Page last updated: 2024-10-24
histone acetyltransferase binding
Definition
Target type: molecularfunction
Binding to an histone acetyltransferase. [GOC:bf]
Histone acetyltransferases (HATs) are a family of enzymes that catalyze the acetylation of lysine residues on histone proteins. Acetylation is a reversible post-translational modification that plays a crucial role in regulating gene expression. HATs can be broadly classified into two main groups: Type A HATs, which are primarily involved in nucleosome assembly and DNA replication, and Type B HATs, which are involved in transcriptional regulation.
Histone acetylation is a complex process that involves the transfer of an acetyl group from acetyl-CoA to the ε-amino group of a lysine residue on histone tails. This modification alters the electrostatic charge of the histone tails, reducing their affinity for DNA. This change in chromatin structure can lead to increased accessibility of DNA to transcription factors, ultimately leading to gene activation.
The binding of HATs to their substrates is influenced by a variety of factors, including the specific histone tail sequence, the presence of other histone modifications, and the cellular environment.
The molecular function of HAT binding can be summarized as follows:
* **Recognition of target histone tails:** HATs specifically recognize and bind to their target histone tails via specific protein-protein interactions.
* **Catalysis of acetylation:** Once bound, HATs catalyze the transfer of an acetyl group from acetyl-CoA to the ε-amino group of a lysine residue on the histone tail.
* **Regulation of chromatin structure:** Histone acetylation, catalyzed by HATs, alters the electrostatic charge of the histone tails, leading to changes in chromatin structure.
* **Modulation of gene expression:** The changes in chromatin structure induced by HAT binding can impact the accessibility of DNA to transcription factors, leading to the modulation of gene expression.
* **Crosstalk with other histone modifications:** HAT binding can be influenced by and can also influence other histone modifications, creating a complex network of regulatory mechanisms.
Overall, HAT binding plays a pivotal role in regulating gene expression by modulating chromatin structure and influencing the accessibility of DNA to transcription factors.'
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Proteins (4)
| 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) |
| NAD-dependent protein deacetylase sirtuin-2 | An NAD-dependent protein deacetylase sirtuin-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8IXJ6] | Homo sapiens (human) |
| Signal transducer and activator of transcription 1-alpha/beta | A signal transducer and activator of transcription 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P42224] | Homo sapiens (human) |
| Proliferating cell nuclear antigen | A proliferating cell nuclear antigen that is encoded in the genome of human. [PRO:DNx] | Homo sapiens (human) |
Compounds (57)
| 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 |
| niacinamide | nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group. | pyridine alkaloid; pyridinecarboxamide; vitamin B3 | anti-inflammatory agent; antioxidant; cofactor; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; Escherichia coli metabolite; geroprotector; human urinary metabolite; metabolite; mouse metabolite; neuroprotective agent; Saccharomyces cerevisiae metabolite; Sir2 inhibitor |
| bisindolylmaleimide i | bisindolylmaleimide I: a bis(indolyl)maleimide | ||
| 2-(1-(2-(1-methylpyrrolidino)ethyl)-1h-indol-3-yl)maleimide | bisindolylmaleimide II: protein kinase C inhibitor; see also bisindolylmaleimide I | ||
| bisindolylmaleimide iv | indoles; maleimides | ||
| bisindolylmaleimide v | bisindolylmaleimide V: used as a negative control compound for protein kinase C inhibition; structure in first source; | indoles | |
| 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 |
| go 6976 | indolocarbazole; organic heterohexacyclic compound | EC 2.7.11.13 (protein kinase C) inhibitor | |
| idebenone | 1,4-benzoquinones; primary alcohol | antioxidant; ferroptosis inhibitor | |
| nsc 664704 | kenpaullone : An indolobenzazepine that is paullone in which the hydrogen at position 9 is replaced by a bromo substituent. It is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3beta (GSK3beta). kenpaullone: inhibits CDK1/cyclin B; structure in first source | indolobenzazepine; lactam; organobromine compound | cardioprotective agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor; geroprotector |
| fenamic acid | fenamic acid : An aminobenzoic acid that is the N-phenyl derivative of anthranilic acid. It acts as a parent skeleton for the synthesis of several non-steroidal anti-inflammatory drugs. fenamic acid: has chloride and potassium channel-blocking activity; RN given refers to parent cpd | aminobenzoic acid; secondary amino compound | membrane transport modulator |
| ro 31-8220 | Ro 31-8220: a protein kinase C inhibitor | imidothiocarbamic ester; indoles; maleimides | EC 2.7.11.13 (protein kinase C) inhibitor |
| fenofibrate | benzochromenone; delta-lactone; naphtho-alpha-pyrone | platelet aggregation inhibitor; Sir2 inhibitor | |
| suramin | suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties. | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
| 3,3',5-triiodothyroacetic acid | tiratricol : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)acetic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxy-3-iodophenoxy group. It is a thyroid hormone analogue that has been used in the treatment of thyroid hormone resistance syndrome. | ||
| 3,3',5-triiodothyropropionic acid | aromatic ether | ||
| thyroxine | thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions. Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism. | 2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine; thyroxine zwitterion | antithyroid drug; human metabolite; mouse metabolite; thyroid hormone |
| triiodothyronine | 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism. Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3. | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| suramin sodium | suramin sodium : An organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness. | organic sodium salt | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
| 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 | ||
| 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 |
| toxoflavin | toxoflavin : A pyrimidotriazine that is 1,6-dimethyl-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine with oxo groups at positions 5 and 7. toxoflavin: azapteridine antibiotic; structure | carbonyl compound; pyrimidotriazine | antibacterial agent; antineoplastic agent; apoptosis inducer; bacterial metabolite; toxin; virulence factor; Wnt signalling inhibitor |
| coenzyme a | adenosine 3',5'-bisphosphate | coenzyme; Escherichia coli metabolite; mouse metabolite | |
| 3,5-diiodothyronine, (l)-isomer | phenylalanine derivative | ||
| 3,3'-diiodothyronine | 3,3'-diiodothyronine: RN given refers to unlabeled cpd without isomeric designation | 3,3'-diiodothyronine; amino acid zwitterion | human metabolite |
| 3,5-diiodothyropropionic acid | 3,5-diiodothyropropionic acid : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)propanoic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxyphenyl group. An ionotropic analogue of L-thyroxine. 3,5-diiodothyropropionic acid: a cardiotonic thyroid hormone analog | aromatic ether; monocarboxylic acid; organoiodine compound; phenols | |
| 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 |
| nsc 74859 | NSC 74859: inhibits Stat3 binding activity; structure in first source S3I-201 : An amidobenzoic acid obtained by formal condensation of the carboxy group of [(4-methylbenzene-1-sulfonyl)oxy]acetic acid with the amino group of 4-amino-2-hydroxybenzoic acid. | amidobenzoic acid; monohydroxybenzoic acid; tosylate ester | STAT3 inhibitor |
| paullone | paullone : An indolobenzazepine that is 5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine carrying an oxo substituent at position 6. paullone: structure in first source | indolobenzazepine; lactam | EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor |
| hyperforin | hyperforin : A cyclic terpene ketone that is a prenylated carbobicyclic acylphloroglucinol derivative produced by St. John's Wort, Hypericum perforatum. hyperforin: a prenylated acylphloroglucinol derivative; antibiotic component of novoimanine; psychoactive agent in St. John's wort; Russian; structure; | ||
| resveratrol | trans-resveratrol : A resveratrol in which the double bond has E configuration. | resveratrol | antioxidant; phytoalexin; plant metabolite; quorum sensing inhibitor; radical scavenger |
| 2-(3-Chloro-2-fluorophenyl)-2,3-dihydroisothiazol-3-one | organofluorine compound | ||
| 3-(1-azepanylsulfonyl)-n-(3-bromphenyl)benzamide | 3-(1-azepanylsulfonyl)-N-(3-bromphenyl)benzamide: a sirtuin 2 inhibitor; structure in first source | ||
| 1,4-bis[2-(4-hydroxyphenyl)ethylamino]anthracene-9,10-dione | anthraquinone | ||
| sirtinol | aldimine; benzamides; naphthols | anti-inflammatory agent; EC 3.5.1.98 (histone deacetylase) inhibitor; Sir2 inhibitor | |
| cambinol | cambinol: inhibitor of human silent information regulator 2 enzymes; structure in first source | ||
| (4-chlorophenyl)-[4-(8-nitro-5-quinolinyl)-1-piperazinyl]methanone | N-arylpiperazine | ||
| ex 527 | 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide : A member of the class of carbazoles that is 2,3,4,9-tetrahydro-1H-carbazole which is substituted at position 1 by an aminocarbohyl group and at position 6 by a chlorine. 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide: structure in first source | carbazoles; monocarboxylic acid amide; organochlorine compound | |
| su 11248 | monocarboxylic acid amide; pyrroles | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist | |
| guttiferone e | guttiferone E: isolated from the fruits of Garcinia pyrifera collected in Malaysia; structure in first source | ||
| nf 449 | |||
| panobinostat | panobinostat : A hydroxamic acid obtained by formal condensation of the carboxy group of (2E)-3-[4-({[2-(2-methylindol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enoic acid with the amino group of hydroxylamine. A histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma. Panobinostat: An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA. | cinnamamides; hydroxamic acid; methylindole; secondary amino compound | angiogenesis modulating agent; antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor |
| 2-hydroxy-6-[(8Z,11Z)-pentadeca-8,11,14-trien-1-yl]benzoic acid | hydroxybenzoic acid | ||
| oblongifolin c | oblongifolin C: has antineoplastic activity; isolated from Garcinia yunnanensis; structure in first source | ||
| 5,15-diphenylporphine | 5,15-diphenylporphine: structure in first source | ||
| quisinostat | indoles | ||
| guttiferone k | guttiferone K: antiproliferative compound of Rheedia calcicola from the Madagascar rain forest; structure in first source | ||
| srt1460 | SRT1460: small molecule activator of SIRT1 as therapeutics for the treatment of type 2 diabetes; structure in first source | ||
| srt1720 | |||
| srt2183 | SRT2183: small molecule activator of SIRT1 as therapeutics for the treatment of type 2 diabetes; structure in first source | ||
| tenovin-6 | tenovin-6 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-(dimethylamino)pentanoic acid with the aromatic amino group of N-[(4-aminophenyl)carbamothioyl]-4-tert-butylbenzamide. | monocarboxylic acid amide; tertiary amino compound; thioureas | antineoplastic agent; p53 activator; Sir2 inhibitor |
| i-bet726 | |||
| acy-1215 | ricolinostat: an HDAC6 inhibitor; structure in first source | pyrimidinecarboxylic acid | |
| 1,2-bis(isothiazol-5-yl)disulfane | 1,2-bis(isothiazol-5-yl)disulfane: structure in first source | ||
| aristoforin | Aristoforin: derivative of hyperforin, is a potent anticancer agent; structure in first source | ||
| n-(3-((2-hydroxynaphthalen-1-ylmethylene)amino)phenyl)-2-phenylpropionamide |