2 minute read

Apicomplexan portfolio

Our teams work to develop new treatments for malaria and cryptosporidiosis, two infectious diseases caused by apicomplexan parasites. These diseases disproportionally affect children in Low- and Middle-Income countries, particularly in Africa. There is no effective treatment for the diarrheal disease cause by Cryptosporidium in malnourished infants. Resistance to current malaria treatments is spreading in Africa and Asia and this increases the need for new antimalarial medicines.

In addition, in our portfolio, we have a drug discovery project to discovery new treatments for schistosomiasis, an infectious diseases cause by worms that affects 250 million people per year.

Portfolio overview

Our projects expand from hit identification to pre-clinical candidate selection. We lead the Structure-guided Drug Discovery Coalition (SDDC). The SDDC aims to apply structurebased drug design to deliver Early Lead series for malaria and TB. We have a project in lead optimisation for malaria in collaboration with Eisai and MMV and a more advanced project at the late lead profiling stage for cryptosporidiosis in collaboration with Prof. Chris Huston (University of Vermont) and Eisai. Our schistosomiasis project is a collaboration with Prof. Karl Hoffman (Aberystwyth University) and Prof. Andrea Brancale (Cardiff University) and it is funded by Wellcome.

Key highlights for 2022

→ Our cryptosporidiosis lead has progressed to rat toxicological studies.

→ In collaboration with MalDA partners we published the validation Plasmodium acetyl-CoA synthetase as a promising malaria target: doi.org/10.1016/j. chembiol.2021.07.010

→ We have obtained proof of concept of efficacy for our acetylCoA synthetase inhibitors in a mouse model of malaria.

→ In May we welcomed our MalDA partners to Dundee for the first face to face meeting for the consortium since December 2019.

→ In September we organised a workshop in London to discuss drug discovery for schistosomiasis. More than 50 academic and industry experts discussed key challenges and proposed solutions to accelerate the discovery of new medicines.

“The highlight for me is getting to proof of concept of efficacy for PfAcCS, which represents a major goal for the development of compounds for this target. Being part of the apicomplexan team within the DDU also means being part of a wider international team focused on the same goals, with access to a wealth of knowledge, experience and support.”

Andy, Senior Biologist

“For me the highlight of the year was the MalDA/ SDDC meetings held in Dundee. I enjoyed finally being able to attend a work event in person and meeting many of the great people involved in the consortia.”

Joel, Structural Biologist.

Malaria- Cabamiquine

Cryptosporidiosis - KRS

Malaria- Pf KRS

Malaria- Pf AcCS

Malaria- Pf KRS BU

Multiple target-based series

Funders and consortia

“My highlight of the year was expanding the Schistosomiasis team and traveling down to London together for our Target Product Profile meeting. I think the Apicomplexan team works really well together, everyone is friendly and supportive”. Nicola, Medicinal Chemist Team Leader.

“It has been very exciting to work on a new antimalarial target and getting high quality hits from our screening campaigns. Being part of the Apicomplexan portfolio is a great pleasure; it is a challenging but friendly environment. The highly collaborative nature of our work and involvement of several partners across the world make the job rewarding and stimulating whilst contributing to the ambitious and relevant goal of malaria eradication.”

Luma, Biologist