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- W2015585963 abstract "Costimulatory molecules are important regulators of T cell activation and thus favored targets for therapeutic manipulation of immune responses. One of the key costimulatory receptors is CD80, which binds the T cell ligands, CD28, and CTLA-4. We describe a set of small compounds that bind with high specificity and low nanomolar affinity to CD80. The compounds have relatively slow off-rates and block both CD28 and CTLA-4 binding, implying that they occlude the shared ligand binding site. The compounds inhibit proinflammatory cytokine release in T cell assays with submicromolar potency, and as such, they represent promising leads for the development of novel therapeutics for immune-mediated inflammatory disease. Our results also suggest that other predominantly β proteins, such as those that dominate the cell surface, may also be accessible as potentially therapeutic targets." @default.
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- W2015585963 date "2004-12-01" @default.
- W2015585963 modified "2023-09-23" @default.
- W2015585963 title "High-Affinity Small Molecule Inhibitors of T Cell Costimulation: Compounds for Immunotherapy" @default.
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- W2015585963 doi "https://doi.org/10.1016/j.chembiol.2004.09.011" @default.
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