Exploration of Labeling of Near Infrared Dyes on the Polyproline Linker for Bivalent-Type CXCR4 Ligands.
Exploration of Labeling of Near Infrared Dyes on the Polyproline Linker for Bivalent-Type CXCR4 Ligands.
复制标题
二价型 CXCR4 配体聚脯氨酸接头上近红外染料标记的探索。
DOI：
10.1016/j.bmc.2015.09.040
复制
发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Takaaki Mizuguchi & Hirokazu Tamamura
中科院分区：
文献类型：
--
作者：
Wataru Nomura;Haruo Aikawa;Shohei Taketomi;Miho Tanabe;Takaaki Mizuguchi & Hirokazu Tamamura
我们之前使用聚-L-脯氨酸接头来开发趋化因子受体 CXCR4 的二价型配体。具有最佳接头的二价配体显示出与CXCR4的特异性结合，表明CXCR4可能作为细胞膜上的二聚体存在，并且能够定义CXCR4表达的量。本文报道了通过铜催化的叠氮-炔环加成反应作为关键反应，合成了二价 CXCR4 配体，在聚-L-脯氨酸连接体的末端或中心具有近红外 (NIR) 染料。一些 NIR 标记的配体已被获得，它们将成为有价值的探针，可用于研究表达 CXCR4 的细胞的行为。有关 NIR 染料标记位置对其结合特性影响的信息对于修饰二价型 CXCR4 配体的设计非常有用。
We have previously used poly-l-proline linkers for the development of bivalent-type ligands for the chemokine receptor, CXCR4. The bivalent ligands with optimum linkers showed specific binding to CXCR4, suggesting the existence of CXCR4 possibly as a dimer on the cell membrane, and enabled definition of the amount of CXCR4 expressed. This paper reports the synthesis by a copper-catalyzed azide–alkyne cycloaddition reaction as the key reaction, of bivalent CXCR4 ligands with near infrared (NIR) dyes at the terminus or the center of the poly-l-proline linker. Some of the NIR-labeled ligands, which would be valuable probes useful in studies of the behavior of cells expressing CXCR4, have been obtained. The information concerning the effects of the labeling positions of NIR dyes on their binding properties is useful for the design of modified bivalent-type CXCR4 ligands.