Nonsymmetrically Substituted 1,1′-Biphenyl-Based Small Molecule Inhibitors of the PD-1/PD-L1 Interaction
Aleksandra Hec-Gałązka,
Urszula Tyrcha,
Jan Barczyński
et al.
Abstract:Therapeutic antibodies directed against either programmed
cell
death-1 protein (PD-1) or its ligand PD-L1 have demonstrated efficacy
in the treatment of various cancers. In contrast with antibodies,
small molecules have the potential for increased tissue penetration;
better pharmacology; and therefore, improved antitumor activity. A
series of nonsymmetric C2 inhibitors were synthesized and evaluated
for PD-1/PD-L1 interaction inhibition. These compounds induced PD-L1
dimerization and effectively blocked PD-L1/… Show more
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