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Open access Sep 2026

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...

Kaitlin Rhee, L. Shue, Akimasa Adachi et al. · 0 citations

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