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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.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.3.1.48

Cloned(Commentary)

Cloned (Comment) Organism
gene GCN5B, DNA and amino acid sequence determination and analysis, real-time PCR enzyme expression analysis, recombinant expression of N-terminally HA-tagged enzyme TgGCN5b from parasites overexpressing an ectopic enzyme copy Toxoplasma gondii

Inhibitors

Inhibitors Comment Organism Structure
garcinol garcinaol inhibits TgGCN5b and mediates changes in the parasite transcriptome. Treatment of tachyzoites with garcinol leads to a reduction of global lysine acetylation, particularly on histone H3 and TgGCN5b itself 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 Toxoplasma gondii preferred substrate CoA + acetylhistone H3
-
 ?
acetyl-CoA + histone H3 Toxoplasma gondii ME49 preferred substrate CoA + acetylhistone H3
-
 ?

Organism

Organism UniProt Comment Textmining
Toxoplasma gondii S8F3V2 TgGCN5b
-
Toxoplasma gondii ME49 S8F3V2 TgGCN5b
-

Purification (Commentary)

Purification (Comment) Organism
recombinant N-terminally HA-tagged enzyme TgGCN5b from parasites overexpressing an ectopic enzyme copy by immunoaffinity chromatography 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
-
 Toxoplasma gondii CoA + acetylhistone H3
-
 ?
acetyl-CoA + histone H3 preferred substrate Toxoplasma gondii CoA + acetylhistone H3
-
 ?
acetyl-CoA + histone H3
-
 Toxoplasma gondii ME49 CoA + acetylhistone H3
-
 ?
acetyl-CoA + histone H3 preferred substrate Toxoplasma gondii ME49 CoA + acetylhistone H3
-
 ?

Synonyms

Synonyms Comment Organism
GCN5b
-
 Toxoplasma gondii
histone acetyltransferase
-
 Toxoplasma gondii
KAT
-
 Toxoplasma gondii
lysine acetyltransferase
-
 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
malfunction the dysregulated gene expression induced by garcinol inhibition of the enzyme significantly inhibits Toxoplasma tachyzoite replication without being toxic to the human host cell. Garcinol inhibits TgGCN5b KAT activity and reduces global lysine acetylation in vivo in treated parasites, including its preferred substrate, histone H3 Toxoplasma gondii
physiological function lysine acetylation is a critical post-translational modification that influences protein activity, stability, and binding properties. The acetylation of histone proteins in particular is a feature of gene expression regulation. TgGCN5b is the only nuclear GCN5-family KAT known to be required for Toxoplasma tachyzoite replication Toxoplasma gondii