A solid-phase synthetic strategy for labeled peptides:: Synthesis of a biotinylated derivative of the δ opioid receptor antagonist TIPP (Tyr-Tic-Phe-Phe-OH)
A solid-phase synthetic strategy for labeled peptides:: Synthesis of a biotinylated derivative of the δ opioid receptor antagonist TIPP (Tyr-Tic-Phe-Phe-OH)
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DOI：
10.1021/ol027044s
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发表时间：
2003-03-06
期刊：
影响因子：
5.2
通讯作者：
Aldrich, JV
中科院分区：
文献类型：
--
作者：
Kumar, V;Aldrich, JV
[图表]开发了标记肽的通用固相合成策略，并用于制备 δ 阿片受体拮抗剂 TIPP (Tyr-Tic-Phe-Phe-OH) 的生物素化衍生物。通过还原胺化将单保护的亲水二胺接头连接到含醛固相树脂上，然后引入生物素和肽合成，生成 Tyr-Tic-Phe-Phe-Asp-NH(CH2CH2O)(2)CH2CH2NH-生物素 (2)。 2 的高 δ 受体亲和力和选择性证明了这种设计方法对于标记肽衍生物的适用性。
[GRAPHICS]A general solid-phase synthetic strategy for labeled peptides was developed and used to prepare a biotinylated derivative of the delta opioid receptor antagonist TIPP (Tyr-Tic-Phe-Phe-OH). A monoprotected hydrophilic diamine linker was attached to an aldehyde-containing solid-phase resin by reductive amination, followed by introduction of biotin and peptide synthesis to yield Tyr-Tic-Phe-Phe-Asp-NH(CH2CH2O)(2)CH2CH2NH-biotin (2). The high delta receptor affinity and selectivity of 2 demonstrate the applicability of this design approach for labeled peptide derivatives.