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Kinase Regulation by Phase Separation

Project description

Protein kinase action in phase-separated condensates

The addition of phosphates to proteins – protein phosphorylation – is an important regulatory mechanism in biological and cellular functions. Dysfunction of the protein kinases responsible for phosphorylation is associated with diseases including Alzheimer’s and cancer. These important drug targets are likely regulated spatially and temporally as part of so-called phase-separated condensates, clusters of biomolecules into organelles without conventional membranes. ERC-funded PhaseKin project aims to shed light on the molecular mechanisms governing kinase action in phase-separated condensates. The project will study in atomic detail the action of protein kinases intimately involved in Alzheimer’s disease, paving the way to more specific and effective drugs targeting kinases.

Objective

Protein phosphorylation is a process that activates biological and cellular pathways. This process is carried out by enzymes called protein kinases that add phosphates to proteins. Protein kinases are crucial drug targets involved in the onset and progression of human diseases such as cancer and Alzheimers disease. Growing evidence suggests that protein kinases are regulated spatially and temporally by the phase separation and condensation of biomolecules into cellular organelles that are not surrounded by membranes. The molecular mechanisms that govern the action of kinases in phase-separated condensates, however, are unknown. Knowledge of these mechanisms is crucial for the development of better drugs that target protein kinases. To address this challenge, I have designed an interdisciplinary project that goes well beyond the state-of-the-art to explore in atomic detail the action of protein kinases intimately involved in Alzheimers disease and the abnormal phosphorylation of the protein Tau. The PhaseKin project aims to (i) reveal the specificity and reaction kinetics of protein kinases inside phase-separated condensates in vitro and in cells, (ii) decipher the dynamic conformational landscape of the protein kinases MARK2 and GSK3 by advanced NMR methods that will grant unprecedented detail on their modes of regulation, (iii) disentangle changes in population distributions and rates of interconversion between structurally distinct kinase states inside condensates, (iv) unravel the physicochemical basis of kinase drug partitioning into condensates. The highly innovative nature of the project is devised to delve into the heart of protein kinase function and to revolutionize our knowledge about the chemistry of drug-kinase interactions. Findings from the PhaseKin project will provide critical guidance in the development of more efficacious and specific drugs which target protein kinases.

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HORIZON-ERC - HORIZON ERC Grants

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Call for proposal

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(opens in new window) ERC-2023-ADG

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Host institution

DEUTSCHES ZENTRUM FUR NEURODEGENERATIVE ERKRANKUNGEN EV
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.

€ 2 499 943,00
Address
VENUSBERG-CAMPUS 1/99
53127 BONN
Germany

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Region
Nordrhein-Westfalen Köln Bonn, Kreisfreie Stadt
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.

€ 2 499 943,00

Beneficiaries (1)

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