靶向 CXCR4 趋化因子受体的多价氧化铁纳米粒子。

Multivalency in CXCR4 chemokine receptor targeted iron oxide nanoparticles.

机构信息

Centre of Nanotechnology, King Abdul-Aziz University, Jeddah, Saudi Arabia and Department of Chemistry, University of Hull, Cottingham Road, Hull, HU6 7RX, UK.

Department of Biomedical Sciences and PET Research Centre, University of Hull Cottingham Road, Hull, HU6 7RX, UK.

出版信息

Dalton Trans. 2021 Feb 9;50(5):1599-1603. doi: 10.1039/d0dt02626c.

DOI:10.1039/d0dt02626c

PMID:33502425

Abstract

The CXCR4 chemokine receptor is an important biomolecular target in cancer diagnostics and therapeutics. In a new multivalent approach, iron oxide nanoparticles were conjugated with multiple binding units of a low affinity azamacrocylic CXCR4 antagonist. The silica coated nanostructure has good suspension stability, a mode size of 72 nm and high affinity for CXCR4, showing >98% inhibition of anti-CXCR4 mAb binding in a receptor binding competition assay on Jurkat cells.

摘要

趋化因子受体 4（CXCR4）是癌症诊断和治疗的重要生物分子靶标。在一种新的多价方法中，氧化铁纳米粒子与低亲和力氮杂大环 CXCR4 拮抗剂的多个结合单位连接。这种硅涂层纳米结构具有良好的悬浮稳定性、72nm 的模态尺寸和对 CXCR4 的高亲和力，在 Jurkat 细胞的受体结合竞争测定中，对抗-CXCR4 mAb 结合的抑制率超过 98%。