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Content archived on 2024-06-25

Designing therapeutic protein-protein inhibitors for brain cancer treatments

Objective

Protein-protein interactions are central elements in cellular processes and important targets for selective therapeutic agents. They constitute a rich area for discovery of novel small ligand-based therapies.This proposal seeks to utilise such interactions, in particular those featuring an alpha-helix binding groove, such as p53-MDM2, or more novel targets e.g. n23-prune to develop targeted small molecule libraries with physico-chemical properties appropriate for therapeutic effect against various tumour types such as the brain cancers of glioblastoma and medulloblastoma. Combination of the concepts below should provide an opportunity to unlock the potential of protein interactions as key components in signalling pathways via design of selective small molecule modulators targeting the kinase-effector interaction instead of the ATP active site.Data-mining of ADME and drug-drug interactions to build a predictive database for library design.
Develop quantitative structure/property relationships, with an emphasis on CYP-mediated metabolism,ABC transporters at the blood/brain and brain/tumour interfaces,mutagenicity, solubility, pKa,and passive permeability,and predictive tools for mutagenicity and other genetic toxicology end-points.Develop predictive PK and PBPK models to improve understanding of BBB and tumour penetration.In vitro and in vivo PK/PD and TK/TD characterisation of compounds, to increase understanding of their mechanism of action and reduced the use of laboratory animals.Develop an understanding of the elements controlling selectivity in protein-protein signalling networks by developing approaches for design of small molecules that target alpha-helix binding groove interactions through use of structure based and fragment based approaches. Such knowledge-based approaches will also be applicable to the design of small molecules for other protein-protein interactions that utilize an alpha-helix binding groove and for other therapeutic areas.

Fields of science (EuroSciVoc)

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Topic(s)

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Call for proposal

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FP6-2005-LIFESCIHEALTH-7
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Funding Scheme

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STREP - Specific Targeted Research Project

Coordinator

SIENA BIOTECH SPA
EU contribution
No data
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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Participants (7)

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