Synthesis of an Uncharged Tetra-cyclopeptide Acting as a Transmembrane Carrier: Enhanced Cellular and Nuclear Uptake

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• 作者：Flaviane Francisco Hilário ; Mohamed Dit Mady Traoré ; Vincent Zwick ; Laurence Berry ; Claudia A. Simões-Pires ; Muriel Cuendet ; Nicolas Fantozzi ; Rossimiriam Pereira de Freitas ; Marjorie Maynadier ; Sharon Wein ; Henri Vial ; Yung-Sing Wong
• 刊名：Organic Letters
• 出版年：2017
• 出版时间：February 3, 2017
• 年：2017
• 卷：19
• 期：3
• 页码：612-615
• 全文大小：340K
• ISSN：1523-7052

文摘

A small uncharged cyclopeptide scaffold inspired by a natural product and designed to undergo postfunctionalizations was used as a new transmembrane vector. A bioactive and fluorescent triazole aminocoumarin was bound to this carrier to facilitate its moving across cell and subcellular membranes, and this led to an increase in its cell toxicity.