Medical Research Council

Start : May 2014 | Status : Complete

The scientist: Dr Ana Sánchez Azqueta is focusing her research on the discovery of new drugs against malaria through a project titled ‘Screening and identification of anti-malarial compounds that act via the inhibition of the PfCLK family of protein kinases’. Ana is a postdoctoral researcher in Prof. Andrew Tobin’s group at the MRC’s Toxicology Unit in Leicester. Her area of expertise is protein-ligand interactions and enzyme kinetics.

The sponsor: The UK’s Medical Research Council has been at the forefront of scientific discovery to improve human health. Founded in 1913, the MRC currently invests UK taxpayers’ money into some of the best medical research in the world across every area of health. 
The laboratory of Prof. Andrew Tobin has developed expertise in the role of protein phosphorylation in maintaining essential processes in P. falciparum. The laboratory has received an MRC Developmental Gap Fund (DGF) Award to co-fund the Open Lab collaboration. The MRC DGF Award exists to bridge the translational gap between MRC scientists’ basic research and the next translational milestone on the way to patient benefit.

Foundation funding: The Foundation is providing £14,000 in support.

GSK’s contribution: GSK is providing in-kind contributions, including expertise, facilities and consumables to develop and perform the HTS, access to compound collection (TCAMS), early in vitro toxicology and in vitro ADME studies as well as drug discovery expertise for hit prioritisation once the HTS campaign has been completed.

Project Description: This project will address whether protein kinase inhibitors specific against the PfCLK kinases can be developed as a safe and curative treatment for malaria. Furthermore, this project will also contribute to the question of whether protein kinase inhibitors can be used to target malaria beyond the blood stage. This project will specifically address the following problems:
- To define selective inhibitors to the PfCLK family
- To determine the anti-malarial activity of PfCLK the inhibitors (in vitro and in vivo) and establish the mode of action of the inhibitors
The duration of the project is expected to be 12 months and will involve a close collaboration between the MRC’s Toxicology Unit and scientists at GSK’s Tres Cantos Medicines Development Campus.