Compound class:
Synthetic organic
Comment: The peptide vinyl sulfone, WLL-vs, is a highly selective covalent inhibitor of the P. falciparum proteasome [1].
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. ![]() Ligand Activity Visualisation ChartsThese 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. ✖ |
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Bioactivity Comments |
WLL-vs inhibits the P. falciparum proteasome β2 and β5 subunits (IC50 of 0.9 and 0.8 μM, respectively), but is only effective against human β5 activity (IC50 of 1 μM) [1]. In the same study, the compound was tested in a murine P. chabaudi infection model, with almost complete clearance of the parasite following a single dose of 35 mg/kg. WLL-vs is particularly potent against the early asexual blood stage (young trophozoite or ring-stage) and eliminates genetically diverse strains, including artemisinin-resistant lines [2]. Note: P. falciparum proteasome subunit beta type-2 is not yet included in the database, with subunit beta type-5 tagged as the target for this ligand for data retrieval purposes. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click on species/strain names for details | Click column headers to sort | ||||||||||||||||||||||||||||||||
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Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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Whole organism assay data | |||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click on species/strain names for details | Click column headers to sort | |||||||||||||||||||||||||||||||||||
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