Beyond IC 50 : Reframing Microcystin Potency against Protein Phosphatase 2A by Defining Two-Step Irreversible Inhibition Kinetics

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Authors: Kelli N. Hummel, Blake B. Stringer, Sharmila I. Thenuwara, Judy A. Westrick, Jeremy J. Kodanko
Cited by: 1
References: 58

Abstract

] MC-RR binds PP2A with picomolar affinity despite lacking a highly reactive electrophile, demonstrating that high-affinity engagement is mechanistically separable from covalent inactivation. These results reveal that MC potency is driven by exceptionally tight and persistent PP2A binding rather than fast reactivity, providing a kinetic framework that links molecular structure to sustained phosphatase inactivation and real-world toxicity during harmful algal bloom exposure.

Fields of Study & Subjects

Aquatic Ecosystems and Phytoplankton Dynamics Microtubule and mitosis dynamics Protein Kinase Regulation and GTPase Signaling

Publication details

Journal / source
ACS Omega
Publisher
American Chemical Society (ACS)
Volume
11
Issue
19
Pages
29202–29210
Publication date
30 April 2026
Language
EN