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Table 3 Potential drugs intervening PD-L1 and CTLA-4

From: Regulatory mechanisms of immune checkpoints PD-L1 and CTLA-4 in cancer

Drugs

Mechanism

PD-L1 or CTLA-4

Cancer types

References

PD-L1

metformin

phosphorylating oncogene YAP1

Downregulation

CRC

[243]

MS NPs

 

Downregulation

breast cancer

[244]

PARPi

inactivating GSK3β

Upregulation

breast cancer

[245]

TMZ

 

Upregulation

GBM

[246]

actinomycin D

 

Downregulation

GBM

[246]

Pemetrexed and sildenafil

 

Downregulation

NSCLC

[247]

AR42 and valproate

inhibiting histone deacetylase

Downregulation

NSCLC

[247]

DSF/Cu2+

inactivating PARP1 and phosphorylating GSK3βat Ser9

Upregulation

HCC

[248]

ipatasertib, capivasertib, uprosertib, and MK-2206

inhibiting Akt

Downregulation

breast cancer

[249]

DS-8201a

targeting HER2

Upregulation

breast cancer

[250]

Verteporfin

inhibiting STAT1-IRF1-TRIM28 signaling cascade

Downregulation

T-cell leukemia, B-cell leukemia, ovarian, osteoblastoma, and NSCLC

[251]

LY294002

inhibiting PI3K

Downregulation

gastric cancer

[61]

cetuximab, erlotinib, and selumetinib

inhibiting MAPK signaling

Downregulation

LUAD

[57]

trametinib

inhibiting MAPK signaling

Upregulation

breast cancer

[56]

Belinostat

inducing IFN-γ

Upregulation

HCC

[252]

C108

Inhibiting G3BP2

Downregulation

GBM

[139]

Pembrolizumab

inhibiting interaction of PD-L1 with PD-1

 

urothelial cancer, melanoma, HNSCC, and NSCLC

[253]

Nivolumab and Atezolizumab

inhibiting interaction of PD-L1 with PD-1

 

NSCLC, urothelial cancer, RCC, and melanoma

[253]

Durvalumab and Avelumab

inhibiting interaction of PD-L1 with PD-1

 

urothelial cancer

[253]

Envafolimab

inhibiting interaction of PD-L1 with PD-1

 

prostate cancer, NSCLC, breast cancer, gastrointestinal cancer, melanoma, cervical cancer, HNSCC, bladder cancer, cholangiocarcinoma

[254]

MDX-1105 and CS-1001

inhibiting interaction of PD-L1 with PD-1

 

NSCLC, melanoma, RCC

[9]

CK-301

inhibiting interaction of PD-L1 with PD-1

 

NSCLC, HNSCC, melanoma, RCC, urothelial cancer, Hodgkin’s lymphoma

[254]

TQB-2450

inhibiting interaction of PD-L1 with PD-1

 

melanoma

[254]

BGB-A333

inhibiting interaction of PD-L1 with PD-1

 

advanced solid tumor

[254]

CTLA-4

Ipilimumab

inhibiting interaction of CTLA-4 with B7

 

RCC, prostate cancer, cervical cancer, CRC, NSCLC, gastric cancer, pancreatic cancer, ovarian cancer, urothelial cancer, and melanoma

[255]

Tremelimumab

inhibiting interaction of CTLA-4 with B7

 

HCC

[256]

p344

inhibiting interaction of CTLA-4 with B7

  

[257]

SAHA

 

Downregulation

 

[258]

CKD-L

 

Upregulation

 

[259]