London School of Hygiene and Tropical Medicine

Start : January 2017 | Status : Active

The scientists: Dr Alexios Matralis and Adnan Malik will work in the optimization of imidazopyridine and thiazole scaffolds targeting plasmodial kinases. Both researchers are medicinal/organic chemists with post-doctoral experience. Their main role will be the design, synthesis and characterization of the new compounds as well as the proposal of new ideas based on the acquired knowledge.

The Sponsor: London School of Hygiene & Tropical Medicine

Foundation funding: The Foundation is providing £107,140 in support.

GSK’s contribution: GSK will contribute its experience in phenotypic programs, medchem expertise, parasitology, in vitro assays, safety, and its in vivo humanized mouse model.

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.