TC217

London School of Hygiene and Tropical Medicine - Optimization of imidazopyridine and thiazole scaffolds targeting plasmodial kinases to generate a fast killing compound to treat malaria infection and block transmission

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Principal Investigator (PI)

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Project location

the sponsor

Home Institution

London School of Hygiene & Tropical Medicine

foundation funding

Foundation funding

The Foundation is providing £132,140 in support.

Open Labs Fellow/s

Dr Alexios Matralis - Adnan Malik

GSK’s contribution

Project Description

Starting from a set of compounds prepared by D. Baker’s group that showed activity in GSK phenotypic and dual gamete formation assays on top of its activity against P. falciparum cGMP-dependent protein kinase (PfPKG), this open lab will focus on improve the physchem profile of these families, increase their potency in the phenotypic/dual gamete formation assays, abolish toxicity issues, and gain knowledge of their in vitro killing profile in order to focus only in fast killing compounds. The aim of the project is to deliver compounds active in vivo in the P. falciparum mouse model, with physicochemical properties that allow developability and adequate safety profile.