- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: The peptide vinyl sulfone, WLL-vs, is a highly selective covalent inhibitor of the P. falciparum proteasome .
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.✖
1. Li H, O'Donoghue AJ, van der Linden WA, Xie SC, Yoo E, Foe IT, Tilley L, Craik CS, da Fonseca PC, Bogyo M. (2016)
Structure- and function-based design of Plasmodium-selective proteasome inhibitors.
Nature, 530 (7589): 233-6. [PMID:26863983]
2. Stokes BH, Yoo E, Murithi JM, Luth MR, Afanasyev P, da Fonseca PCA, Winzeler EA, Ng CL, Bogyo M, Fidock DA. (2019)
Covalent Plasmodium falciparum-selective proteasome inhibitors exhibit a low propensity for generating resistance in vitro and synergize with multiple antimalarial agents.
PLoS Pathog, 15 (6): e1007722. [PMID:31170268]
3. Yoo E, Stokes BH, de Jong H, Vanaerschot M, Kumar T, Lawrence N, Njoroge M, Garcia A, Van der Westhuyzen R, Momper JD et al.. (2018)
Defining the Determinants of Specificity of Plasmodium Proteasome Inhibitors.
J Am Chem Soc, 140 (36): 11424-11437. [PMID:30107725]