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Elucidating the Role of Subcellular GPCR Nanoswitches in Signaling Specificity

Project description

How tiny hubs inside cells control cell functions

Cells rely on G protein-coupled receptors (GPCRs) to sense and respond to their environment. They control vital functions such as hormone action and cell communication. Traditionally, GPCRs were thought to signal through freely moving messengers like cAMP, but this model cannot successfully explain how specific responses are achieved when multiple receptors are active. The ERC-funded CLARITY project proposes a groundbreaking idea: GPCRs form localised nanoswitches that precisely control cAMP signalling at specific locations within cells. Researchers will use cutting-edge imaging and proteomics tools to map these nanoswitches and explore their role in processes such as insulin secretion. The proposed research could transform drug discovery, enabling highly targeted therapies with fewer side effects.

Objective

G protein-coupled receptors (GPCRs) relay extracellular information across the cell membrane to mediate most physiological cell functions. Many cell-surface GPCRs stimulate the production of cyclic adenosine monophosphate (cAMP), a diffusible second messenger, to elicit receptor-specific, long-range cell functions. However, given the mobility of second messengers, this canonical model fails to explain receptor-specific functions across multiple GPCRs that signal via cAMP.

This application proposes that GPCRs, in dramatic contrast to the second messenger concept, form highly-localized, nanometer-size cAMP signaling units at various subcellular locations, i.e. subcellular GPCR nanoswitches. At these locations, GPCR nanoswitches tightly control cAMP signaling at the nanometer scale in a receptor- and location-specific manner. These nanoswitches enable cells to retain the spatial-ID of every cAMP molecule and, thus, allow precise, spatially encoded, and receptor-specific cell functions even in the presence of multiple co-activated receptors.

The combination of cutting-edge technologies such as genetically encoded Foerster resonance energy transfer (FRET)-based biosensors, fluorescence-lifetime imaging microscopy (FLIM)-FRET multiplexing, and advanced proximity proteomics, will enable mapping the architecture and dynamics of these subcellular GPCR nanoswitches at nanometer scales. This proposal will then explore how endogenous GPCR nanoswitches control insulin secretion from pancreatic beta-cells in response to endogenous incretins as well as licensed obesity drugs. This will establish the physiological relevance of subcellular GPCR nanoswitches.

If successful, this proposal has the potential to revolutionize our understanding of cell signaling and to fundamentally transform GPCR drug discovery, offering opportunities for the development of location-specific drugs with reduced side effects that precisely modulate individual subcellular GPCR nanoswitches

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Call for proposal

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(opens in new window) ERC-2025-COG

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Host institution

UNIVERSITAETSMEDIZIN DER JOHANNES GUTENBERG-UNIVERSITAET MAINZ
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 2 000 000,00
Address
Langenbeckstrasse 1
55131 Mainz
Germany

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Region
Rheinland-Pfalz Rheinhessen-Pfalz Mainz, Kreisfreie Stadt
Activity type
Higher or Secondary Education Establishments
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Total cost

The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.

€ 2 000 000,00

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