Target type: molecularfunction
Catalysis of the reaction: crotonyl-CoA + histone = CoA + crotonyl-histone. [PMID:25818647]
Histone crotonyltransferase activity is a critical molecular function that involves the transfer of a crotonyl group (CH3CH=CHCO-) from a crotonyl donor molecule, typically acetyl-CoA, to a specific lysine residue on histone proteins. Histones are the primary structural proteins that organize DNA into nucleosomes, the basic unit of chromatin. Crotonylation, like acetylation, is a post-translational modification that alters the chemical structure of histones, influencing chromatin accessibility and gene expression.
The process of histone crotonylation involves the following key steps:
1. **Substrate Recognition:** The crotonyltransferase enzyme recognizes and binds to the histone substrate. This recognition typically involves specific amino acid sequences surrounding the lysine residue targeted for modification.
2. **Crotonyl Donor Binding:** The enzyme binds to the crotonyl donor molecule, typically acetyl-CoA. The crotonyl group is then transferred from the donor to the enzyme's active site.
3. **Catalysis:** The enzyme catalyzes the transfer of the crotonyl group from the enzyme to the lysine residue on the histone protein. This reaction involves the formation of a covalent bond between the crotonyl group and the lysine side chain.
4. **Product Release:** The enzyme releases the modified histone and the remaining donor molecule.
The functional consequences of histone crotonylation are multifaceted:
* **Chromatin Remodeling:** Crotonylation can alter chromatin structure by modifying histone-DNA interactions. It can increase chromatin accessibility, promoting gene expression, or decrease accessibility, repressing gene expression.
* **Transcription Regulation:** Crotonylation influences the recruitment of transcription factors and other regulatory proteins to specific genomic regions. It can activate or repress gene transcription depending on the location and context of the modification.
* **Cellular Processes:** Crotonylation plays a role in diverse cellular processes, including DNA repair, cell cycle regulation, and development. It can modulate the activity of various proteins involved in these processes.
Understanding the molecular function of histone crotonyltransferase activity is crucial for comprehending the intricate mechanisms that regulate gene expression and cellular function. This research area continues to grow, revealing the diverse roles of crotonylation in various physiological and pathological contexts.'
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Protein | Definition | Taxonomy |
---|---|---|
Histone acetyltransferase p300 | A histone acetyltransferase p300 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q09472] | Homo sapiens (human) |
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 |
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 |
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 |
palmatine | burasaine: structure in first source | berberine alkaloid; organic heterotetracyclic compound | plant metabolite |
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 | ||
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 |
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 |
umi-77 | UMI-77: an Mcl-1 inhibitor; structure in first source | ||
cyqualon | cyclovalone: is a synthetic curcumin derivative; structure in first source | ||
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 | ||
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 | ||
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 | |
i-bet726 | |||
1,2-bis(isothiazol-5-yl)disulfane | 1,2-bis(isothiazol-5-yl)disulfane: structure in first source |