Protein Variants | Comment | Organism |
---|---|---|
T612G | site-directed mutagenesis, the mutant is able to activate a series of alkynyl and azido acyl-CoA for histone acylation. Residue Thr612 is conserved in the PCAF/GCN5 family | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
0.0002 | - |
3-azidopropionyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.0003 | - |
6-heptynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.0006 | - |
5-hexynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.0009 | - |
4-pentynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.0024 | - |
4-pentynoyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
0.0037 | - |
acetyl-CoA | wild-type GCN5, pH and temperature not specified in the publication | Homo sapiens | |
0.004 | - |
acetyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.0082 | - |
3-azidopropionyl-CoA | wild-type GCN5, pH and temperature not specified in the publication | Homo sapiens | |
0.0086 | - |
3-azidopropionyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
0.0173 | - |
acetyl-CoA | pH and temperature not specified in the publication | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
acetyl-CoA + [protein]-L-lysine | Homo sapiens | - |
CoA + [protein]-N6-acetyl-L-lysine | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q09472 | - |
- |
Homo sapiens | Q92830 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
3-azidopropionyl-CoA + [histone peptide H3-20]-L-lysine | - |
Homo sapiens | CoA + [histone peptide H3-20]-N6-3-azidopropionyl-L-lysine | - |
? | |
3-azidopropionyl-CoA + [histone peptide H3-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H3-20]-N6-3-azidopropionyl-L-lysine | - |
? | |
3-azidopropionyl-CoA + [histone peptide H4-20]-L-lysine | - |
Homo sapiens | CoA + [histone peptide H4-20]-N6-3-azidopropionyl-L-lysine | - |
? | |
3-azidopropionyl-CoA + [histone peptide H4-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H4-20]-N6-3-azidopropionyl-L-lysine | - |
? | |
4-pentynoyl-CoA + [histone peptide H3-20]-L-lysine | - |
Homo sapiens | CoA + [histone peptide H3-20]-N6-4-pentynoyl-L-lysine | - |
? | |
4-pentynoyl-CoA + [histone peptide H3-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H3-20]-N6-4-pentynoyl-L-lysine | - |
? | |
4-pentynoyl-CoA + [histone peptide H4-20]-L-lysine | - |
Homo sapiens | CoA + [histone peptide H4-20]-N6-4-pentynoyl-L-lysine | - |
? | |
4-pentynoyl-CoA + [histone peptide H4-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H4-20]-N6-4-pentynoyl-L-lysine | - |
? | |
5-hexynoyl-CoA + [histone peptide H3-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H3-20]-N6-5-hexynoyl-L-lysine | - |
? | |
5-hexynoyl-CoA + [histone peptide H3-20]-L-lysine | very low activity with 5-hexynoyl-CoA | Homo sapiens | CoA + [histone peptide H3-20]-N6-5-hexynoyl-L-lysine | - |
? | |
5-hexynoyl-CoA + [histone peptide H4-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H4-20]-N6-5-hexynoyl-L-lysine | - |
? | |
5-hexynoyl-CoA + [histone peptide H4-20]-L-lysine | very low activity with 5-hexynoyl-CoA | Homo sapiens | CoA + [histone peptide H4-20]-N6-5-hexynoyl-L-lysine | - |
? | |
6-heptynoyl-CoA + [histone peptide H3-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H3-20]-N6-6-heptynoyl-L-lysine | - |
? | |
6-heptynoyl-CoA + [histone peptide H3-20]-L-lysine | very low activity with 6-heptynoyl-CoA | Homo sapiens | CoA + [histone peptide H3-20]-N6-6-heptynoyl-L-lysine | - |
? | |
6-heptynoyl-CoA + [histone peptide H4-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H4-20]-N6-6-heptynoyl-L-lysine | - |
? | |
6-heptynoyl-CoA + [histone peptide H4-20]-L-lysine | very low activity with 6-heptynoyl-CoA | Homo sapiens | CoA + [histone peptide H4-20]-N6-6-heptynoyl-L-lysine | - |
? | |
acetyl-CoA + [histone peptide H3-20]-L-lysine | - |
Homo sapiens | CoA + [histone peptide H3-20]-N6-acetyl-L-lysine | - |
? | |
acetyl-CoA + [histone peptide H3-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H3-20]-N6-acetyl-L-lysine | - |
? | |
acetyl-CoA + [histone peptide H4-20]-L-lysine | - |
Homo sapiens | CoA + [histone peptide H4-20]-N6-acetyl-L-lysine | - |
? | |
acetyl-CoA + [histone peptide H4-20]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [histone peptide H4-20]-N6-acetyl-L-lysine | - |
? | |
acetyl-CoA + [protein]-L-lysine | - |
Homo sapiens | CoA + [protein]-N6-acetyl-L-lysine | - |
? | |
acetyl-CoA + [protein]-L-lysine | substrate of wild-type enzyme GCN5 and enzyme mutant T612G | Homo sapiens | CoA + [protein]-N6-acetyl-L-lysine | - |
? | |
additional information | screening of interacting proteins for substrate identification, testing of more than four hundred proteins, KAT substrate enrichment with biotin-streptavidin pulldown and semiquantitative LC-MS/MS studies, overview. The proteins are either p300- or GCN5-unique or shared by the two KATs. 3-Azidopropionyl CoA (3AZ-CoA) is applied as a bioorthogonal surrogate of acetyl-, propionyl- and butyryl-CoA for KAT substrate identification, method overview. Comparison of the substrate profiles of p300 and GCN5, different acetyl-CoA surrogates and histone peptide H3-20 or H4-20 (the first 20 amino acids from the N-terminus of histone H3 or H4) are used as substrates. 3AZ-CoA is a sensitive and specific probe for both p300 and GCN5-T612G with comparable or even stronger activity than Ac-CoA. Substrate validations | Homo sapiens | ? | - |
- |
Synonyms | Comment | Organism |
---|---|---|
Gcn5 | - |
Homo sapiens |
KAT | - |
Homo sapiens |
Kat2A | - |
Homo sapiens |
lysine acetyltransferase | - |
Homo sapiens |
p300 | - |
Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.005 | - |
3-azidopropionyl-CoA | wild-type GCN5, pH and temperature not specified in the publication | Homo sapiens | |
0.0067 | - |
4-pentynoyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
0.063 | - |
6-heptynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.148 | - |
3-azidopropionyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.208 | - |
4-pentynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.233 | - |
3-azidopropionyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
0.24 | - |
5-hexynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.567 | - |
acetyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
0.642 | - |
acetyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
0.788 | - |
acetyl-CoA | wild-type GCN5, pH and temperature not specified in the publication | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
3-azidopropionyl-CoA | - |
Homo sapiens | |
4-pentynoyl-CoA | - |
Homo sapiens | |
5-hexynoyl-CoA | - |
Homo sapiens | |
5-hexynoyl-CoA | a poor surrogate for acetyl-CoA with p300 | Homo sapiens | |
6-heptynoyl-CoA | - |
Homo sapiens | |
6-heptynoyl-CoA | a poor surrogate for acetyl-CoA with p300 | Homo sapiens | |
acetyl-CoA | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
evolution | there are three major families of KATs grouped according to their sequence homology and domain organizations, which include the MYST family, GCN5/PCAF family, and p300/CBP family | Homo sapiens |
physiological function | p300 and GCN5 are two representative lysine acetyltransferases (KATs) in mammalian cells. They possess multiple acyltransferase activities including acetylation, propionylation, and butyrylation of the epsilon-amino group of lysine residues of histones and non-histone protein substrates. The protein substrates are extensively involved in various biological events including gene expression, cell cycle, and cellular metabolism. Canonical KAT-related processes such as gene expression, DNA repair, cell cycle, and apoptosis involve both known and newly identified substrates of p300 and GCN5, overview | Homo sapiens |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.61 | - |
3-azidopropionyl-CoA | wild-type GCN5, pH and temperature not specified in the publication | Homo sapiens | |
2.79 | - |
4-pentynoyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
27.09 | - |
3-azidopropionyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
32.78 | - |
acetyl-CoA | pH and temperature not specified in the publication | Homo sapiens | |
160.5 | - |
acetyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
210 | - |
6-heptynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
212.97 | - |
acetyl-CoA | wild-type GCN5, pH and temperature not specified in the publication | Homo sapiens | |
231.11 | - |
4-pentynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
400 | - |
5-hexynoyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens | |
740 | - |
3-azidopropionyl-CoA | mutant GCN5 T612G, pH and temperature not specified in the publication | Homo sapiens |