Esterase-Sensitive Cyclic Prodrugs of Peptides: Evaluation of an Acyloxyalkoxy Promoiety in a Model Hexapeptide

@article{Pauletti1996EsteraseSensitiveCP,
  title={Esterase-Sensitive Cyclic Prodrugs of Peptides: Evaluation of an Acyloxyalkoxy Promoiety in a Model Hexapeptide},
  author={Giovanni M. Pauletti and Sanjeev Gangwar and Franklin W. Okumu and Teruna J. Siahaan and Valentine J. Stella and Ronald T. Borchardt},
  journal={Pharmaceutical Research},
  year={1996},
  volume={13},
  pages={1615-1623}
}
Purpose. To evaluate a cyclic acyloxyalkoxycarbamate prodrug of a model hexapeptide (H-Trp-Ala-Gly-Gly-Asp-Ala-OH) as a novel approach to enhance the membrane permeation of the peptide and stabilize it to metabolism. Methods. Conversion to the linear hexapeptide was studied at 37°C in aqueous buffered solutions and in various biological milieus having… CONTINUE READING