Page last updated: 2024-10-24
histone acetyltransferase activity
Definition
Target type: molecularfunction
Catalysis of the reaction: acetyl-CoA + histone = CoA + acetyl-histone. [EC:2.3.1.48]
Histone acetyltransferases (HATs) are a family of enzymes that catalyze the transfer of an acetyl group from acetyl coenzyme A (acetyl-CoA) to the ε-amino group of lysine residues on histone proteins. This process is known as histone acetylation. Histone acetylation is a key regulatory mechanism that influences gene expression by altering the accessibility of DNA to transcription factors.
Acetylation of histone lysine residues typically occurs at specific residues within the N-terminal tails of histones, particularly H3 and H4. When lysine residues are acetylated, they become less positively charged. This neutralization of positive charge weakens the interaction between histone tails and the negatively charged DNA, leading to a more relaxed chromatin structure. This relaxed structure allows for easier access of transcription factors and other regulatory proteins to the DNA, promoting gene transcription.
The molecular function of histone acetyltransferases is therefore to regulate gene expression by modifying the chromatin structure. HATs play a critical role in various cellular processes, including development, differentiation, and cell cycle control. Disruptions in HAT activity can lead to various diseases, including cancer and neurodevelopmental disorders.'
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Proteins (11)
| Protein | Definition | Taxonomy |
|---|---|---|
| Histone acetyltransferase KAT2B | A histone acetyltransferase KAT2B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92831] | Homo sapiens (human) |
| Histone acetyltransferase KAT2A | A histone acetyltransferase KAT2A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92830] | Homo sapiens (human) |
| Histone acetyltransferase p300 | A histone acetyltransferase p300 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q09472] | Homo sapiens (human) |
| Histone acetyltransferase KAT5 | A histone acetyltransferase KAT5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92993] | Homo sapiens (human) |
| Histone acetyltransferase KAT2B | A histone acetyltransferase KAT2B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92831] | Homo sapiens (human) |
| Histone acetyltransferase KAT2A | A histone acetyltransferase KAT2A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92830] | Homo sapiens (human) |
| CREB-binding protein | A CREB-binding protein that is encoded in the genome of human. [PMID:11331617] | Homo sapiens (human) |
| Transcription initiation factor TFIID subunit 1-like | A transcription initiation factor TFIID 210 kDa subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8IZX4] | Homo sapiens (human) |
| Histone acetyltransferase p300 | A histone acetyltransferase p300 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q09472] | Homo sapiens (human) |
| Transcription initiation factor TFIID subunit 1 | A transcription initiation factor TFIID subunit 1 that is encoded in the genome of human. [PRO:DNx] | Homo sapiens (human) |
| Transcription initiation factor TFIID subunit 1 | A transcription initiation factor TFIID subunit 1 that is encoded in the genome of human. [PRO:DNx] | Homo sapiens (human) |
Compounds (54)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| 4-aminophenol | 4-aminophenol : An amino phenol (one of the three possible isomers) which has the single amino substituent located para to the phenolic -OH group. 4-aminophenol: RN given refers to parent cpd | aminophenol | allergen; metabolite |
| altretamine | Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine. | triamino-1,3,5-triazine | |
| cgs 15943 | 9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine: non-xanthine triazoloquinazoline adenosine antagonist CGS 15943 : A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors. | aromatic amine; biaryl; furans; organochlorine compound; primary amino compound; quinazolines; triazoloquinazoline | adenosine A1 receptor antagonist; adenosine A2A receptor antagonist; antineoplastic agent; central nervous system stimulant |
| embelin | embelin : A member of the class of dihydroxy-1,4-benzoquinones that is 2,5-dihydroxy-1,4-benzoquinone which is substituted by an undecyl group at position 3. Isolated from Lysimachia punctata and Embelia ribes, it exhibits antimicrobial, antineoplastic and inhibitory activity towards hepatitis C protease. embelin: from Embelia fruit (Myrsinaceae) | dihydroxy-1,4-benzoquinones | antimicrobial agent; antineoplastic agent; hepatitis C protease inhibitor; plant metabolite |
| etazolate | etazolate : A pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted at positions 1, 4, and 5 by ethyl, 2-isopropylidenehydrazino, and ethoxycarbonyl groups, respectively. A phosphodiesterase IV inhibitor with antidepressant and anxiolytic properties. Etazolate: A potent phosphodiesterase inhibitor proposed as an antipsychotic agent. | ethyl ester; hydrazone; pyrazolopyridine | alpha-secretase activator; antidepressant; antipsychotic agent; anxiolytic drug; GABA agent; neuroprotective agent; phosphodiesterase IV inhibitor |
| nocodazole | aromatic ketone; benzimidazoles; carbamate ester; thiophenes | antimitotic; antineoplastic agent; microtubule-destabilising agent; tubulin modulator | |
| papaverine | papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels. | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| ici 136,753 | pyrazolopyridine | ||
| 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole | 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole: antineoplastic; activates platelet guanylate cyclase; a radiosensitizing agent and guanylate cyclase activator; structure in first source lificiguat : A member of the class of indazoles that is 1H-indazole which is substituted by a benzyl group at position 1 and a 5-(hydroxymethyl)-2-furyl group at position 3. It is an activator of soluble guanylate cyclase and inhibits platelet aggregation. | aromatic primary alcohol; furans; indazoles | antineoplastic agent; apoptosis inducer; platelet aggregation inhibitor; soluble guanylate cyclase activator; vasodilator agent |
| colchicine | (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions. | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| plumbagin | plumbagin : A hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogens at positions 2 and 5 are substituted by methyl and hydroxy groups, respectively. plumbagin: a superoxide anion generator | hydroxy-1,4-naphthoquinone; phenols | anticoagulant; antineoplastic agent; immunological adjuvant; metabolite |
| ferrocin c | N-methyl-2-quinolone: structure in first source | ||
| n-methylpyrrolidone | 1-methylpyrrolidin-2-one: structure in first source N-methylpyrrolidin-2-one : A member of the class of pyrrolidine-2-ones that is pyrrolidin-2-one in which the hydrogen attached to the nitrogen is replaced by a methyl group. | lactam; N-alkylpyrrolidine; pyrrolidin-2-ones | polar aprotic solvent |
| palmatine | burasaine: structure in first source | berberine alkaloid; organic heterotetracyclic compound | plant metabolite |
| 4-Methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one | benzodiazepine | ||
| epigallocatechin gallate | (-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin. epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis) | flavans; gallate ester; polyphenol | antineoplastic agent; antioxidant; apoptosis inducer; geroprotector; Hsp90 inhibitor; neuroprotective agent; plant metabolite |
| delphinidin | delphinidin chloride : An anthocyanidin chloride that has delphinidin as the cationic counterpart. Paraffin: A mixture of solid hydrocarbons obtained from petroleum. It has a wide range of uses including as a stiffening agent in ointments, as a lubricant, and as a topical anti-inflammatory. It is also commonly used as an embedding material in histology. | anthocyanidin chloride | |
| haloprogin | venenatine: RN given for (3beta,16beta,17beta,20alpha)-isomer; structure in first source | ||
| taxodione | taxodione: structure | diterpenoid | |
| coenzyme a | adenosine 3',5'-bisphosphate | coenzyme; Escherichia coli metabolite; mouse metabolite | |
| c.i. direct red 23 | C.I. Direct Red 23: azo dye; structure in first source | ||
| oxoglaucine | 1,2,9,10-tetramethoxy-7H-dibenzo(de,g)quinolin-7-one: a phosphatidylinositol 3-kinase p110alpha inhibitor that reactivates latent HIV-1; structure in first source | isoquinoline alkaloid | |
| n-(4-(7-diethylamino-4-methylcoumarin-3-yl)phenyl)maleimide | 7-diethylamino-3-(4-maleimidophenyl)-4-methylcoumarin : A member of the class of coumarins that is 2H-chromen-2-one substituted by 4-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)phenyl, methyl, and diethylamino groups at positions 3, 4 and 7, respectively. It is a thiol-reactive fluorescent dye. N-(4-(7-diethylamino-4-methylcoumarin-3-yl)phenyl)maleimide: structure given in first source | benzenes; coumarins; maleimides; tertiary amino compound | fluorescent dye |
| anacardic acid | anacardic acid : A hydroxybenzoic acid that is salicylic acid substituted by a pentadecyl group at position 6. It is a major component of cashew nut shell liquid and exhibits an extensive range of bioactivities. anacardic acid: isolated from Anacardium occidentale; monophenol monooxygenase inhibitor | hydroxy monocarboxylic acid; hydroxybenzoic acid | anti-inflammatory agent; antibacterial agent; anticoronaviral agent; apoptosis inducer; EC 2.3.1.48 (histone acetyltransferase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; neuroprotective agent; plant metabolite |
| mrs 1220 | 9-chloro-2-(2-furyl)-5-phenylacetylamino(1,2,4)triazolo(1,5-c)quinazoline: structure in first source | quinazolines | |
| rolipram | (-)-rolipram : The (R)-enantiomer of rolipram. | rolipram | |
| 2-methyl-2,3,4,5-tetrahydro-1,5-benzoxazepin-4-one | organonitrogen heterocyclic compound; oxacycle | ||
| methyl indole-3-carboxylate | methyl indole-3-carboxylate : The methyl ester of indole-3-carboxylic acid. | indoles; methyl ester | metabolite |
| 2-(3-Chloro-2-fluorophenyl)-2,3-dihydroisothiazol-3-one | organofluorine compound | ||
| 4-(1H-benzimidazol-2-ylmethylthio)-2-methylbenzofuro[3,2-d]pyrimidine | benzimidazoles | ||
| 2-(4-benzofuro[3,2-d]pyrimidinylthio)-1-thiophen-2-ylethanone | benzofurans | ||
| curcumin | curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa. Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes. | aromatic ether; beta-diketone; diarylheptanoid; enone; polyphenol | anti-inflammatory agent; antifungal agent; antineoplastic agent; biological pigment; contraceptive drug; dye; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; flavouring agent; food colouring; geroprotector; hepatoprotective agent; immunomodulator; iron chelator; ligand; lipoxygenase inhibitor; metabolite; neuroprotective agent; nutraceutical; radical scavenger |
| 4-[2-(9-methyl-6-indolo[3,2-b]quinoxalinyl)ethyl]morpholine | quinoxaline derivative | ||
| umi-77 | UMI-77: an Mcl-1 inhibitor; structure in first source | ||
| N-[4,6-bis(4-morpholinyl)-1,3,5-triazin-2-yl]-2-(methylthio)-1,3-benzothiazol-6-amine | benzothiazoles | ||
| cyqualon | cyclovalone: is a synthetic curcumin derivative; structure in first source | ||
| fisetin | 3'-hydroxyflavonoid; 7-hydroxyflavonol; tetrahydroxyflavone | anti-inflammatory agent; antioxidant; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; geroprotector; metabolite; plant metabolite | |
| guttiferone e | guttiferone E: isolated from the fruits of Garcinia pyrifera collected in Malaysia; structure in first source | ||
| 2-hydroxy-6-[(8Z,11Z)-pentadeca-8,11,14-trien-1-yl]benzoic acid | hydroxybenzoic acid | ||
| 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- | organonitrogen heterocyclic compound; organosulfur heterocyclic compound | ||
| chetomin | |||
| cambogin | isogarcinol: has immunosuppresant activity; isolated from Garcinia mangostana; structure in first source | ||
| icg 001 | peptide | ||
| bi 2536 | |||
| 3,4-dimethoxy-n-((2,2-dimethyl-2h-chromen-6-yl)methyl)-n-phenylbenzenesulfonamide | 3,4-dimethoxy-N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-N-phenylbenzenesulfonamide: has antineoplastic activity; structure in first source | ||
| 3-furancarboxylic acid, tetrahydro-4-methylene-5-oxo-2-propyl-, (2r,3s)-rel- | gamma-lactone | ||
| (3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholine | indoles | ||
| jq1 compound | carboxylic ester; organochlorine compound; tert-butyl ester; thienotriazolodiazepine | angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; bromodomain-containing protein 4 inhibitor; cardioprotective agent; ferroptosis inducer | |
| gsk525762a | molibresib: mimicks acetylated histones; structure in first source | benzodiazepine | |
| gsk1210151a | GSK1210151A: inhibitor of the BET family of proteins; structure in first source | imidazoquinoline | |
| i-bet726 | |||
| 2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide | 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide: a probe for bromo and extra C-terminal domain proteins; structure in first source | quinazolines | |
| 1,2-bis(isothiazol-5-yl)disulfane | 1,2-bis(isothiazol-5-yl)disulfane: structure in first source | ||
| rvx 208 | apabetalone: a bromodomain and extra-terminal domain protein (BET) inhibitor; prevents interactions between BET proteins and acetyl-lysine residues on histone tails to modify epigenetic regulation |