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Format:
Print
Author:
Wang, Jian
Dept./Program:
Chemistry
Year:
2004
Degree:
M.S.
Abstract:
Based on the lead peptide sequence LRKKKKKH, which has shown very impressive inhibition potency and selectivity during the cyclic GMP-dependent protein kinase Ia screening of peptide libraries, a small library of arginine diversified peptides and peptide-peptoid hybrids has been synthesized by solid phase peptide synthesis technique to study the structure-activity relationship for the future optimization of the lead peptide. The method, how to diversify the guanidine group on the solid phase in the presence of protecting groups, was demonstrated. The preliminary screening data indicated that the peptide-peptoid backbone modification is a very promising strategy, and all of the five hybrids showed comparable inhibition potency to the lead peptide. On the contrast, the Arg-diversified peptides did not show such impressive inhibition activities compared with the lead peptide.