Literature summary for 2.3.1.48 extracted from

Voloshchuk, N.; Zhu, A.Y.; Snydacker, D.; Montclare, J.K.
Positional effects of monofluorinated phenylalanines on histone acetyltransferase stability and activity (2009), Bioorg. Med. Chem. Lett., 19, 5449-5451.

Search for more literature for 2.3.1.48

Cloned(Commentary)

Cloned (Comment)	Organism
expression of monofluorinated phenylalanine analogues, incorporated into tGCN5, using a phenylalanine auxotrophic Escherichia coli strain AFIQ containing the plasmid IQ, which constitutively expresses the lacIq repressor. Determination of Phe replacement by MALDI-TOF mass spectrometry	Tetrahymena thermophila

Protein Variants

Protein Variants	Comment	Organism
additional information	recombinant enzyme containing fluorinated Phe analogues shows reduced half-life: 27.5 min for the recombinant p-fluorophenylalanine-substituted tGCN5, 5.4 min for recombinant m-fluorophenylalanine-substituted tGCN5, and 6.8 min for recombinant o-fluorophenylalanine-substituted tGCN5	Tetrahymena thermophila

General Stability

General Stability	Organism
the recombinant wild-type tGCN5 shows a half-life of 31.2 min	Tetrahymena thermophila

Inhibitors

Inhibitors	Comment	Organism	Structure
additional information	effects of three monofluorinated phenylalanine analogs p-fluorophenylalanine, m-fluorophenylalanine, and o-fluorophenylalanine on the stability and enzymatic activity of tGCN5, overview	Tetrahymena thermophila

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.69	-	histone H3	recombinant p-fluorophenylalanine-substituted tGCN5	Tetrahymena thermophila
0.8	-	histone H3	recombinant o-fluorophenylalanine-substituted wild-type tGCN5	Tetrahymena thermophila
1.05	-	histone H3	recombinant wild-type tGCN5	Tetrahymena thermophila
2.09	-	histone H3	recombinant m-fluorophenylalanine-substituted wild-type tGCN5	Tetrahymena thermophila

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
acetyl-CoA + histone H3	Tetrahymena thermophila	acetylation of Lys14 by tGCN5 in the consensus sequence QTARKSTGGK14APRKLASK	CoA + acetylhistone H3	-	?

Organism

Organism	UniProt	Comment	Textmining
Tetrahymena thermophila	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
acetyl-CoA + histone H3	acetylation of Lys14 by tGCN5 in the consensus sequence QTARKSTGGK14APRKLASK	Tetrahymena thermophila	CoA + acetylhistone H3	-	?
acetyl-CoA + histone H3	acetylation of Lys14 by tGCN5 in the consensus sequence QTARKSTGGK14APRKLASK. Phe125 and Phe164 interact with the substrate, but are not directly involved in the acetylation reaction, while residues Glu122, Val123 and Tyr160 are critical for catalysis	Tetrahymena thermophila	CoA + acetylhistone H3	-	?

Subunits

Subunits	Comment	Organism
More	tGCN5 is comprised of five alpha-helices and six beta-strands, with N-terminal and C-terminal regions separated by a deep hydrophobic cleft, structure, overview. Phe125 and Phe164 interact with the substrate, but are not directly involved in the acetylation reaction, while residues Glu122, Val123 and Tyr160 are critical for catalysis	Tetrahymena thermophila

Synonyms

Synonyms	Comment	Organism
HAT	-	Tetrahymena thermophila
tGCN5	-	Tetrahymena thermophila

Cofactor

Cofactor	Comment	Organism	Structure
acetyl-CoA	-	Tetrahymena thermophila

kcat/KM [mM/s]

kcat/KM Value [1/mMs^-1]	kcat/KM Value Maximum [1/mMs^-1]	Substrate	Comment	Organism	Structure
0.053	-	histone H3	recombinant o-fluorophenylalanine-substituted tGCN5	Tetrahymena thermophila
0.14	-	histone H3	recombinant p-fluorophenylalanine-substituted tGCN5	Tetrahymena thermophila
0.25	-	histone H3	recombinant m-fluorophenylalanine-substituted tGCN5	Tetrahymena thermophila
0.87	-	histone H3	recombinant wild-type tGCN5	Tetrahymena thermophila

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Release 2023.1 (January 2023)