Cladosporin, A Highly Potent Antimalaria Drug?

Abstract Cladosporin, a unique natural product from the fungus Cladosporium cladosporioides , exhibits nanomolar inhibitory activity against Plasmodium falciparum by targeting its cytosolic lysyl‐tRNA synthetase ( Pf KRS) 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.