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Synonyms: NKTR-214 | NKTR214
Compound class:
Peptide or derivative
Comment: Bempegaldesleukin (NKTR-214) is an engineered variant of human interleukin-2 [4] in which Ala1 has been removed and Cys125 is substituted by Ser. The peptide is produced in E. coli and an average of 6 lysine residues are N6 substituted with [(2,7-bis{[methylpoly(oxyethylene)]carbamoyl}-9H-fluoren-9-yl)methoxy]carbonyl (PEG-Lys). In the PEG-bound form the IL-2 is inactive, but In vivo the PEG chains are released slowly which provides a more controlled release of active IL-2 peptide [4] (the IL-2 conjugates with 1 or 2 PEG chains are the most biologically active conjugates [3]). This prodrug strategy mitigates against the severe side effects which limit maximal dosing of parental aldesleukin.
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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