TY  - JOUR
AU  - Leung, Macyn
AU  - Pipchuk, Alexander
AU  - Yang, Xiaolong
PY  - 2021
DA  - 2021/03/24
TI  - Current Progress in Cancer Immunotherapies Using Small Molecules Targeting PD-L1 Stability
JO  - OBM Genetics
SP  - 127
VL  - 05
IS  - 01
AB  - PD-L1 is an immune checkpoint protein that is frequently overexpressed by the cells in the tumor microenvironment. PD-L1 binds to PD-1 present on the activated antitumor T-cells, which allows for tumor immune escape. The ability of the PD-1/PD-L1 axis to suppress antitumor immunity enables its application as a potential target for small-molecule-based immunotherapies. Targeting the PD-L1-mediated tumor immune evasion represents a promising approach for immune checkpoint blockade therapies. However, the existing monoclonal antibody-based therapies present poor overall response rates, warranting the development of small molecule drugs with the ability to regulate PD-L1 stability and enhance antitumor immunity. In this context, the present review summarizes the mechanisms of upstream PD-L1 regulation by kinases, cell cycle modulators, ubiquitin ligases, and glycosylation modulators, as well as the efficacy of small molecules targeting PD-L1 stability in regulating PD-L1-mediated immune evasion.
SN  - 2577-5790
UR  - https://doi.org/10.21926/obm.genet.2101127
DO  - 10.21926/obm.genet.2101127
ID  - Leung2021
ER  -