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Therapeutic molecules and druggable sites to suppress aberrant ion channel activity in cancer.

Project description

The two-pore potassium channel protein complex as a therapeutic target in cancer treatment

TASK-3 protein is a member of the recently discovered two-pore potassium channels family responsible for maintaining the membrane resting potential. It is implicated in neurological diseases, and recent studies have demonstrated TASK-3 aberrant expression in breast, lung and colorectal cancer cells. The EU-funded InterTask project aims to complete a structural and functional analysis of the complex between TASK-3 and the cation co-transporter KCC2 that affects TASK-3 trafficking to the membrane. Structural information on the complex will uncover TASK-3 regions involved in protein-protein interactions as potential targets for drug discovery to modulate ion channel activity.

Objective

TASK-3 is a potassium channel member of the recently discovered two-pore potassium channels family (K2P) responsible for the background current maintaining the membrane resting potential. TASK-3 is involved in several neurological diseases but recent studies pointed out its oncogenic potential. TASK-3 aberrant expression was detected in breast, lung and colorectal cancer cells. This research proposal aims at 1) generate antibodies that can directly reduce TASK-3 function. The potency, the binding mode of the best antibodies will be characterized functionally and structurally to provide an atomic-resolution view of the mechanism of binding, paving the way for antibody engineering. The structural approach will also produce the three-dimensional structure of TASK-3, which will deepen our understanding on the biophysical properties of this channel and its involvement in several other pathologies. 2) Reduce TASK-3 activity by understanding the molecular basis of its trafficking to the membrane. The project aims at providing a structural and functional analysis of the complex between TASK-3 and the cation cotrasporter KCC2, a recently identified partner that affect TASK-3 trafficking to the membrane. Structural information on the complex will uncover regions of the channel involved in binding protein partners, opening the possibility of pursuing these protein-protein interactions surfaces as targets for drug discovery, with the ultimate goal of modulating ion channel activity. I will undertake a multidisciplinary study that spans protein biochemistry, structural biology, electrophysiology and antibody engineering. The project tackles – side by side - basic science questions (ion channel structure and regulation) and translational research (antibody-based therapy). It offers a molecular understanding of the structural and biophysical properties of TASK-3 -currently unavailable- and opens the venue to the therapeutic targeting of this ion channel.

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

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Call for proposal

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(opens in new window) H2020-MSCA-IF-2020

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Coordinator

UNIVERSITA DEGLI STUDI DI PAVIA
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.

€ 275 209,92
Address
STRADA NUOVA 65
27100 Pavia
Italy

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Region
Nord-Ovest Lombardia Pavia
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.

€ 275 209,92
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