Target type: molecularfunction
Catalysis of the reaction: acetyl-CoA + histone H4 L-lysine (position 5) = CoA + histone H4 N6-acetyl-L-lysine (position 5). [EC:2.3.1.48]
Histone H4K5 acetyltransferase activity refers to the enzymatic ability of certain proteins to catalyze the transfer of an acetyl group from acetyl coenzyme A (acetyl-CoA) to the epsilon-amino group of lysine 5 (K5) on histone H4. This modification is a key component of epigenetic regulation, influencing gene expression and other cellular processes.
Here's a detailed explanation of the molecular function:
1. **Substrate Recognition:** The acetyltransferase recognizes and binds to histone H4, specifically targeting the lysine 5 residue. This interaction involves specific amino acid sequences and electrostatic interactions that create a binding pocket for the histone.
2. **Acetyl-CoA Binding:** The acetyltransferase binds to acetyl-CoA, the donor molecule carrying the acetyl group. The enzyme's active site contains a cysteine residue that forms a thioester bond with the acetyl group, preparing it for transfer.
3. **Catalysis:** Through a complex series of steps, the acetyltransferase facilitates the transfer of the acetyl group from acetyl-CoA to the lysine 5 residue on histone H4. This involves nucleophilic attack by the epsilon-amino group of lysine 5 on the acetyl group, releasing CoA and forming an acetylated lysine residue.
4. **Product Release:** After acetylation, the enzyme releases the modified histone H4, allowing it to interact with other proteins or DNA.
**Significance of H4K5 Acetylation:**
* **Gene Regulation:** Acetylation of histone H4 at lysine 5 is associated with increased gene expression. It typically alters chromatin structure, making DNA more accessible to transcription factors and promoting transcription initiation.
* **Chromatin Remodeling:** This modification can influence the recruitment of other proteins involved in chromatin remodeling, such as ATP-dependent chromatin remodelers. These proteins can reposition nucleosomes, altering the accessibility of DNA and regulating gene expression.
* **Cellular Processes:** H4K5 acetylation is implicated in various cellular processes, including development, cell cycle regulation, and response to stress. It plays a role in maintaining genomic stability, DNA repair, and cell differentiation.
**Note:** Specific acetyltransferases responsible for H4K5 acetylation and their regulatory mechanisms are being actively investigated, and the exact roles of this modification in different cellular contexts continue to be explored.'
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Protein | Definition | Taxonomy |
---|---|---|
Bromodomain and PHD finger-containing protein 3 | A bromodomain and PHD finger-containing protein 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9ULD4] | Homo sapiens (human) |
Histone acetyltransferase KAT8 | A histone acetyltransferase KAT8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H7Z6] | Homo sapiens (human) |
Histone acetyltransferase KAT8 | A histone acetyltransferase KAT8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H7Z6] | Homo sapiens (human) |
Peregrin | A peregrin that is encoded in the genome of human. [PRO:DNx, UniProtKB:P55201] | Homo sapiens (human) |
Bromodomain-containing protein 1 | A bromodomain-containing protein 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O95696] | 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 |
1-nitronaphthalene | 1-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. | mononitronaphthalene | environmental contaminant; mouse metabolite |
phenylhydrazine | phenylhydrazines | xenobiotic | |
4-chloroaniline | 4-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-naphthylamine | 1-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. | naphthylamine | human xenobiotic metabolite |
4-fluoroaniline | 4-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 | |
isocarbostyril | isoquinolinone : An isoquinoline containing one or more oxo groups. | isoquinolines | |
ferrocin c | N-methyl-2-quinolone: structure in first source | ||
4-phenylpyridine | phenylpyridine | ||
tricyclazole | tricyclazole : A triazolobenzothiazole that is [1,2,4]triazolo[3,4-b][1,3]benzothiazole which is substituted at position 5 by a methyl group. A fungicide used for the control of rice blast, it is not approved for use within the European Union. tricyclazole: RN given refers to parent cpd | triazolobenzothiazole | antifungal agrochemical; melanin synthesis inhibitor |
phenylhydrazine hydrochloride | phenylhydrazine hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of phenylhydrazine and hydrogen chloride. | hydrochloride | |
4-fluorobenzylamine | |||
4-hydroxyquinoline | 4-quinolone : A quinolone that is 1,4-dihydroquinoline substituted by an oxo group at position 4. | monohydroxyquinoline; quinolone | |
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 |
2,8-dimercapto-6-hydroxypurine | |||
2-hydroxy-6-[(8Z,11Z)-pentadeca-8,11,14-trien-1-yl]benzoic acid | hydroxybenzoic acid | ||
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 | |
i-bet726 |