- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: Bestatin is a transition-state analogue of the dipeptide PheLeu, a substrate for aminopeptidases.
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. Grembecka J, Mucha A, Cierpicki T, Kafarski P. (2003)
The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.
J Med Chem, 46 (13): 2641-55. [PMID:12801228]
2. Orning L, Krivi G, Fitzpatrick FA. (1991)
Leukotriene A4 hydrolase. Inhibition by bestatin and intrinsic aminopeptidase activity establish its functional resemblance to metallohydrolase enzymes.
J Biol Chem, 266 (3): 1375-8. [PMID:1846352]
3. Taylor A, Peltier CZ, Torre FJ, Hakamian N. (1993)
Inhibition of bovine lens leucine aminopeptidase by bestatin: number of binding sites and slow binding of this inhibitor.
Biochemistry, 32 (3): 784-90. [PMID:8422382]