Target intelligence / Profile preview

Protein Phosphatase 2A (PP2A)

Target
PP2A
Molecular classification
Enzyme, Serine/threonine protein phosphatase
01

Overview

Protein Phosphatase 2A (PP2A) is a major serine/threonine phosphatase that is highly conserved across eukaryotes and plays essential roles in regulating numerous cellular processes. It regulates cell proliferation, signal transduction, apoptosis, DNA repair, and cytoskeletal organization by dephosphorylating key signaling molecules such as Akt, p53, c-Myc, and β-catenin. It functions as a heterotrimeric holoenzyme composed of three subunits: Catalytic (C), Scaffolding (A), and Regulatory (B). Historically recognized as a tumor suppressor, pharmacological inhibition has shown therapeutic potential in some contexts.

02

Mechanism of action

Modulation of PP2A activity

03

Biological functions

DephosphorylationCell cycleApoptosisSignal transductionCell proliferationCytoskeletal organizationImmune response
04

Disease associations

Cancer
05

Safety considerations

Potential for off-target effects due to broad substrate specificityParadoxical effects (tumor suppressor vs. therapeutic target)
06

Interacting drugs

LB100

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