Drug intelligence / Profile preview

terriec acid

Development stage
Preclinical
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

Terreic acid is a naturally occurring metabolite produced by the fungus Aspergillus terreus. It is a quinone epoxide with notable antibiotic properties and functions as a covalent inhibitor of the bacterial cell wall biosynthetic enzyme UDP-N-acetylglucosamine 1-carboxyvinyltransferase (MurA), which catalyzes an essential step in peptidoglycan synthesis. Terreic acid inactivates MurA by covalently binding to Cys115 in the enzyme's active site. Additionally, it acts as an inhibitor of Bruton's tyrosine kinase (BTK), interfering with B-cell and mast cell activation by blocking BTK catalytic activity and its interaction with protein kinase C beta type (PKCβII). Terreic acid has demonstrated antibacterial and anticancer activities in vitro[1][3][4][7][9].

Other names
2-hydroxy-3-methyl-1,4-benzoquinone 5,6-epoxide5,6-epoxy-3-hydroxy-p-toluquinone(-)-terreic acid
02

Targets

BTK (Bruton tyrosine kinase)MurA (UDP-N-acetylglucosamine 1-carboxyvinyltransferase)

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