Project

Optimizing PROTACs for Targeted AURKA Degradation Towards an Orally Bioavailable Lead for Proof-Of-Concept Studies.

Code
1S26025N
Duration
01 November 2024 → 31 October 2028
Funding
Research Foundation - Flanders (FWO)
Research disciplines
  • Medical and health sciences
    • Medicinal chemistry
Keywords
Oncology Target degradation PROTACs
 
Project description

In this research proposal, we aim to develop and optimise novel PROTACs targeting Aurora kinase A (AURKA) for potential therapeutic applications in cancer treatment. The project focuses on refining the structure of existing PROTACs, previously synthesised at the Laboratory of Medicinal Chemistry at UGent, and enhancing their efficacy, selectivity, and physicochemical properties. By systematically optimising the Cereblon ligand, linker, and AURKA binding moiety, we aim to create PROTACs with improved oral availability and therapeutic potential.