FRET-Based High-Throughput Screening of Small-Molecule Inhibitors of TNF Receptors

摘要

Tumor necrosis factor receptor 1(TNFRi)is a transmembrane receptor that binds tumor necrosis factor or lymphotoxin-alpha and plays a critical role in regulating the inflammatory response.Upregulation of these ligands is associated with inflammatory and autoimmune diseases.Current treatments reduce symptoms by sequestering free ligands,but this can cause adverse side effects by unintentionally inhibiting ligand binding to off-target receptors.Hence,there is a need for new small molecules that specifically target the receptors,rather than the ligands.