Lead optimisation of super-selective CSF-1R kinase inhibitors against glioblastoma multiforme

Glioblastoma multiforme (GBM) is the most aggressive type of brain cancer. It is characterised by genetic alterations that results in disruption of receptor tyrosine kinase (RTK) signalling. We have identified a new class of compounds that potently inhibits GBM cell proliferation by blocking the RTK CSF-1R. Phenomics studies across patient-derived GBM cells showed that the lead compound displays preferential activity against GBM cells of the mesenchymal subtype, one of the most invasive of all GBM subclasses. Given the prominent role of CSF-1R in tumour immune evasion in GBM and other cancers, with the support of MRS we propose to recruit a PhD student and develop a lead optimisation campaign to progress to in vivo studies and IP protection. Joining forces with Nuvectis Pharma, the student will perform a cross-disciplinary project at the interface of medicinal chemistry, cancer biology and drug discovery, aiming to find a targeted therapy against the most life-threatening brain cancer.