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Table 1 Therapeutic targets being explored in ARID1A mutated cancers

From: EZH2 inhibition in ARID1A mutated clear cell and endometrioid ovarian and endometrioid endometrial cancers

EZH-2

Epigenetic synthetic lethality, promotion of apoptosis

GSK126

[33, 34]

PIK3IP1 mediated inhibition of PI3K/AKT pathway

mTOR

Inhibition of downstream regulator of PI3K/AKT pathway

Temsirolimus

[35, 36]

Ridaforolimuus

Everolimus

AP23573

TP53

Stabilization of wild-type p53 to overcome ARID1A loss, resume tumor suppressor function

Nutlin 3

[13, 37]

PI3K/AKT

Inhibit upregulated AKT phosphorylation caused by concurrent mutations

Sorafenib

[38, 39]

Copanlisib

[36]

BKM120

 

XL147

BRCA

Enhance DNA-damaging effects of platinum chemotherapies

EZH2 modulated function of BRCA1

 

[40, 41]

ARID1B

Inhibition of residual AWI/SNF complex to suppress cell growth

 

[42, 43]

Anti-IL6

Inhibit inflammatory microenvironment and escape from anti-tumor immune response

 

[44]