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Last Updated: 19/06/2024
Development of malaria-selective covalent inhibitors targeting serine-metabolizing enzymes
Objectives
*Original title and abstract were machine translated from Japanese.
This study aims to elucidate the inhibition mechanism of malaria serine metabolizing enzyme (SHMT) selective inhibitor candidates obtained from drug search, and to develop into a covalent inhibitor that can inhibit Plasmodium in a physiological environment.
Serine metabolizing enzyme (SHMT) is responsible for serine-glycine conversion, is involved in in vivo nucleic acid synthesis, and is an essential enzyme for the survival of Plasmodium malaria. Therefore, SHMT has been attracting attention in recent years as a new drug discovery target for Plasmodium malaria, whose drug resistance is becoming more serious every day. However, SHMTs are very similar between species and are also essential for maintaining normal human vital activity. Therefore, in the development of malaria SHMT inhibitors, it is an issue to have both “selectivity” and “medicinal efficacy” that inhibit only malaria SHMT.
Apr 2022 — Mar 2025
$21,031