GPCR antagonism via rewiring of receptor trafficking and degradation
G protein–coupled receptors (GPCRs) represent one of the most important yet incompletely addressed classes of therapeutic targets1. Here, we report a novel strategy for functional GPCR antagonism via bispecific antibody-mediated endocytosis and lysosomal degradation. GPCR-TfR1 targeting chimeras (GTACs) achieve potent...