An organic sulfide that is the S-adenosyl derivative of L-homocysteine. S-Adenosylhomocysteine: 5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions. | adenosines; amino acid zwitterion; homocysteine derivative; homocysteines; organic sulfide | cofactor; EC 2.1.1.72 [site-specific DNA-methyltransferase (adenine-specific)] inhibitor; EC 2.1.1.79 (cyclopropane-fatty-acyl-phospholipid synthase) inhibitor; epitope; fundamental metabolite |
| epz004777 | N-glycosyl compound | ||
| epz-5676 | 5'-deoxyribonucleoside | ||
| gsk343 | GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM). GSK343: an EZH2 methyltransferase inhibitor | aminopyridine; indazoles; N-alkylpiperazine; N-arylpiperazine; pyridone; secondary carboxamide | antineoplastic agent; apoptosis inducer; EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor |
| 6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine | 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine: a SETD8 inhibitor; structure in first source |