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Content archived on 2024-06-18

Discovering and exploiting hidden pockets at protein-protein interfaces

Objective

"Protein-protein interactions play critical roles in normal human physiology, as well as in numerous diseases such as cancers and neurodegenerative disorders. However, identifying small molecule drugs to block protein interactions is a very difficult task. One of the major difficulties is that often the proteins involved are extremely flexible and readily change shape, which greatly complicates efforts to find small molecule ligands of matching shape. In this project, we aim to exploit protein flexibility to create new opportunities for drug discovery.

Interactions between a given pair of proteins commonly requires one or both partners to transiently form pockets that allow selective binding. Therefore, most protein interfaces likely possess many more binding pockets than those apparent in the static picture of a protein structure revealed by crystallographic experiments. We propose to identify these ""hidden"" pockets using computational methods. Thus, we will develop and validate molecular simulation methodologies to detect hidden pockets at protein interfaces and assess their small molecule ""druggability"" using docking calculations and binding site scoring functions. Such capacity would greatly strengthen the reliability of in silico drug design. We will perform virtual screens to find small molecule ligands binding to hidden pockets in medicinally important proteins such as FcgammaRIIA or PCNA. Finally, we will purchase or synthesize promising ligands and assay their activity against protein targets. These studies will allow us to test the utility of our computational approach in rational drug design.

The objectives of this research are part of a broader program we are currently developing and whose purpose is to provide a comprehensive set of computational/biophysical methods to allow the widespread targeting of seemingly ""undruggable"" protein families with small molecules, thereby expanding the scope of modern molecular medicine."

Fields of science (EuroSciVoc)

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Topic(s)

Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.

Call for proposal

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

FP7-PEOPLE-2010-RG
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Funding Scheme

Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.

MC-IRG - International Re-integration Grants (IRG)

Coordinator

THE UNIVERSITY OF EDINBURGH
EU contribution
€ 100 000,00
Address
OLD COLLEGE, SOUTH BRIDGE
EH8 9YL Edinburgh
United Kingdom

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Region
Scotland Eastern Scotland Edinburgh
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.

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