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)

ProteinDefinitionTaxonomy
Histone acetyltransferase KAT2BA histone acetyltransferase KAT2B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92831]Homo sapiens (human)
NAD-dependent protein deacetylase sirtuin-2An 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/betaA 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 antigenA proliferating cell nuclear antigen that is encoded in the genome of human. [PRO:DNx]Homo sapiens (human)

Compounds (57)

CompoundDefinitionClassesRoles
4-aminophenol4-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
aminophenolallergen;
metabolite
niacinamidenicotinamide : 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 ibisindolylmaleimide I: a bis(indolyl)maleimide
2-(1-(2-(1-methylpyrrolidino)ethyl)-1h-indol-3-yl)maleimidebisindolylmaleimide II: protein kinase C inhibitor; see also bisindolylmaleimide I
bisindolylmaleimide ivindoles;
maleimides
bisindolylmaleimide vbisindolylmaleimide V: used as a negative control compound for protein kinase C inhibition; structure in first source;indoles
embelinembelin : 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-benzoquinonesantimicrobial agent;
antineoplastic agent;
hepatitis C protease inhibitor;
plant metabolite
go 6976indolocarbazole;
organic heterohexacyclic compound
EC 2.7.11.13 (protein kinase C) inhibitor
idebenone1,4-benzoquinones;
primary alcohol
antioxidant;
ferroptosis inhibitor
nsc 664704kenpaullone : 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 acidfenamic 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 31-8220Ro 31-8220: a protein kinase C inhibitorimidothiocarbamic ester;
indoles;
maleimides
EC 2.7.11.13 (protein kinase C) inhibitor
fenofibratebenzochromenone;
delta-lactone;
naphtho-alpha-pyrone
platelet aggregation inhibitor;
Sir2 inhibitor
suraminsuramin : 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 acidtiratricol : 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 acidaromatic ether
thyroxinethyroxine : 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
triiodothyronine3,3',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 sodiumsuramin 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 saltangiogenesis 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
plumbaginplumbagin : 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 cN-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
toxoflavintoxoflavin : 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 aadenosine 3',5'-bisphosphatecoenzyme;
Escherichia coli metabolite;
mouse metabolite
3,5-diiodothyronine, (l)-isomerphenylalanine derivative
3,3'-diiodothyronine3,3'-diiodothyronine: RN given refers to unlabeled cpd without isomeric designation3,3'-diiodothyronine;
amino acid zwitterion
human metabolite
3,5-diiodothyropropionic acid3,5-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 acidanacardic 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 74859NSC 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
paullonepaullone : 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
hyperforinhyperforin : 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;
resveratroltrans-resveratrol : A resveratrol in which the double bond has E configuration.resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
2-(3-Chloro-2-fluorophenyl)-2,3-dihydroisothiazol-3-oneorganofluorine compound
3-(1-azepanylsulfonyl)-n-(3-bromphenyl)benzamide3-(1-azepanylsulfonyl)-N-(3-bromphenyl)benzamide: a sirtuin 2 inhibitor; structure in first source
1,4-bis[2-(4-hydroxyphenyl)ethylamino]anthracene-9,10-dioneanthraquinone
sirtinolaldimine;
benzamides;
naphthols
anti-inflammatory agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Sir2 inhibitor
cambinolcambinol: inhibitor of human silent information regulator 2 enzymes; structure in first source
(4-chlorophenyl)-[4-(8-nitro-5-quinolinyl)-1-piperazinyl]methanoneN-arylpiperazine
ex 5276-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 11248monocarboxylic 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 eguttiferone E: isolated from the fruits of Garcinia pyrifera collected in Malaysia; structure in first source
nf 449
panobinostatpanobinostat : 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 acidhydroxybenzoic acid
oblongifolin coblongifolin C: has antineoplastic activity; isolated from Garcinia yunnanensis; structure in first source
5,15-diphenylporphine5,15-diphenylporphine: structure in first source
quisinostatindoles
guttiferone kguttiferone K: antiproliferative compound of Rheedia calcicola from the Madagascar rain forest; structure in first source
srt1460SRT1460: small molecule activator of SIRT1 as therapeutics for the treatment of type 2 diabetes; structure in first source
srt1720
srt2183SRT2183: small molecule activator of SIRT1 as therapeutics for the treatment of type 2 diabetes; structure in first source
tenovin-6tenovin-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-1215ricolinostat: an HDAC6 inhibitor; structure in first sourcepyrimidinecarboxylic acid
1,2-bis(isothiazol-5-yl)disulfane1,2-bis(isothiazol-5-yl)disulfane: structure in first source
aristoforinAristoforin: derivative of hyperforin, is a potent anticancer agent; structure in first source
n-(3-((2-hydroxynaphthalen-1-ylmethylene)amino)phenyl)-2-phenylpropionamide