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Literature summary for 2.3.1.108 extracted from

  • Fiorentino, F.; Mai, A.; Rotili, D.
    Lysine acetyltransferase inhibitors structure-activity relationships and potential therapeutic implications (2018), Future Med. Chem., 10, 1067-1091 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
additional information analysis of KATi, bisubstrate analogues, natural compounds and synthetic derivatives, mechanism of action, structure-activity relationships, and pharmacokinetic/pharmacodynamic properties, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acetyl-CoA + [alpha-tubulin]-L-lysine40 Homo sapiens
-
CoA + [alpha-tubulin]-N6-acetyl-L-lysine40
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q5SQI0
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + [alpha-tubulin]-L-lysine40
-
Homo sapiens CoA + [alpha-tubulin]-N6-acetyl-L-lysine40
-
?
additional information the enzyme shows tubulin-specific acetylation activity Homo sapiens ?
-
-

Synonyms

Synonyms Comment Organism
alpha-tubulin N-acetyltransferase 1 UniProt Homo sapiens
alphaTAT1
-
Homo sapiens
ATAT1
-
Homo sapiens
KAT
-
Homo sapiens
lysine acetyltransferase
-
Homo sapiens

General Information

General Information Comment Organism
malfunction the dysregulation of this enzyme activity is implicated in many human pathologies such as cancer, neurological and inflammatory disorders Homo sapiens
additional information despite having a tertiary structure similar to that of Gcn5, alphaTAT1 contains a relatively wide substrate binding pocket and unique structural elements that play an essential role in alpha-tubulin-specific acetylation, which is associated with many cellular processes connected to cancer dissemination such as cell adhesion, migration and invasion, tertiary enzyme structure in complex with acetyl-CoA (PDB ID 4gs4) Homo sapiens
physiological function lysine acetylation is a post-translational modification of both histone and nonhistone proteins that is catalyzed by lysine acetyltransferases and plays a key role in numerous biological contexts. Enzyme alphaTAT1 is involved in cell adhesion, migration, and invasion. It is the main KAT responsible for alpha-tubulin acetylation at Lys40 in higher organisms Homo sapiens