Microcystin analogues comprised only of Adda and a single additional amino acid retain moderate activity as PP1/PP2A inhibitors.
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.
Gulledge
Brian M
BM
Department of Chemistry, University of California at Irvine, 92697, USA.
Aggen
James B
JB
Eng
Hugo
H
Sweimeh
Khuloud
K
Chamberlin
A Richard
AR
D000596:Amino Acids / Q000737:chemistry*; D001427:Bacterial Toxins; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D008387:Marine Toxins; D052998:Microcystins; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000494:pharmacology*; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000596:Amino Acids; D001427:Bacterial Toxins; D004791:Enzyme Inhibitors; D007527:Isoenzymes; D008387:Marine Toxins; D052998:Microcystins; D010456:Peptides, Cyclic; C078588:microcystin; D010749:Phosphoprotein Phosphatases; C057862:cyanoginosin LR