Unknown

Dataset Information

0

Small molecule inhibitors against PD-1/PD-L1 immune checkpoints and current methodologies for their development: a review.


ABSTRACT: Programmed death-1/programmed death ligand-1 (PD-1/PD-L1) based immunotherapy is a revolutionary cancer therapy with great clinical success. The majority of clinically used PD-1/PD-L1 inhibitors are monoclonal antibodies but their applications are limited due to their poor oral bioavailability and immune-related adverse effects (irAEs). In contrast, several small molecule inhibitors against PD-1/PD-L1 immune checkpoints show promising blockage effects on PD-1/PD-L1 interactions without irAEs. However, proper analytical methods and bioassays are required to effectively screen small molecule derived PD-1/PD-L1 inhibitors. Herein, we summarize the biophysical and biochemical assays currently employed for the measurements of binding capacities, molecular interactions, and blocking effects of small molecule inhibitors on PD-1/PD-L1. In addition, the discovery of natural products based PD-1/PD-L1 antagonists utilizing these screening assays are reviewed. Potential pitfalls for obtaining false leading compounds as PD-1/PD-L1 inhibitors by using certain binding bioassays are also discussed in this review.

SUBMITTER: Liu C 

PROVIDER: S-EPMC8077906 | biostudies-literature |

REPOSITORIES: biostudies-literature

Similar Datasets

| S-EPMC7584369 | biostudies-literature
| S-EPMC5641120 | biostudies-literature
| S-EPMC10817355 | biostudies-literature
| S-EPMC6712002 | biostudies-literature
| S-EPMC8125578 | biostudies-literature
| S-EPMC8199613 | biostudies-literature
| S-EPMC9866166 | biostudies-literature
| S-EPMC8178863 | biostudies-literature
| S-EPMC8952773 | biostudies-literature
| S-EPMC7523356 | biostudies-literature