The spread of drug-resistant malaria parasites urges the search for new antimalarial drugs. Malarial aspartic proteases – plasmepsins (Plms) – are attractive drug targets. In collaboration with the group of Prof. A. Jirgensons (Institute of Organic Synthesis), we are involved in the development of Plm inhibitors as antimalarial drugs.
Funding
ERAF grants No. 2DP/2.1.1.1.0/14/APIA/VIAA/062 and No. 1.1.1.1/16/A/290
Publications
46. Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent In Vitro and In Vivo Antimalarial Activity
DOI: https://doi.org/10.1021/acs.jmedchem.3c00812.
28. Tetrahydroisoquinoline-Based Non-Peptidomimetic Plasmepsin Inhibitors
23. Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
Zogota, R.; Kinena, L.; Withers-Martinez, C.; Blackman, M., J.; Bobrovs, R.; Pantelejevs, T.; Kanepe-Lapsa, I.; Ozola, V.; Jaudzems, K.; Suna, E.; Jirgensons, A. Eur. J. Med. Chem. 2019, 163, 344-352.
21. Azole‐based non‐peptidomimetic plasmepsin inhibitors
Kinena, L.; Leitis, G.; Kanepe-Lapsa, I.; Bobrovs, R.; Jaudzems. K.; Ozola, V.; Suna, E.; Jirgensons, A. Arch. Pharm. Chem. Life Sci. 2018, 351, 1800151.