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血管活性肠肽(VIP)N端十肽的合成及其药理性质

Synthesis and pharmacological properties of the N-terminal decapeptide of the vasoactive intestinal peptide (VIP).

作者信息

Bodanszky M, Henes J B, Yiotakis A E, Said S I

出版信息

J Med Chem. 1977 Nov;20(11):1461-4. doi: 10.1021/jm00221a019.

Abstract

The decapeptide derivative, L-histidyl-L-seryl-L-aspartyl-L-alanyl-L-valyl-L-phenylalanyl-L-threonyl-L-aspartyl-L-asparaginyl-L-tyrosine methyl ester, corresponding to the N-terminal sequence of both porcine and chicken VIP was synthesized in solution, by the stepwise strategy. Its pharmacological properties resemble those of VIP itself, but with a much lower potency, comparable to that of peptides with C-terminal sequences. The presence of two independent sequences carrying similar instructions was recognized in VIP.

摘要

采用逐步合成策略,在溶液中合成了与猪和鸡血管活性肠肽(VIP)的N端序列相对应的十肽衍生物,即L-组氨酰-L-丝氨酰-L-天冬氨酰-L-丙氨酰-L-缬氨酰-L-苯丙氨酰-L-苏氨酰-L-天冬氨酰-L-天冬酰胺基-L-酪氨酸甲酯。其药理特性与VIP本身相似,但效力低得多,与具有C端序列的肽相当。在VIP中识别出存在两个携带相似指令的独立序列。

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