The scientists: Dr Katja Laqua and Mr Henok Asfaw will focus their research on the discovery of new drugs for Tuberculosis disease, through a project entitled “Turning small potent antimycobacterial cyclo(depsi) peptides into drug-like scaffolds”. Dr. Katja Laqua has just finished her PhD at University Halle with Prof. Peter Imming. Her colleague, Mr Henok Asfaw Sahile, holds a Master Degree in Medicinal Chemistry, and he is a PhD student in Peter’s group. Both have extensive experience in organic synthesis and design of biologically active compounds.
The sponsors: Martin Luther University Halle-Wittenberg – founded in 1502 – is an efficient, modern full-university, which maintains the highest academic requirements. At present, more than 21000 students are enrolled in the university, which encompasses over 190 courses of study in 18 faculties and departments. Its Institute of Pharmacy - part of the Biosciences Faculty – houses 13 professorships covering all aspects of drug-related research and teaching. Prof. Imming's department focusses on synthetic medicinal chemistry in the fields of antimycobacterial compounds and stable free radicals as ESR probes. His group also collaborates with a tuberculosis research institute and the university in Addis Ababa, Ethiopia.
Foundation funding: The Foundation is providing £ 154,794 in support.
GSK’s contribution: GSK will allocate in-kind contributions to the project, including scientific expertise in M.tuberculosis in vitro and in vivo assays, medicinal chemistry, DMPK and further profiling activities. GSK will provide access to the relevant facilities as well as the necessary laboratory supplies to carry out the different work packages.
Project Description: Although the Millennium Development Goal to halt and reverse the TB epidemic by 2015 has been achieved, the global burden of TB remains enormous. In 2012, there were 8.6M new cases of TB and 1.3M deaths. Additionally, MDR-TB cases were reported in all the countries surveyed by WHO. According to their estimates, there were roughly 500,000 new MDR-TB cases that year. As of March 2013, 84 countries had reported at least one XDR-TB case. Outcomes for these patients are depressingly poor.
Small peptides, cyclopeptides and cyclodepsipeptides have recently come to the forefront as potential antimycobacterial drug substances. At the Open Lab, Katja and Henok will be focused on the optimization of cyclodepsipeptides and related analogues that have shown good growth inhibitory against TB and no cytotoxicity, in order to turn active compounds of the peptide-type into drug-like molecules by means of combining activity and stability with suitable solubility and membrane permeability properties.
The duration of the project is 24 months and will involve a close collaboration between Martin Luther University Halle and GSK’s Medicines Development Campus at Tres Cantos.