Design and Optimisation of Bioactive Cyclic Peptides: Generation of a Down-Regulator of TNF Secretion
AbstractAlthough strong binding interactions between protein receptor and ligand do not require the participation of a large number of amino acids in either site, short peptide chains are generally poor at recreating the types of protein-protein interactions which take place during cell recognition and signalling process, probably because their flexible backbones prevent the side chains from forming sufficiently rigid and stable epitopes, which can take part in binding with the desired strength and specificity. In a recently-reported study, it was shown that a proto-epitope containing F, R and S amino acids has the ability to down-regulate TNF secretion by macrophages. This paper extends these findings, putting those amino acids into a short cyclic peptide scaffold, and determining the optimal configuration required to overcome the problems of conformational instability, and give rise to molecules which have potential as therapeutic agents in human disease, such as rheumatoid arthritis. View Full-Text
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New, R.; Bansal, G.S.; Dryjska, M.; Bogus, M.; Green, P.; Feldmann, M.; Brennan, F. Design and Optimisation of Bioactive Cyclic Peptides: Generation of a Down-Regulator of TNF Secretion. Molecules 2014, 19, 21529-21540.
New R, Bansal GS, Dryjska M, Bogus M, Green P, Feldmann M, Brennan F. Design and Optimisation of Bioactive Cyclic Peptides: Generation of a Down-Regulator of TNF Secretion. Molecules. 2014; 19(12):21529-21540.Chicago/Turabian Style
New, Roger; Bansal, Gurpal S.; Dryjska, Malgorzata; Bogus, Michal; Green, Patricia; Feldmann, Marc; Brennan, Fionula. 2014. "Design and Optimisation of Bioactive Cyclic Peptides: Generation of a Down-Regulator of TNF Secretion." Molecules 19, no. 12: 21529-21540.