OAU Scientists Achieve Landmark Breakthrough in Global Malaria Drug Research
A team of researchers at Obafemi Awolowo University (OAU), Ile-Ife, Osun State, has made a significant scientific advancement in the fight against malaria, marking a historic moment for Nigerian biomedical research.
The team successfully determined and deposited the first crystal structure of Plasmodium falciparum transketolase bound to an inhibitor into the global Protein Data Bank (PDB). This represents the first Protein Data Bank entry authored entirely by Nigerian scientists, positioning the country as a contributor — rather than merely a user — in advanced structural biology research.
The breakthrough was achieved at the laboratory of Dr. Olatomide Fadare, Associate Professor of Chemistry at OAU. Originally trained as a synthetic organic chemist, Fadare has expanded his expertise into medicinal chemistry, integrating organic synthesis, computational biology, and biochemical testing to design new drug candidates targeting malaria.
Malaria remains endemic across sub-Saharan Africa, with Plasmodium falciparum responsible for the most severe and deadly cases. A growing concern among scientists is the parasite’s increasing resistance to artemisinin-based combination therapies (ACTs), currently the frontline treatment.
Speaking on the development, Fadare noted that resistance has historically undermined malaria drugs.
“Fansidar used to be a three-tablet therapy taken at once. Over time, resistance developed. That is the story of malaria treatment. If we don’t continue to design new therapies that target different pathways, the parasite will always catch up with us,” he said.
Why the Discovery Matters
Central to the research is transketolase, a crucial enzyme involved in the metabolic processes of Plasmodium falciparum. For years, rational drug design targeting this enzyme was limited because no experimentally determined crystal structure was available in the Protein Data Bank. Researchers worldwide had to rely on computational models rather than confirmed structural data.
That barrier has now been removed.
“We carried out protein engineering, produced the protein and successfully crystallised it. Getting to the point where you can create a crystal from your protein is highly advanced science,” Fadare explained.
By depositing the structure in the Protein Data Bank — a global repository of protein crystal structures — the team has provided researchers worldwide with experimentally verified structural information that can accelerate targeted drug design.
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International Collaboration, Nigerian Leadership
The project involved collaboration among internationally based Nigerian scientists, including Dr. Olawale Raimi of the University of Dundee, Scotland; Dr. Abiodun Ogunjimi of Mount Sinai Hospital, Toronto; Prof. Olubanke Ogunlana of Covenant University, Nigeria; and Dr. Oluseyi A. Vanderpuye of Fayetteville State University, United States.
While OAU researchers designed and synthesized new chemical compounds in Ile-Ife, collaborators abroad supported cloning, protein expression, crystallization, inhibition studies, and advanced data analysis.
“We are running interconnected projects across Nigeria, the UK, Canada and the US. This positions Nigeria as a serious contributor to next-generation antimalarial drug discovery,” Fadare said.
Promising Drug Candidates Identified
Beyond structural determination, the team has already identified four to five small molecules that strongly inhibit the parasite’s transketolase enzyme without significantly affecting the human equivalent.
Selectivity is critical because humans also possess transketolase enzymes. According to Fadare, subtle structural differences between the parasite’s enzyme and the human version make selective targeting possible.
“If we inhibit this protein, the parasite’s metabolic processes slow down or stop. That means it cannot grow or replicate,” he explained.
The next phase will focus on optimizing these lead compounds to improve potency and safety before potential preclinical testing.
Broader Implications for Nigeria
Fadare used the opportunity to highlight systemic challenges in African scientific research, including limited funding, dependence on imported pharmaceuticals, and brain drain.
“Virtually every active pharmaceutical ingredient used in Nigeria is imported. We have the expertise to produce them locally, but the industry has not matured to that level,” he said.
He stressed that sustained investment in science and technology is essential for health-sector independence and long-term national development.
Despite operating without direct government or major organizational funding, the team continues its work, mentoring young scientists and building research capacity locally.
“With the right support, what we are doing can cause a tectonic shift in the pharmaceutical industry,” Fadare added.
The achievement not only advances malaria drug discovery but also demonstrates that high-level structural biology and medicinal chemistry research can be led and authored by scientists based in Nigeria.