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Table 1 Direct PP2A activators

From: Altering phosphorylation in cancer through PP2A modifiers

Compounds

Cancer types

Mechanisms

References

SMAPs:

DT-061

DT-1154

DT-794

DT-382

Burkitt’s Lymphoma

Myc degradation via dephosphorylation at Ser62

[55, 62]

KRAS mutant NSCLC

Triple Negative Breast Cancer

Multidrug resistant chronic lymphocytic leukemia (CLL)

Apoptosis activation through inducing mitochrondrial permeability transition pores (mPTPs)

[63]

Glioblastoma

Blood–Brain Barrier Permeable

[134]

TKI-resistant advanced lung adenocarcinoma

Downregulation of PI3K and MAPK pathways

[61]

Neuroblastoma

Decreased MYCN

[68]

iHAP1

T-ALL

Dephosphorylates MYBL2

Inhibits tubulin polymerization

[64, 69]

Perphenazine

T-ALL

Dephosphorylates c-Myc, AKT1, p70S6K, ERK, and BAD

[58,59,60, 69]

NSC49L

Colorectal Cancer

Decreased AKT11, mTOR, 4E-BP1, p21

[70]

5-FU resistant Colorectal Cancer

ATUX-792

Neuroblastoma

Decreased MYCN (prognostic factor for neuroblastoma)

[68]

ATUX-3364

Hepatoblastoma

Decreased cell cycle progression, motility, and stemness, decreased mRNA expression of OCT4, NANOG, SOX2

[67]

ATUX-8385

Forskolin

Colorectal cancer

Dephosphorylates PP2Ac

[135]

Acute myeloid leukemia

Caspase-dependent apoptosis, decreased phosphorylated Akt and ERK1/2

[24]

Metformin

Breast Cancer

Decreased phosphorylated Bax, c-Myc, and AKT1

[71, 72]

Lung Cancer

Prostate Cancer

Sodium selenate

Castration-resistant prostate cancer

Decreased angiogenesis

[73,74,75]

Hormone-refractory prostate cancer