Epitopes noncontinuous

For the cycloscan, conformational libraries are synthesized by cyclization of continuous or noncontinuous bioactive epitopes and not by their insertion into a scaffold. Originally, the concept of cycloscan was introduced for the generation of backbone-cyclized peptide libraries 467 however, cycloscan can also be applied to other modes of cyclization. In this approach all components of each sublibrary bear the identical sequence, and differ from each other in distinct parameters that affect their conformation, but do not alter their connectivity, and hence their potential bioactivity. This is achieved by gradually introducing discrete conformational perturbations, which allow an efficient screening of the conformational space of the parent peptide. The majority of the components of such libraries should be inactive, because they do not overlap the bioactive conformation. However, the peptide that does fit the bioactive conformation should be very potent and have all the pharmacological advantages of cyclic peptides. 

Daniels, A.J., Matthews, J.E., Viveros, O.H., Leban, JJ., Cory, M. Heyer, D. (1995b) Structure-activity relationship of novel pentapeptide neuropeptide Y receptor antagonist is consistent with a noncontinuous epitope for ligand-receptor binding. Mol. Pharmacology 48, 425-432. 

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