K. Burgess et al., A SMALL LIBRARY OF PEPTIDOMIMETICS TO SYSTEMATICALLY VARY AND TEST THE EFFECTS OF X(1) CONSTRAINTS, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2761-2764
A library of 47 peptidomimetics of YGGFLRFa was prepared wherein 32 of
these contained 2,3-methanoleucine. This library was tested for bindi
ng the neuropeptide FF receptor where neuropeptide FF is FLFQPQRFa, an
anti-opiate peptide. This study illustrates how conformational constr
aints can be systematically varied in a library format to determine th
e best conformational restrictions for the desired activity. Copyright
(C) 1996 Elsevier Science Ltd