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A new era of GPCR structural and chemical biology

G protein–coupled receptors (GPCRs) are versatile molecular machines that regulate the majority of physiological responses to chemically diverse hormones and neurotransmitters. Recent breakthroughs in structural studies have advanced our understanding of GPCR signaling, particularly the selectivity of ligand recognition and receptor activation of G proteins.

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Figure 1: Diversity of ligand binding domains in class A GPCRs.
Figure 2: Comparison of binding pockets within receptor subtypes.
Figure 3: Potential domains to target for regulating receptor function.

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Correspondence to Brian Kobilka.

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Granier, S., Kobilka, B. A new era of GPCR structural and chemical biology. Nat Chem Biol 8, 670–673 (2012). https://doi.org/10.1038/nchembio.1025

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