- Guide to PHARMACOLOGY
Compound class: Natural product or derivative
Comment: Borrelidin is a macrolide antibiotic originally isolated from Streptomyces. It is a noncompetitive inhibitor of both bacterial and eukaryotic threonyl-tRNA synthetases (also known as threonine--tRNA ligase), exhibiting antibacterial, antimalarial and antiangiogenic activities.
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.✖
|Borrelidin is toxic at low concentrations in human cell culture (HEK293 cells, IC50 of 345 nM), and it thought to inhibit human threonyl-tRNA synthetase 1 (TARS1).
In P. falciparum, borrelidin acts rapidly and has potent asexual blood stage activity against both drug-sensitive and drug-resistant strains of the parasite.
|Whole organism assay data|
|Key to terms and symbols||Click on species/strain names for details||Click column headers to sort|