Target intelligence / Profile preview

Protein phosphatase 2 regulatory subunit B alpha (PPP2R2A) (PPP2R2A)

Target
PPP2R2A
Molecular classification
Phosphatase regulatory subunit, Protein phosphatase 2A (PP2A) subunit, Tumor suppressor
01

Overview

Protein phosphatase 2 regulatory subunit B alpha (PPP2R2A), also known as B55alpha, is a critical regulatory component of the Protein Phosphatase 2A (PP2A) holoenzyme, which serves as a major serine/threonine phosphatase in eukaryotic cells [1, 2]. PPP2R2A specifically directs the PP2A catalytic core to substrates involved in cell cycle progression, DNA damage repair, and survival signaling pathways such as AKT and MAPK [2, 4]. In many human cancers, particularly prostate, breast, and colorectal carcinomas, PPP2R2A is frequently downregulated or genomically deleted, functioning as a tumor suppressor whose loss promotes uncontrolled proliferation and genomic instability [3]. While direct therapeutic targeting of the PPP2R2A mRNA or protein remains an area of active research, its absence serves as a significant biomarker for synthetic lethality approaches, such as the use of PARP or WEE1 inhibitors [3]. Current pharmacological efforts include the development of Small Molecule Activators of PP2A (SMAPs) that aim to stabilize the PPP2R2A-PP2A complex and restore its phosphatase activity to suppress tumor growth [4].

Other names
B55AB55-ALPHAPR52APR55AB55alphaPPP2R2A mRNA
02

Mechanism of action

Activation of the PP2A-B55alpha complex to restore phosphatase activity; synthetic lethality via PARP or WEE1 inhibition in the context of PPP2R2A deficiency.

03

Biological functions

Cell cycle regulationDNA damage responseSignal transductionApoptosisMitotic exitTau dephosphorylation
04

Disease associations

CancerAlzheimer's diseaseProstate cancerBreast cancerColorectal cancer
05

Safety considerations

Potential for systemic toxicity due to broad PP2A activityRisk of promoting tumor growth if PP2A is inhibitedChallenges in achieving isoform-specific modulation
06

Interacting drugs

LB-100

4 more in the full profile.

07

Biomarkers

PPP2R2A genomic lossPPP2R2A mRNA expression levelsB55alpha protein expression

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