Download Peptidomimetics Protocols by Wieslaw M. Kazmierski PDF

By Wieslaw M. Kazmierski

A cutting-edge choice of precise man made methods that result in numerous scaffolds, flip mimetics, peptide-bound replacements, and enzyme inhibitors. issues diversity from strange syntheses of amino acids to using quite a few linear and heterocyclic scaffolds in preference to the peptide spine. very important chemical techniques and techniques contain the temporary safeguard of charged peptides as impartial prodrugs for enhanced blood-brain penetration and the substitute of peptide bonds with heterocyclic earrings, olefins and fluoroolefins, and ketomethylenes. artificial protocols in the direction of the transition-state mimics and reactive "warheads," appropriate in enzyme inhibitors, also are disclosed.

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23. Hidalgo, I. , Raub, T. , and Borchardt, R. T. (1989) Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 96, 736-749. 24. , Hassan, I. , Dix, C. , and Mackay, M. (1990) Transport and permeability properties of human Caco-2 cells: An in vitro model of the intestinal epithelial cell barrier. J. Controlled Release 11,254O. 25. , and Zweibaum, A. (1983) Enterocyte-like differentiation and polarization of the human colon carcinoma cell line Caco-2 in culture.

2. Solid Phase Approach to the Synthesis of the Cyclic Prodrug 77 (Fig. 7. Synthesis of the Linear Peptide 15 A typical synthesis uses Wang’s alkoxy resin (Bachem Btoscience) (14) Fmoc protected ammo acids were used for the solid phase peptide synthesis unless otherwise indicated (15). The couplmg of the first ammo acid (p-benzyl-asparttc actd) requires direct acttvation of the carboxyl groups with DIC for optimal yields The couplmg of subsequent ammo acids used the DIC/HOBt method, and the reaction was monitored by the nmhydrm test (161, as well as by the weight of the resin The final cleavage of the peptide from the resin was accomplished by treatment with 50% TFA/DCM.

Burton, P. , Conradi, R. , Hilgers, A. , Ho, N. F. , and Maggiora, L. L. (1992) The relationship between peptide structure and transport across epithelial cell monolayers. J. Controlled Release 19, 87-98. 3. Burton, P. , Conradi, R. , and Ho, N. F. H. (1993) Evidence for a polarized efflux system for peptides in the apical region of Caco-2 cells. Biochem. Biophys. Res. Commun. 190,760-766. 4. Bocci, V. (1990) Catabolism of therapeutic proteins and peptides with implications for drug delivery. Adv.

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