denileukin diftitox

Ligand id: 7044

Name: denileukin diftitox

No information available.
Summary of Clinical Use
Denileukin diftitox is used to destroy malignant leukemia and lymphoma cells which express cell surface IL-2 receptors.
Mechanism Of Action and Pharmacodynamic Effects
The IL-2 sequence of this dual domain drug binds to cell surface IL-2 receptors and upon internalisation via receptor-mediated endocytosis and endocytic processing, the diptheria toxin is liberated and is able to act on its intracellular target, EEF2 (eukaryotic translation elongation factor 2) [1], effectively shutting down protein synthesis in the cell. Diptheria toxin belongs to a diphthamide-specific class of ADP-ribose transferases, and is able to inactvate EEF2 by catalysing the transfer of NAD+ to the diphthamide residue (a posttranslationally modified histidine residue, PubChem CID 6438375) contained in this protein. Mutation of this dipthamide resudue renders EEF2 resistant to diptheria toxin [2].