Focus Oncotherapies #11


June 9, 2021

Focus Oncotherapies #11

The Campania Oncoterapie project has created a multidisciplinary consortium that includes the greatest Campania excellence in the field of anticancer research. The best result that this project can boast is the collaboration between the different partners in numerous scientific works, which demonstrate the skills of each area involved.

The EBRIS Foundation and the Department of Pharmacy of the University of Salerno collaborate together especially in the chemical-pharmaceutical field.

Among the various shared works, one of these is composed of the identification of an indole scaffold, 5-carboxyamide, tested as a multi-kinase inhibitor. This work arises from Inverse Virtual Screening (IVS) studies through which some potential target protein kinases have been identified. The involvement of the ERK kinase in the mechanism of action of the synthesized molecule was confirmed with subsequent binding assays. In fact, the best compound of the series showed an interesting inhibitory activity against a certain kinase, important regulator responsible for the progression of cancer. In cancer cells tested (HeLa), but not in normal cells, the compound identified modulates ERK levels suggesting a selective action on activated kinases, related to the intracellular ERK pathway ( .2019.01.066)

Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach