Biagiotti Giacomo, Angeli Andrea, Giacomini Arianna, Toniolo Gianluca, Landini Luca, Salerno Gianluca, Di Cesare Mannelli Lorenzo, Ghelardini Carla, Mello Tommaso, Mussi Silvia, Ravelli Cosetta, Marelli Marcello, Cicchi Stefano, Menna Enzo, Ronca Roberto, Supuran Claudiu T, Richichi Barbara
Department of Chemistry "Ugo Schiff", University of Firenze, Via della Lastruccia 13, Sesto Fiorentino, 50019 Florence, Italy.
Consorzio Interuniversitario Nazionale per la Scienza e Tecnologia dei Materiali (INSTM, Via G. Giusti, 9, 50121 Firenze, Florence, Italy.
ACS Appl Nano Mater. 2021 Dec 24;4(12):14153-14160. doi: 10.1021/acsanm.1c03603. Epub 2021 Nov 17.
The bioimaging of cancer cells by the specific targeting of overexpressed biomarkers is an approach that holds great promise in the identification of selective diagnostic tools. Tumor-associated human carbonic anhydrase (hCA) isoforms IX and XII have been considered so far as well-defined biomarkers, with their expression correlating with cancer progression and aggressiveness. Therefore, the availability of highly performant fluorescent tools tailored for their targeting and able to efficiently visualize such key targets is in high demand. We report here on the design and synthesis of a kind of quantum dot (QD)-based fluorescent glyconanoprobe coated with a binary mixture of ligands, which, according to the structure of the terminal domains, impart specific property sets to the fluorescent probe. Specifically, monosaccharide residues ensured the dispersibility in the biological medium, CA inhibitor residues provided specific targeting of membrane-anchored hCA IX overexpressed on bladder cancer cells, and the quantum dots imparted the optical/fluorescence properties.
通过特异性靶向过表达的生物标志物对癌细胞进行生物成像，是一种在识别选择性诊断工具方面极具前景的方法。肿瘤相关的人类碳酸酐酶（hCA）同工型IX和XII，迄今已被视为明确的生物标志物，其表达与癌症进展和侵袭性相关。因此，迫切需要能够针对其进行靶向且能有效可视化此类关键靶点的高性能荧光工具。我们在此报告一种基于量子点（QD）的荧光糖纳米探针的设计与合成，该探针涂覆有配体二元混合物，根据末端结构域的结构，赋予荧光探针特定的性能集。具体而言，单糖残基确保了在生物介质中的分散性，CA抑制剂残基提供了对膀胱癌细胞上过表达的膜锚定hCA IX的特异性靶向，而量子点赋予了光学/荧光特性。
