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Peptide-drug conjugates for weight loss maintenance

Project description

Peptide-drug conjugates preventing weight regain

The global obesity epidemic poses a challenge to human health. While effective weight-loss therapies exist, long-term maintenance remains difficult due to the body’s natural drive to regain lost weight. In response to food deprivation, specific hunger-promoting neurons become more excitable, triggering weight recidivism. The ERC-funded PDC-MAIN project aims to prevent this process by developing innovative peptide-drug conjugates (PDCs) that target the cellular mechanisms underlying homeostatic weight regain. By focusing on G protein-coupled receptors (GPCRs) in hypothalamic cells, the project will design GPCR-targeted PDCs to disrupt this cycle. Advanced neurobiological techniques, including fibre photometry, will be used to assess target engagement, while preclinical models will evaluate the potential for sustained weight loss following dietary and pharmacological interventions.

Objective

The worldwide rise in obesity rates is causing significant harm to human health. While effective weight loss therapies are emerging, the challenge of maintaining weight loss remains unresolved. With this project, we will leverage expertise in drug development to engineer novel peptide-drug conjugates designed to obstruct homeostatic weight regain in a cell specific fashion. In the food deprived state, a subset of hunger promoting neurons undergo structural changes that increases excitability and thus drives homeostatic weight regain. Capitalizing on our knowledge of G protein-coupled receptors (GPCRs) expressed in hypothalamic cell populations we will develop GPCR-targeting peptide-drug conjugates specifically designed to obstruct weight recidivism. To evaluate this drug-targeting approach, neurobiological methods including fiber photometry will be employed to confirm target engagement. Preclinical models are used to investigate the translational potential for treatment of weight loss maintenance following dietary and pharmacological weight loss interventions. The molecular mechanisms of action and receptor-target selectivity of the conjugates will be determined using loss-of-function mouse models. Pharmacokinetic properties of lead candidates will be optimized by incorporating chemical half-life extenders. This bridging between medicinal chemistry, neuroscience and pharmacology will give rise to new multimodal molecules targeting homeostatic weight regain mechanisms to address a vastly growing unmet medical need for weight loss maintenance pharmacotherapies.

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Call for proposal

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(opens in new window) ERC-2024-COG

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Host institution

KOBENHAVNS UNIVERSITET
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.

€ 1 999 610,00
Address
NORREGADE 10
1165 KOBENHAVN
Denmark

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Region
Danmark Hovedstaden Byen København
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.

€ 1 999 610,00

Beneficiaries (1)

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