Abstract
A series of greatly simplified microcystin analogues comprised only of Adda (the beta-amino acid common to the microcystins, nodularins, and motuporin,) and a single additional amino acid residue was synthesized and screened for inhibition of the protein phosphatases 1 and 2A. Several of the analogues were shown to be mid-nanomolar inhibitors of the enzymes.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Amino Acids / chemistry*
-
Bacterial Toxins
-
Enzyme Inhibitors / chemistry*
-
Enzyme Inhibitors / pharmacology
-
Inhibitory Concentration 50
-
Isoenzymes / antagonists & inhibitors
-
Marine Toxins
-
Microcystins
-
Peptides, Cyclic / chemistry*
-
Peptides, Cyclic / pharmacology*
-
Phosphoprotein Phosphatases / antagonists & inhibitors*
-
Structure-Activity Relationship
Substances
-
Amino Acids
-
Bacterial Toxins
-
Enzyme Inhibitors
-
Isoenzymes
-
Marine Toxins
-
Microcystins
-
Peptides, Cyclic
-
microcystin
-
Phosphoprotein Phosphatases
-
cyanoginosin LR