Design, Synthesis, and Validation of a Branched Flexible Linker for Bioactive Peptides

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• 作者：Martina E. Bowen ; Yasunari Monguchi ; Rajesh Sankaranarayanan ; Josef Vagner ; Lucinda J. Begay ; Liping Xu ; Bhumasamudram Jagadish ; Victor J. Hruby ; Robert J. Gillies ; Eugene A. Mash
• 刊名：Journal of Organic Chemistry
• 出版年：2007
• 出版时间：March 2, 2007
• 年：2007
• 卷：72
• 期：5
• 页码：1675 - 1680
• 全文大小：193K
• 年卷期：v.72,no.5(March 2, 2007)
• ISSN：1520-6904

文摘

A branched flexible linker that incorporates a fluorescent dansyl moiety was synthesized and used toconnect two high affinity NDP--MSH ligands or two low affinity MSH(4) ligands. The linker wasincorporated into the conjugate by solid-phase synthesis. In vitro biological evaluations showed thatpotency of binding to the human melanocortin 4 receptor was not diminished for linker-ligandcombinations relative to the corresponding ligand alone.