
Revolutionary drug development method eliminates side effects.
Japanese researchers have discovered a new way of activating G protein-coupled receptors (GPCRs) by triggering shape changes in the intracellular region of the receptor, which can help design drugs with fewer or no side effects. The team synthesized a non-peptide message molecule called PCO371, which binds to the intracellular region of the receptor and interacts directly with G protein subunits, making it a suitable candidate for potential small-molecule-based drugs for class B1 GPCRs, like PTH1R, which currently lack oral administrative drug ligands.
