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Compound class: Natural product or derivative
Comment: Cladosporin is a tricyclic octaketide that is a secondary metabolite produced by several fungal genera including Cladosporium and Aspergillus. Cladosporin exhibits broad-spectrum bioactivity, including antimalarial, antifungal, antibiotic, plant growth inhibitory properties and mammalian anti-inflammatory effects.
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|Guide to Malaria Pharmacology Comments|
|Although cladosporin exhibits potent antimalarial activity, poor oral bioavailability has precluded the compound from further advancement in the antimalarial drug development pipeline. A recent SAR study has identified a simplified cladosporin analogue (compound 28) that has higher antimalarial potency and improved metabolic stability .
Potential Target/Mechanism Of Action: Postgenomic methods indicate that cladosporin inhibits protein synthesis by directly targeting P. falciparum lysine--tRNA ligase (PfcKRS) .