Journal
MOLECULES
Volume 24, Issue 11, Pages -Publisher
MDPI
DOI: 10.3390/molecules24112071
Keywords
peptide-based and small synthetic molecule inhibitors; lead optimization; scaffold hopping; PD-1; PD-L1 pathway; rational drug design; cancer immunotherapy; cocrystal structures; structure-activity relationship
Funding
- European Union under the European Regional Development Fund [POIR.04.04.00-00-420F/17-00]
- European Union's Horizon 2020 research and innovation programme under the Marie Sklodowska-Curie grant [713482]
- Kanker Bestrijding (KWG grant) [10504]
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Cancer immunotherapy based on antibodies targeting the immune checkpoint PD-1/PD-L1 pathway has seen unprecedented clinical responses and constitutes the new paradigm in cancer therapy. The antibody-based immunotherapies have several limitations such as high production cost of the antibodies or their long half-life. Small-molecule inhibitors of the PD-1/PD-L1 interaction have been highly anticipated as a promising alternative or complementary therapeutic to the monoclonal antibodies (mAbs). Currently, the field of developing anti-PD-1/PD-L1 small-molecule inhibitors is intensively explored. In this paper, we review anti-PD-1/PD-L1 small-molecule and peptide-based inhibitors and discuss recent structural and preclinical/clinical aspects of their development. Discovery of the therapeutics based on small-molecule inhibitors of the PD-1/PD-L1 interaction represents a promising but challenging perspective in cancer treatment.
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