FPR1 (Formyl peptide receptor 1) is a member of G protein-coupled receptor (GPCR) family, it mediates neutrophil chemotaxis to the sites of bacterial infection by binding to molecules released during necrosis such as N-formylated peptides fMLF and extracellular annexin A1. More recently, high level expression of FPR1 was found in a number of cancers, including glioblastoma. Binding of FPR1 to its ligand then regulate many of their behaviours in glioblastoma cells and contributes to, proliferation, resistance to apoptosis, angiogenesis and invasion. Here we report the synthesis and in vitro evaluation of a series of analogues of pyrazole-based FPR1 antagonists, including ICT12035, in order to optimize their potency and BBB penetrations. In addition, we demonstrate the efficacy of ICT12035, in a number of 2D and 3D in vitro proliferation and invasion assays as well as in an in vivo model.

Structure-activity relationships of FPR1 antagonist for the treatment of glioma

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.