近红外荧光二价 RGD 配体用于整合素 αvβ₃ 靶向光学成像。
Near-infrared fluorescent divalent RGD ligand for integrin αvβ₃-targeted optical imaging.
机构信息
Department of Radiology, Optical Radiology Laboratory, Washington University School of Medicine, 4525 Scott Avenue, Saint Louis, MO 63108, USA.
出版信息
Bioorg Med Chem Lett. 2012 Sep 1;22(17):5405-9. doi: 10.1016/j.bmcl.2012.07.044. Epub 2012 Jul 20.
Abstract
A new near-infrared fluorescent compound containing two cyclic RGD motifs, cypate-c(RGDfK) (1), was synthesized based on a carbocyanine fluorophore bearing two carboxylic acid groups (cypate) for integrin α(v)β(3)-targeting. Compared with its monovalent counterpart cypate-c(RGDfK) (2), 1 exhibited remarkable improvements in integrin α(v)β(3) binding affinity and tumor uptake in nude mice of A549. The results suggest that cypate-linked divalent ligands can serve as an important molecular platform for exploring receptor-targeted optical imaging and treatment of various diseases.
摘要
一种新的近红外荧光化合物，包含两个环状 RGD 基序，cypate-[c(RGDfK)] (2)（1），是基于带有两个羧酸基团的碳菁荧光团（cypate）合成的，用于整合素 α(v)β(3)靶向。与单价类似物 cypate-c(RGDfK)（2）相比，1 在裸鼠 A549 中显示出对整合素 α(v)β(3)结合亲和力和肿瘤摄取的显著提高。结果表明，cypate 连接的二价配体可以作为探索受体靶向光学成像和治疗各种疾病的重要分子平台。
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