This study identifies and characterizes novel small-molecule inhibitors that disrupt the PD-1/PD-L1 interaction, aiming to enhance antitumor immune responses. Utilizing in silico screening, in vitro assays, and in vivo models, the researchers demonstrated that these compounds promote T-cell activation and infiltration into tumors. Notably, compound 69 showed significant efficacy in restoring T-cell function and reducing tumor growth.
The novel small-molecule inhibitors effectively block PD-1/PD-L1 interactions, leading to enhanced cytotoxic T-cell infiltration and antitumor activity in humanized mouse models, highlighting their potential as immunotherapeutic agents.
Humanized PD-1 Knockin mouse model developed by genOway, engineered to express the human extracellular domain of PD-1, enabling the evaluation of human-specific PD-1/PD-L1 interactions and therapeutics in vivo.
Cancer immunotherapy, PD-1/PD-L1 blockade, Small-molecule inhibitors, T-cell activation, Tumor microenvironment
Humanized Knockin model, PD-1 extracellular domain replacement, Immune checkpoint modulation, In vivo efficacy studies
From model design to experimental results
Tailor-made solutions adapted to scientific questions
Comprehensive dataset package
Generated with biopharma partners and in-house
Scientific follow-up and advice along the project
Collaborative approach for problem solving and development of innovative models
Breeding facilities in US and Europe
Certified health status from professional breeders
