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Table 2 Indirect PP2A activators

From: Altering phosphorylation in cancer through PP2A modifiers

Compounds

Cancer Types

Mechanisms

References

FTY720

Acute myeloid leukemia

Impairs interaction of PP2Ac with SET

[81]

Neuroblastoma

Inhibits proliferation, migration, and invasion

[68, 136]

Chronic myeloid leukemia

Impairs interaction of SET-PP2A, inhibits the BCR-ABL1 recruitment of JAK2, and activates GSK-3β

[137]

Colorectal cancer

Decreased phosphorylation of AKT1 and Erk1/2

[79]

Breast cancer

Increases activation and expression of ERα and inhibits histone deacetylase

[23, 138]

Oral squamous cell carcinoma

Decreased phosphorylated GSK-3β

[25]

Multiple myeloma

Ferroptosis, autophagy, apoptosis, and ROS activation

[84, 85]

Ovarian cancer

Autophagy and non-apoptotic cell death

[88]

Gastric cancer

Increases PTEN and p53,

decreases p-AKT1 and MDM2,

induces G1 cell cycle arrest and apoptosis

[87]

Lung cancer

Decreases S1P-induced IL-6 and IL-8 and TNF-induced COX2, activation of PP2A-RIPK1-dependent necroptosis

[82, 86]

Hepatocellular carcinoma

ROS-dependent activation of PKCδ and caspase-3-dependent apoptosis

[139]

CM-1231

Acute myeloid leukemia

Targets SET

[91]

OSU-2S

Acute myeloid leukemia

Impairs interaction of SET and PP2Ac, c-Myc degradation and increased p21

[90]

Chronic lymphocytic leukemia

Nuclear translocation of SHP1S591

[89]

OP449

Acute myeloid leukemia

Antagonizes SET

[81, 140]

Chronic myeloid leukemia

[140]

Bortezomib

Triple negative breast cancer

Inhibits CIP2A, decreased p-AKT1

[78, 79]

Colorectal cancer

  

Ethoxysanguinarine (ESG)

Lung cancer

Inhibits CIP2A, decreased c-Myc and p-AKT1, apoptosis

[94]

TD52

Triple negative breast cancer

Inhibits CIP2A, interrupts ELK1 binding to CIP2A promoter, decreased p-AKT1

[93]

Hepatocellular carcinoma

[95]

Arctigenin

Triple negative breast cancer

Inhibits CIP2A

[141]

Celastrol

Gastric cancer

CIP2A degradation, increased apoptosis

[142]

Niclosamide

Non-small cell lung cancer

Inhibits CIP2A, increased mitochondrial ROS

[143]

Polyphyllin I

Prostate cancer

Inhibits CIP2A and ERK

[99]

Lapatinib

Triple negative breast cancer

Inhibits CIP2A and p-AKT1

[98]