Discovery of the first-efficacious A2AR negative allosteric modulators for high adenosine cancer immunotherapies
Margot Boujut, Margaux Héritier, Aurélie Gouiller, Camille Süess, Alessandro Scapozza, Thibaut De Smedt, M. Guibert, Sébastien Tardy, Hesham M. Ismail, David Pejoski, Léonardo Scapozza
The paper identifies potent A2AR negative allosteric modulators through high-throughput screening and SAR analysis, showing their efficacy in high-adenosine conditions for safer cancer immunotherapies.
Journal of Medicinal Chemistry · Jan 24, 2025Peer-reviewedPharmacology & Toxicology