A small library of peptidomimetics to systematically vary and test the effects of X1 constraints
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A library of 47 peptidomimetics of YGGFLRFa was prepared wherein 32 of these contained 2,3-methanoleucine. This library was tested for binding the neuropeptide FF receptor where neuropeptide FF is FLFQPQRFa, an anti-opiate peptide. This study illustrates how conformational constraints can be systematically varied in a library format to determine the best conformational restrictions for the desired activity.
author list (cited authors)
Burgess, K., Godbout, C., Wen, L. i., & Payza, K.