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Bridging biophysics and cell biology: The role of G protein-coupled receptor conformations in signalling

Objective

G protein coupled receptors (GPCRs) are a class of membrane receptors that transmits extracellular signals into the cell. They can be activated by a diverse set of ligands including small molecules, hormones, neurotransmitters or photons and are targeted by a third of currently marketed drugs. Endogenous ligands and drugs may exhibit different efficacy profiles, ranging from full activation to complete inactivation of a signalling pathway. The key to the selective interaction with signalling partners in response to ligand binding lies in the conformational flexibility of the membrane receptors. Previous research has extensively studied the three-dimensional structures of GPCRs and their signalling. However, the link between active conformations and signalling is still missing.
In the proposed project, first I will use exhaustive single-point mutagenesis coupled to functional assays to determine how the sequence and secondary structure of GPCRs contribute to signaling. Second, biophysical techniques studying protein conformations will help us to understand the connection between conformations and signalling outcome. These techniques give insights into the conformational fingerprints of the receptor. The link to signalling will be achieved by biasing the receptor towards a selected signalling partner either though addition of the selected signalling partner or the insertion of specific mutations tested in the first part of the project. Finally, I will use computational techniques to compare the activation of signalling partners in different GPCRs.
With my research I hope to improve our understanding of the molecular basis of membrane protein function and contribute to the development of strategies for the design of more specific drugs with fewer side effects.

Fields of science (EuroSciVoc)

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Programme(s)

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Topic(s)

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Funding Scheme

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MSCA-IF - Marie Skłodowska-Curie Individual Fellowships (IF)

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Call for proposal

Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.

(opens in new window) H2020-MSCA-IF-2018

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Coordinator

UNITED KINGDOM RESEARCH AND INNOVATION
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.

€ 271 732,80
Address
POLARIS HOUSE NORTH STAR AVENUE
SN2 1FL SWINDON
United Kingdom

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Region
South West (England) Gloucestershire, Wiltshire and Bristol/Bath area Swindon
Activity type
Research Organisations
Links
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.

€ 271 732,80

Partners (1)

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