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Cladosporin,A Highly Potent Antimalaria Drug?
Authors:Dr Anwei Hou  Bei Li  Prof Zixin Deng  Dr Min Xu  Prof?Dr Jeroen S Dickschat
Affiliation:1. Tianjin Institute of Industrial Biotechnology, Chinese Academy of Sciences, West 7th Avenue No. 32, 300308 Tianjin, China;2. Tianjin Institute of Industrial Biotechnology, Chinese Academy of Sciences, West 7th Avenue No. 32, 300308 Tianjin, China

Haihe Laboratory of Synthetic Biology, West 15th Avenue No. 21, 300308 Tianjin, China;3. Kekulé-Institute for Organic Chemistry and Biochemistry, University of Bonn, Gerhard-Domagk-Straße 1, 53121 Bonn, Germany

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 (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.
Keywords:antimalarial drugs  biosynthesis  chemical synthesis  cladosporin  structure–activity relationship
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