Literature summary for 2.3.1.48 extracted from

Jeffers, V.; Gao, H.; Checkley, L.A.; Liu, Y.; Ferdig, M.T.; Sullivan, W.J.
Garcinol inhibits GCN5-mediated lysine acetyltransferase activity and prevents replication of the parasite Toxoplasma gondii (2016), Antimicrob. Agents Chemother., 60, 2164-2170 .

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Cloned(Commentary)

Cloned (Comment)	Organism
gene GCN5, quantitative RT-PCR enzyme expression analysis, recombinant ectopical expression of HA-tagged enzyme TgGCN5b	Toxoplasma gondii

Inhibitors

Inhibitors	Comment	Organism	Structure
garcinol	isolated from Garcinia indica, inhibits GCN5-mediated lysine acetyltransferase activity and prevents the replication of the parasite. Treatment of tachyzoites with garcinol leads to a reduction of global lysine acetylation, particularly on histone H3 and TgGCN5b itself. transcriptome sequencing (RNA-seq), which reveals increasing aberrant gene expression coincident with increasing concentrations of garcinol. The majority of the genes that are most significantly affected by garcinol are also associated with TgGCN5b in a previously reported chromatin immunoprecipitation assay with microarray technology analysis. The dysregulated gene expression induced by garcinol significantly inhibits Toxoplasma tachyzoite replication, and the concentrations used exhibit no overt toxicity on human host cells. Garcinol also reduces autoacetylation of TgGCN5b, garcinol treatment results in a 65% reduction in the acetylation level of HA-tagged TgGCN5b. Garcinol-mediated changes in the parasite transcriptome, overview	Toxoplasma gondii

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
nucleus	-	Toxoplasma gondii	5634	-

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
acetyl-CoA + [histone H3]-L-lysine9	Toxoplasma gondii	-	CoA + [histone H3]-N6-acetyl-L-lysine9	-	?
acetyl-CoA + [protein]-L-lysine	Toxoplasma gondii	-	CoA + [protein]-N6-acetyl-L-lysine	-	?

Organism

Organism	UniProt	Comment	Textmining
Toxoplasma gondii	Q9NIS0	-	-

Purification (Commentary)

Purification (Comment)	Organism
wild-type and recombinant HA-tagged enzyme	Toxoplasma gondii

Source Tissue

Source Tissue	Comment	Organism	Textmining
tachyzoite	-	Toxoplasma gondii	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
acetyl-CoA + [histone H3]-L-lysine9	-	Toxoplasma gondii	CoA + [histone H3]-N6-acetyl-L-lysine9	-	?
acetyl-CoA + [protein]-L-lysine	-	Toxoplasma gondii	CoA + [protein]-N6-acetyl-L-lysine	-	?
additional information	TgGCN5b performs autoacetylation. Proteome-wide acetylome analyses of Toxoplasma tachyzoites identifies seven acetylated lysines on TgGCN5b, i.e. K811, K857, K941, K989, K997, K1002, and K1027	Toxoplasma gondii	?	-	-

Synonyms

Synonyms	Comment	Organism
GCN5 family KAT	-	Toxoplasma gondii
GCN5 lysine acetyltransferase	-	Toxoplasma gondii
TgGCN5b	-	Toxoplasma gondii

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Toxoplasma gondii

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
8	-	assay at	Toxoplasma gondii

Cofactor

Cofactor	Comment	Organism	Structure
acetyl-CoA	-	Toxoplasma gondii

General Information

General Information	Comment	Organism
physiological function	enzyme TgGCN5b is the only nuclear GCN5 family KAT known to be required for Toxoplasma tachyzoite replication	Toxoplasma gondii

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Release 2023.1 (January 2023)