Exploratory Research for Drug Discovery

Malaria is one of the three largest infectious diseases in the world, which aligns with HIV and tuberculosis. More than 200 million people are infected with malaria and more than 600,000 people died annually. Although Mosquirix (RTS, S/AS01) and R21/MM were recommended by WHO as anti-malaria vaccines in 2022 and 2023, there are still some issues such as insufficient efficacy so on. In addition, resistant malaria to existing therapeutic drugs have been reported. In this situation, the development of new drugs is urgently needed.

Members

Visiting Associate Professor
Kenichi Matsumura

Activities

In this department, a Shionogi’s researcher is in charge of a principal investigator, and conduct small molecule drug discovery together with Department of Molecular Infection Dynamics. We will take on the role of research hubs that connect research assets of Nagasaki University such as know-how and global network for malaria research and SAR(structure-activity relationship) engine for small molecule drug discovery of SHIONOGI. By taking advantage of strengths of each department, the drug discovery research will be promoted to create a therapeutic or a prophylaxis/chemoprevention drug with strong antimalarial activity and high safety. We are also collaborating with domestic and overseas research organizations including MMV (Medicines for Malaria Venture), promoting further optimization of the lead scaffolds and phenotypic screening hits that we have created so far.

Research activities are as follows:

  • Structure-Activity Relationship (SAR) study for lead compounds based on excisting drugs
  • Identifycation of hit compounds from compound libraries and Hit to Lead SAR approach based on screening-based drug descovery
  • Optimization of drug metabolism, safety, and physical parameters of candidate compounds within Shionogi
  • Strengthening external collaboration for SAR study, clinical development and identifying new targets
  • Conducting target discovery and basic research for antimalarial drugs

Recent main research achievement

  1. Tamura et al. Bioorg Med Chem Lett 2022; 68: 128769.
  2. Kato et al. Bioorg Med Chem Lett 2022; 59: 128567.
  3. Kato et al. J Med Chem 2023; 66: 11428.
  4. Tamura et al. Bioorg Med Chem Lett 2023; 79: 129059.