Dextrin-Phospholipase A(2): Synthesis and Evaluation as a Bioresponsive Anticancer ConjugateBiomacromolecules, 2009 Apr 8
There is still an urgent need for improved treatments for metastatic cancer. Although the phospholipase A(2) (PLA(2)) crotoxin, an antitumor protein that appears to act by interaction with epidermal growth factor receptors (EGFR), has recently shown activity in breast cancer in phase I clinical trials, it also displayed nonspecific neurotoxicity.
Therefore, the aim of this study was to apply a novel concept called polymer-masked-unmasked-protein therapy (PUMPT) to give a bioresponsive dextrin-PLA(2) conjugate that would reduce PLA(2) systemic toxicity but retain antitumor activity following alpha-amylase triggered degradation of dextrin in the tumor interstitium…
The reduced toxicity and alpha-amylase triggered activity of the dextrin-PLA(2) conjugate confirmed the potential of this approach for further development as a novel anticancer treatment.
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