Cladosporin, A Highly Potent Antimalaria Drug?

作者：Anwei Hou, Bei Li, Zixin Deng, Min Xu, Jeroen S. Dickschat · 发表于：ChemBioChem · 年份：2023 · DOI：10.1002/cbic.202300154 · 被引用次数：8 · 研究领域：RNA and protein synthesis mechanisms、Peptidase Inhibition and Analysis、Trypanosoma species research and implications

Cladosporin, a unique natural product from the fungus Cladosporium cladosporioides, exhibits nanomolar inhibitory activity against Plasmodium falciparum by targeting its cytosolic lysyl-tRNA synthetase (PfKRS) to inhibit protein biosynthesis. Due to its exquisite selectivity towards pathogenic parasites, cladosporin has become a very promising lead compound for developing antiparasitic drugs to treat drug-resistant malaria and cryptosporidiosis infections. Here we review the recent research progress of cladosporin covering aspects of the chemical synthesis, biosynthesis, bioactivity, cellular target and structure-activity relationship.