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 | Â | Downregulation | breast cancer | [244] | |
PARPi | inactivating GSK3β | Upregulation | breast cancer | [245] | |
TMZ | Â | Upregulation | GBM | [246] | |
actinomycin D | Â | Downregulation | GBM | [246] | |
Pemetrexed and sildenafil | Â | 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 | Â | urothelial cancer, melanoma, HNSCC, and NSCLC | [253] | |
Nivolumab and Atezolizumab | inhibiting interaction of PD-L1 with PD-1 | Â | NSCLC, urothelial cancer, RCC, and melanoma | [253] | |
Durvalumab and Avelumab | inhibiting interaction of PD-L1 with PD-1 | Â | urothelial cancer | [253] | |
Envafolimab | inhibiting interaction of PD-L1 with PD-1 | Â | 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 | Â | 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 | Â | melanoma | [254] | |
BGB-A333 | inhibiting interaction of PD-L1 with PD-1 | Â | advanced solid tumor | [254] | |
CTLA-4 | Ipilimumab | inhibiting interaction of CTLA-4 with B7 | Â | 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 | Â | HCC | [256] | |
p344 | inhibiting interaction of CTLA-4 with B7 | Â | Â | [257] | |
SAHA | Â | Downregulation | Â | [258] | |
CKD-L | Â | Upregulation | Â | [259] |