Page last updated: 2024-10-24

peptide-lysine-N-acetyltransferase activity

Definition

Target type: molecularfunction

Catalysis of the reaction: acetyl-CoA + lysine in peptide = CoA + N-acetyl-lysine-peptide. [GOC:dph, RHEA:45948]

Peptide-lysine N-acetyltransferase activity refers to the enzymatic activity of transferring an acetyl group from acetyl-CoA to the epsilon-amino group of lysine residues within a peptide substrate. This reaction is catalyzed by enzymes belonging to the GNAT (Gcn5-related N-acetyltransferase) family.

The acetylation process plays a crucial role in regulating various cellular processes, including protein stability, protein-protein interactions, and signal transduction. It can alter the properties of peptides by:

1. Modifying the charge distribution and hydrophobicity of the lysine residue, affecting its interactions with other molecules.
2. Altering the conformation and flexibility of the peptide, influencing its activity and interactions with other proteins.
3. Creating recognition sites for other proteins, like chaperones or signaling molecules, leading to changes in protein localization or function.

The specific molecular function of peptide-lysine N-acetyltransferase activity can vary depending on the target peptide and the cellular context. It may be involved in:

- **Histone acetylation:** Acetylation of lysine residues in histone proteins, which are involved in DNA packaging, can modulate chromatin structure and accessibility to transcription factors, thereby regulating gene expression.
- **Transcriptional regulation:** Acetylation of non-histone proteins, like transcription factors, can affect their binding to DNA, influencing gene expression.
- **Signal transduction:** Acetylation of signaling proteins can regulate their activity and downstream signaling pathways, affecting cellular responses to various stimuli.
- **Protein stability:** Acetylation can protect proteins from degradation by altering their interaction with proteasomes.
- **Protein-protein interactions:** Acetylation can modulate the interaction of peptides with other proteins, influencing the formation of protein complexes and cellular processes.

Overall, peptide-lysine N-acetyltransferase activity is a versatile enzymatic activity that plays a critical role in regulating diverse cellular functions through lysine acetylation, ultimately contributing to cellular homeostasis and organismal development.'
"

Proteins (9)

ProteinDefinitionTaxonomy
Histone acetyltransferase KAT2BA histone acetyltransferase KAT2B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92831]Homo sapiens (human)
CREB-binding proteinA CREB-binding protein that is encoded in the genome of human. [PMID:11331617]Homo sapiens (human)
Histone acetyltransferase p300A histone acetyltransferase p300 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q09472]Homo sapiens (human)
Histone acetyltransferase KAT8A histone acetyltransferase KAT8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H7Z6]Homo sapiens (human)
Histone acetyltransferase KAT5A histone acetyltransferase KAT5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92993]Homo sapiens (human)
Histone acetyltransferase KAT2BA histone acetyltransferase KAT2B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92831]Homo sapiens (human)
Histone acetyltransferase KAT2AA histone acetyltransferase KAT2A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92830]Homo sapiens (human)
CREB-binding proteinA CREB-binding protein that is encoded in the genome of human. [PMID:11331617]Homo sapiens (human)
Histone acetyltransferase p300A histone acetyltransferase p300 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q09472]Homo sapiens (human)

Compounds (60)

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
altretamineAltretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine.triamino-1,3,5-triazine
cgs 159439-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
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
etazolateetazolate : 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
nocodazolearomatic ketone;
benzimidazoles;
carbamate ester;
thiophenes
antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
papaverinepapaverine : 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 136,753pyrazolopyridine
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole3-(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
1-nitronaphthalene1-nitronaphthalene : A mononitronaphthalene substituted by a nitro group at position 1.

1-nitronaphthalene: RN given refers to cpd with locant for nitro moiety in 1 position

mononitronaphthalene : A nitronaphthalene carrying a single nitro group at unspecified position.

nitronaphthalene : A nitroarene that is naphthalene substituted by at least one nitro group.
mononitronaphthaleneenvironmental contaminant;
mouse metabolite
phenylhydrazinephenylhydrazinesxenobiotic
4-chloroaniline4-chloroaniline : A chloroaniline in which the chloro atom is para to the aniline amino group.

4-chloroaniline: RN given refers to parent cpd; structure
chloroaniline;
monochlorobenzenes
1-naphthylamine1-naphthylamine : A naphthylamine that is naphthalene substituted by an amino group at position 1.

1-Naphthylamine: A suspected industrial carcinogen (and listed as such by OSHA). Its N-hydroxy metabolite is strongly carcinogenic and mutagenic.

naphthylamine : A primary arylamine that is naphthalene substituted by an amino group at unspecified position.
naphthylaminehuman xenobiotic metabolite
4-fluoroaniline4-fluoroaniline : A primary arylamine that is the derivative of aniline in which the hydrogen at position 4 has been substituted by fluorine. It is used as an intermediate in the manufacture of pharmaceuticals, herbicides and plant growth regulators.

4-fluoroaniline: chemical intermediate manufactured by the Halex process; RN given refers to parent cpd; structure given in first source
fluoroaniline;
primary arylamine
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
n-methylpyrrolidone1-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
palmatineburasaine: structure in first sourceberberine alkaloid;
organic heterotetracyclic compound
plant metabolite
4-Methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-onebenzodiazepine
phenylhydrazine hydrochloridephenylhydrazine hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of phenylhydrazine and hydrogen chloride.hydrochloride
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
4-fluorobenzylamine
delphinidindelphinidin 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
4-hydroxyquinoline4-quinolone : A quinolone that is 1,4-dihydroquinoline substituted by an oxo group at position 4.monohydroxyquinoline;
quinolone
haloproginvenenatine: RN given for (3beta,16beta,17beta,20alpha)-isomer; structure in first source
taxodionetaxodione: structurediterpenoid
coenzyme aadenosine 3',5'-bisphosphatecoenzyme;
Escherichia coli metabolite;
mouse metabolite
c.i. direct red 23C.I. Direct Red 23: azo dye; structure in first source
oxoglaucine1,2,9,10-tetramethoxy-7H-dibenzo(de,g)quinolin-7-one: a phosphatidylinositol 3-kinase p110alpha inhibitor that reactivates latent HIV-1; structure in first sourceisoquinoline alkaloid
n-(4-(7-diethylamino-4-methylcoumarin-3-yl)phenyl)maleimide7-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 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
mrs 12209-chloro-2-(2-furyl)-5-phenylacetylamino(1,2,4)triazolo(1,5-c)quinazoline: structure in first sourcequinazolines
rolipram(-)-rolipram : The (R)-enantiomer of rolipram.rolipram
2-methyl-2,3,4,5-tetrahydro-1,5-benzoxazepin-4-oneorganonitrogen heterocyclic compound;
oxacycle
methyl indole-3-carboxylatemethyl indole-3-carboxylate : The methyl ester of indole-3-carboxylic acid.indoles;
methyl ester
metabolite
2-(3-Chloro-2-fluorophenyl)-2,3-dihydroisothiazol-3-oneorganofluorine compound
4-(1H-benzimidazol-2-ylmethylthio)-2-methylbenzofuro[3,2-d]pyrimidinebenzimidazoles
2-(4-benzofuro[3,2-d]pyrimidinylthio)-1-thiophen-2-ylethanonebenzofurans
curcumincurcumin : 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]morpholinequinoxaline derivative
umi-77UMI-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-aminebenzothiazoles
cyqualoncyclovalone: is a synthetic curcumin derivative; structure in first source
fisetin3'-hydroxyflavonoid;
7-hydroxyflavonol;
tetrahydroxyflavone
anti-inflammatory agent;
antioxidant;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
metabolite;
plant metabolite
guttiferone eguttiferone 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 acidhydroxybenzoic 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
camboginisogarcinol: has immunosuppresant activity; isolated from Garcinia mangostana; structure in first source
icg 001peptide
3,4-dimethoxy-n-((2,2-dimethyl-2h-chromen-6-yl)methyl)-n-phenylbenzenesulfonamide3,4-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
jq1 compoundcarboxylic 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
gsk525762amolibresib: mimicks acetylated histones; structure in first sourcebenzodiazepine
gsk1210151aGSK1210151A: inhibitor of the BET family of proteins; structure in first sourceimidazoquinoline
i-bet726
2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide2-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 sourcequinazolines
1,2-bis(isothiazol-5-yl)disulfane1,2-bis(isothiazol-5-yl)disulfane: structure in first source
rvx 208apabetalone: 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