Science  21 Sep 2018:
Vol. 361, Issue 6408, pp. 1211-1213
DOI: 10.1126/science.361.6408.1211-r


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The effect of a drug on a G protein–coupled receptor (GPCR) can be determined by monitoring the downstream effects of that receptor, but not for GPCRs whose signaling pathways are unclear. Yanagawa et al. performed single-molecule imaging of different GPCRs in the plasma membrane. They found that the diffusion dynamics correlated with whether the interacting drug activated or inhibited the receptor, resulted in the coupling of GPCRs to G proteins, or induced receptor endocytosis. Thus, analyzing the diffusion of a GPCR provides an estimate for the effect of a candidate drug.

Sci. Signal. 11, eaao1917 (2018).





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