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The quest to understand heterotrimeric G protein signaling

Abstract

Over the past fifteen years, great strides have been made to understand how heterotrimeric G proteins control their downstream targets. However, the mechanism by which heterotrimeric G proteins are activated by their upstream G protein–coupled receptors (GPCRs) remains obscure. Recent structural data support the idea that GPCRs, despite their small size, are sophisticated allosteric machines with multiple signaling outputs.

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Figure 1: The heterotrimeric G protein cycle.
Figure 2: Structural transitions of GPCRs and their interactions with heterotrimeric G proteins.

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Acknowledgements

Support was provided by US National Institutes of Health grants HL086865 and HL071818.

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Correspondence to John J G Tesmer.

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Tesmer, J. The quest to understand heterotrimeric G protein signaling. Nat Struct Mol Biol 17, 650–652 (2010). https://doi.org/10.1038/nsmb0610-650

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