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Restoring the Immune Response in Glioblastoma by Microglial-Targeting of Autophagy Inhibitors.

Project description

Restoring immune response against glioblastoma

Glioblastoma is a highly aggressive brain cancer that affects 15 000 people annually in Europe. Recent research has focused on the tumour microenvironment (TME), where microglial cells – typically immune defenders – support tumour growth. Targeting autophagy in these cells may help restore the immune response against glioblastoma. However, autophagy inhibitors can also harm neurons. With support from the Marie Skłodowska-Curie Actions programme, the MiTAI project aims to develop autophagy inhibitors that selectively target brain microglial cells. It will use a vectorisation approach for ULK1/2 inhibitors and PROTACs, both effective autophagy inhibitors. The project will conduct thorough in vitro and in cellulo investigations, develop selective and effective microglial autophagy inhibitors, and design metabolically stable compounds with sufficient bioavailability in the brain.

Objective

Glioblastoma is a highly aggressive type of brain cancer that kills around 15,000 people per year in Europe alone. It also has a devastating effect on patients' quality of life. Therefore, the clinical need in glioblastoma management is one of the highest in oncology: effective treatments are dearly needed. Over the past decade, the brain tissue surrounding glioblastoma tumors has been intensively studied. In this so-called 'tumor microenvironment' (TME), microglial cells make up the bulk cell type. Although immune cells by nature, TME microglial cells are reprogrammed to take on a tumor-supporting role: they become immunosuppressive and start secreting growth factors and nutrients that fuel tumor proliferation. Autophagy, best known as a cellular recycling pathway, is a masterswitch that determines the immune status in microglial and other immune cells. It also supports the process of nutrient secretion in TME microglia.

Therefore, inhibition of microglial autophagy can be a viable strategy to restore the immune response against glioblastoma tumors. Strong preclinical evidence in favor of this approach is available. However, translation into a new glioblastoma therapy is difficult, because the presence of autophagy inhibitors in the brain could also be dangerous to neurons. In response, this proposal wants to deliver and investigate autophagy inhibitors that selectively target brain microglial cells. A vectorizing approach is proposed for ULK1/2 inhibitors and PROTACS, which are very potent autophagy inhibitors. The proposal will thorougly investigate the compounds in vitro and in cellulo. For selected, highly promising molecules, in vivo proof of concept will be sought in a murine, orthotopic glioblastoma model. Next to obtaining selective and effective microglial autophagy inhibitors, the design of metabolically stable compounds with sufficient bioavailability in brain can be expected to be additional, prime challenges of the project.

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Topic(s)

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Funding Scheme

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HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European Fellowships

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Call for proposal

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(opens in new window) HORIZON-MSCA-2024-PF-01

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Coordinator

UNIVERSITEIT ANTWERPEN
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.

€ 200 400,00
Address
PRINSSTRAAT 13
2000 Antwerpen
Belgium

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Region
Vlaams Gewest Prov. Antwerpen Arr. Antwerpen
Activity type
Higher or Secondary Education Establishments
Links
Total cost

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