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Literature summary for 2.3.1.48 extracted from

  • Han, Z.; Chou, C.W.; Yang, X.; Bartlett, M.G.; Zheng, Y.G.
    Profiling cellular substrates of lysine acetyltransferases GCN5 and p300 with orthogonal labeling and click chemistry (2017), ACS Chem. Biol., 12, 1547-1555 .
    View publication on PubMed
Search for more literature for 2.3.1.48

Protein Variants

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 [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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens Q09472
-
-
Homo sapiens Q92830
-
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
Gcn5
-
 Homo sapiens
KAT
-
 Homo sapiens
Kat2A
-
 Homo sapiens
lysine acetyltransferase
-
 Homo sapiens
p300
-
 Homo sapiens

Turnover Number [1/s]

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

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

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 [mM/s]

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