Hot spots for GPCR signaling: lessons from single-molecule microscopy

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Hot spots for GPCR signaling: lessons from single-molecule microscopy. / Calebiro, Davide; Jobin, Marie-Lise.

In: Current Opinion in Cell Biology, Vol. 57, 03.12.2018, p. 57-63.

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@article{a23dad06d5c4436591f6d1627ccd46b2,
title = "Hot spots for GPCR signaling: lessons from single-molecule microscopy",
abstract = "G protein-coupled receptors (GPCRs) are among the best-studied membrane receptors, mainly due to their central role in human physiology, involvement in disease and relevance as drug targets. Although biochemical and pharmacological studies have characterized the main steps in GPCR signaling, how GPCRs produce highly specific responses in our cells remains insufficiently understood. New developments in single-molecule microscopy have made it possible to study the protein–protein interactions at the basis of GPCR signaling in previously inconceivable detail. Using this approach, it was recently possible to follow individual receptors and G proteins as they diffuse, interact and signal on the surface of living cells. This has revealed hot spots on the plasma membrane, where receptors and G proteins undergo transient interactions to produce rapid and local signals. Overall, these recent findings reveal a high degree of dynamicity and complexity in signaling by GPCRs, which provides a new basis to understand how these important receptors produce specific effects and might pave the way to innovative pharmacological approaches.",
author = "Davide Calebiro and Marie-Lise Jobin",
year = "2018",
month = dec,
day = "3",
doi = "10.1016/j.ceb.2018.11.003",
language = "English",
volume = "57",
pages = "57--63",
journal = "Current Opinion in Cell Biology",
issn = "0955-0674",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Hot spots for GPCR signaling: lessons from single-molecule microscopy

AU - Calebiro, Davide

AU - Jobin, Marie-Lise

PY - 2018/12/3

Y1 - 2018/12/3

N2 - G protein-coupled receptors (GPCRs) are among the best-studied membrane receptors, mainly due to their central role in human physiology, involvement in disease and relevance as drug targets. Although biochemical and pharmacological studies have characterized the main steps in GPCR signaling, how GPCRs produce highly specific responses in our cells remains insufficiently understood. New developments in single-molecule microscopy have made it possible to study the protein–protein interactions at the basis of GPCR signaling in previously inconceivable detail. Using this approach, it was recently possible to follow individual receptors and G proteins as they diffuse, interact and signal on the surface of living cells. This has revealed hot spots on the plasma membrane, where receptors and G proteins undergo transient interactions to produce rapid and local signals. Overall, these recent findings reveal a high degree of dynamicity and complexity in signaling by GPCRs, which provides a new basis to understand how these important receptors produce specific effects and might pave the way to innovative pharmacological approaches.

AB - G protein-coupled receptors (GPCRs) are among the best-studied membrane receptors, mainly due to their central role in human physiology, involvement in disease and relevance as drug targets. Although biochemical and pharmacological studies have characterized the main steps in GPCR signaling, how GPCRs produce highly specific responses in our cells remains insufficiently understood. New developments in single-molecule microscopy have made it possible to study the protein–protein interactions at the basis of GPCR signaling in previously inconceivable detail. Using this approach, it was recently possible to follow individual receptors and G proteins as they diffuse, interact and signal on the surface of living cells. This has revealed hot spots on the plasma membrane, where receptors and G proteins undergo transient interactions to produce rapid and local signals. Overall, these recent findings reveal a high degree of dynamicity and complexity in signaling by GPCRs, which provides a new basis to understand how these important receptors produce specific effects and might pave the way to innovative pharmacological approaches.

U2 - 10.1016/j.ceb.2018.11.003

DO - 10.1016/j.ceb.2018.11.003

M3 - Abstract

VL - 57

SP - 57

EP - 63

JO - Current Opinion in Cell Biology

JF - Current Opinion in Cell Biology

SN - 0955-0674

ER -