Conventional allosteric modulators of G protein–coupled receptors (GPCRs) bind their target from the extracellular site. A new study shows that a GPCR's intracellular face can likewise be exploited. In particular, they sensitize a class B GPCR for activation by a hardly active peptide-hormone metabolite.
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Mohr, K., Kostenis, E. A GPCR's back door. Nat Chem Biol 10, 609–610 (2014). https://doi.org/10.1038/nchembio.1583
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DOI: https://doi.org/10.1038/nchembio.1583
