- Guide to PHARMACOLOGY
Compound class: Natural product or derivative
Comment: Artemisinin is a sesquiterpene lactone with an unusual endoperoxide bridge, believed to be responsible for the antimalarial activity of the compound. It is a natural product, isolated from the qinghao or sweet wormwood plant (Artemisia annua) and used in Chinese traditional medicine to treat fever.
Artemisinin is a prodrug that is converted to the active metabolite artenimol (dihydroartemisinin).
We show one representation of artemisinin here. As with other natural products, there are alternative chemical structures due to the complex stereochemistry.
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.✖
|The interaction table below provides data from an evaluation of the antimalarial (asexual blood stage) activity of artemisinin, using a panel of P. falciparum strains.|
|Whole organism assay data|
|Key to terms and symbols||Click on species/strain names for details||Click column headers to sort|
|Targets where the ligand is described in the comment field|
|zinc finger DHHC-type palmitoyltransferase 6||Catalyses protein S-palmitoylation of substrate proteins. ZDHHC6 substrates include calnexin (CANX), thioredoxin related transmembrane protein 1 (TMX1) , and the oncogenic NRAS GTPase . The antimalarial drug artemisinin inhibits ZDHHC6-mediated palmitoylation of NRAS and calnexin . Blocking NRAS palmitoylation with artemisinin disrupts its subcellular localisation and downstream proliferative signalling, and contributes towards the anticancer activity of artemisinin and its analogues .|