Inhibitory effect of a marine-sponge toxin, okadaic acid, on protein phosphatases. Specificity and kinetics

Biochem J. 1988 Nov 15;256(1):283-90. doi: 10.1042/bj2560283.

Abstract

The inhibitory effect of a marine-sponge toxin, okadaic acid, was examined on type 1, type 2A, type 2B and type 2C protein phosphatases as well as on a polycation-modulated (PCM) phosphatase. Of the protein phosphatases examined, the catalytic subunit of type 2A phosphatase from rabbit skeletal muscle was most potently inhibited. For the phosphorylated myosin light-chain (PMLC) phosphatase activity of the enzyme, the concentration of okadaic acid required to obtain 50% inhibition (ID50) was about 1 nM. The PMLC phosphatase activities of type 1 and PCM phosphatase were also strongly inhibited (ID50 0.1-0.5 microM). The PMCL phosphatase activity of type 2B phosphatase (calcineurin) was inhibited to a lesser extent (ID50 4-5 microM). Similar results were obtained for the phosphorylase a phosphatase activity of type 1 and PCM phosphatases and for the p-nitrophenyl phosphate phosphatase activity of calcineurin. The following phosphatases were not affected by up to 10 microM-okadaic acid: type 2C phosphatase, phosphotyrosyl phosphatase, inositol 1,4,5-trisphosphate phosphatase, acid phosphatases and alkaline phosphatases. Thus okadaic acid had a relatively high specificity for type 2A, type 1 and PCM phosphatases. Kinetic studies showed that okadaic acid acts as a non-competitive or mixed inhibitor on the okadaic acid-sensitive enzymes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcineurin
  • Calmodulin-Binding Proteins / antagonists & inhibitors
  • Dose-Response Relationship, Drug
  • Ethers, Cyclic / pharmacology*
  • Kinetics
  • Marine Toxins / pharmacology*
  • Okadaic Acid
  • Phosphoprotein Phosphatases / antagonists & inhibitors*
  • Polyamines*
  • Polyelectrolytes
  • Polymers / pharmacology
  • Porifera / analysis*

Substances

  • Calmodulin-Binding Proteins
  • Ethers, Cyclic
  • Marine Toxins
  • Polyamines
  • Polyelectrolytes
  • Polymers
  • polycations
  • Okadaic Acid
  • Calcineurin
  • Phosphoprotein Phosphatases