Targeting G protein-coupled receptor signalling by blocking G proteins

Targeting G protein-coupled receptor signalling by blocking G proteins

Targeting G protein-coupled receptor signalling by blocking G proteins, Published online: 28 September 2018; doi:10.1038/nrd.2018.135

Identifying ligands of G protein-coupled receptors (GPCRs) that elicit biased downstream signalling is an established strategy for separating the desired and unwanted effects of these receptors. Campbell and Smrcka describe how inhibiting the downstream G proteins themselves could also be used to bias GPCR signalling, as well as block pathways shared by multiple GPCRs involved in complex diseases, and discuss how the currently available G protein ligands could be optimized to generate therapeutic leads.

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