Researchers at St. Jude have generated a human carboxylesterase that efficiently activates the anticancer drug CPT-11. This was performed using site directed mutagenesis of hCE1 using information provided by the crystal structures of wildtype hCE1 and a rabbit liver CE (rCE).
Previous research developed enzyme/prodrug therapy approaches using rCE and CPT-11, this novel enzyme (hCE1mut6), would replace the rabbit protein in these studies and be much more likely to be used in any clinical application of this technology.
Carboxylesterase, enzyme, cancer, drug, CPT-11
Granted Patents or Published Applications
US 7,906,637; 8,124,393; US Pub. 2012/0142108
Related Scientific References
An improved human carboxylesterase for enzyme/prodrug therapy with CPT-11”, Cancer Gene Therapy (2008) 15:183-192.
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