Abstract
A two-component system (TCS) comprising a histidine kinase (HK) sensor and a response regulator (RR) plays important roles in regulating the virulence of many pathogenic bacteria. We used a new screening method to isolate novel inhibitor Art1 against bacterial sensory HK from an acetone extract of solid cultures of Articulospora sp., an aquatic hypomycete. Art1 inhibited the ATP-dependent autophosphorylation of recombinant glutathione S-transferase-fusion protein SasA, a cyanobacterial HK, with an IC50 value of 9.5 microg/ml.
MeSH terms
-
Ascomycota / chemistry
-
Ascomycota / metabolism*
-
Cyanobacteria / enzymology*
-
Histidine Kinase
-
Magnetic Resonance Spectroscopy
-
Molecular Structure
-
Naphthols / chemistry*
-
Naphthols / isolation & purification
-
Naphthols / metabolism
-
Naphthols / pharmacology*
-
Protein Kinase Inhibitors / chemistry*
-
Protein Kinase Inhibitors / isolation & purification
-
Protein Kinase Inhibitors / metabolism
-
Protein Kinase Inhibitors / pharmacology*
-
Protein Kinases / metabolism*
Substances
-
Art1 compound
-
Naphthols
-
Protein Kinase Inhibitors
-
Protein Kinases
-
Histidine Kinase