Gastrin releasing peptide antagonists with improved potency and stability

DC Heimbrook, WS Saari, NL Balishin…

文献索引：Heimbrook; Saari; Balishin; Fisher; Friedman; Kiefer; Rotberg; Wallen; Oliff Journal of Medicinal Chemistry, 1991 , vol. 34, # 7 p. 2102 - 2107

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被引用次数: 21

摘要

Gastrin releasing peptide (GRP) is a 27 amino acid peptide hormone which is homologous to the amphibian peptide bombeein. Two series of novel GRP antagonists were developed by C-terminal modiication of N-acetyl-GRP-20-27 amide. Peptide derivatives within each series resist enzymatic degradation in serum and exhibit strong affinity for the GRP receptor. The first series of compounds replaces the Leuls-Metn region of GRP with an alkyl ether ...