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Targeting Type 2 Diabetes with Allene-containing Molecules Using a C-N Bond Cleavage Tool

Objective

Type 2 Diabetes is a chronic disease affecting more than 450 million people world-wide and is still an unmet medical need. PPAR´s
(Peroxisome Proliferator-Activated Receptors) and G-protein-coupled receptors (GPCR) FFARs (Free Fatty Acid Receptors) are well
clinical validated targets for type-2 diabetes. Although selective GPR40 agonists have reached clinical phase III, the trials were
recently terminated due to signs of liver toxicity in patients. ALLENEDRUG is designed to provide a new chemical series of GPR40
ligands aiming to bring a safer type-2 diabetes therapy. To achieve this goal, we will use a synthetic tool developed in our laboratory
to prepare enantiomerically enriched allenes through a selective C-N bond cleavage. This ERC-PoC will allow us to test the new
chemical series as potential GPR40 agonists and to get insight into a SAR (Structure Activity Relationship) correlation with liver toxicity
in order to compare the new molecules prepared in this proposal with those currently in clinical phase III trials.

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Host institution

UNIVERSIDAD AUTONOMA DE MADRID
Net EU contribution
€ 150 000,00
Address
CALLE EINSTEIN 3 CIUDAD UNIV CANTOBLANCO RECTORADO
28049 Madrid
Spain

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Region
Comunidad de Madrid Comunidad de Madrid Madrid
Activity type
Higher or Secondary Education Establishments
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Total cost
No data

Beneficiaries (1)