Novel sst4-Selective Somatostatin (SRIF) Agonists. 2. Analogues with β-Methyl-3-(2-naphthyl) alanine Substitutions at Position 8⊥

…, R Cescato, JC Schaer, JC Reubi, J Rivier

文献索引：Erchegyi, Judit; Penke, Botond; Simon, Lajos; Michaelson, Scott; Wenger, Sandra; Waser, Beatrice; Cescato, Renzo; Schaer, Jean-Claude; Reubi, Jean Claude; Rivier, Jean Journal of Medicinal Chemistry, 2003 , vol. 46, # 26 p. 5587 - 5596

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被引用次数: 30

摘要

We present a family of human sst4-selective, high-affinity (IC50= 2-4 nM) cyclic somatostatin (SRIF) octapeptides. These peptides result from the substitution of dTrp8 in Hc [Cys3-Phe6- Phe7-dTrp8-Lys9-Thr10-Phe11-Cys14]-OH (SRIF numbering)(ODT-8) by one of the four conformationally biased stereoisomers of β-methyl-3-(2-naphthyl) alanine (β-Me2Nal). Whereas Hc [Cys-Phe-Phe-dNal-Lys-Thr-Phe-Cys]-OH (ODN-8, 2) has high affinity and ...