Cyclodextrin-peptide conjugate

Chemosensors for Detecting Molecules using Modified Cyclodextrins and Cyclodextrin-Peptide Conjugates... 

Schaschke N, Assfatglvlachleidt I, Machleidt W, et al. P-Cyclodextrin/epoxysuccinyl peptide conjugates a new drag targeting system for tumor cells. Bioorg Med Chem Lett 2000 10 677-680. 

Hristova-Kazmierski, M. K., Horan, R, Davis, P. et al. A new approach to enhance bioavailabihty of biologically active peptides conjugation of a 6-opioid agonist to (3-cyclodextrin. Bioorg. Med. Chem. Lett. 1993, 3, 831-834. 

Peptide-hydrolyzing activity of Ce(IV) has been examined. In the presence of 10 mM Ce(NH4)2(N03)e, small peptides (10 mM) were hydrolyzed with half-lives of 2h at pH 7.0 and 50°C (106). The reaction was, however, accompanied by formation of hydroxide gels. When the gelation was avoided by solubilizing Ce(IV) with y-cyclodextrin and Gly-Gly (10 vaM) was incubated with the Ce(IV)-cyclodextrin conjugate (10 mA/) at pH 8.0 and 60 C, 39% of the peptide was hydrolyzed after 24 h (107). Coordination of cyclodextrin to Ce(IV) apparently lowered the catalytic activity of the metal center considerably. The mechanism of AU or AV was proposed for the peptide hydrolysis of the Ce(IV) complexes. 

Tremendous efforts have been made to overcome these challenges, cationic liposome and positively charged polymers are currently being used as the most common method to complex with negatively charged siRNA for systemic delivery [30, 36]. Other in vivo delivery approaches include conjugation with cholesterol, aptamer, peptide complexation with antibody-protamine fusion protein or encapsulation in cyclodextrin nanoparticles [35, 37-39]. 

---