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Synthesis of a lipid/peptide/drug conjugate: N4-(acylpeptidyl)-ara-C
1Department of Chemistry, Emory University, Atlanta, Georgia 30322.
Bioconjugate Chemistry
|March 1, 1994
Abstract:
A lipid/peptide/drug conjugate, N4-(acylpeptidyl)-ara-C, is synthesized under mild conditions to give an ara-C prodrug protected against cytidine deaminase-catalyzed deactivation. The compounds can be bound, via their hydrocarbon tails, to phospholipid membranes and examined for chymotrypsin-induced drug release. A tripeptide is too short to permit efficient enzyme/membrane contact and subsequent freeing of the drug. Faster rates can, presumably, be achieved by "fine tuning" the length and polarity of the peptide spacer attached to the drug.