Three birds one stone: an enzyme-activatable theragnostic agent for fluorescence diagnosis, photodynamic and inhibitor therapies

• Published in: Chemical communications (Cambridge, England) Vol. 59; no. 31; pp. 4676 - 4679
• Main Authors: Yue, Xiuxiu, Wang, Benhua, Lan, Minhuan, Fan, Jiangli, Song, Xiangzhi, Foley, James W
• Format: Journal Article
• Language: English
• Published: England Royal Society of Chemistry 13.04.2023
• Subjects: Breast Neoplasms - diagnostic imaging; Breast Neoplasms - drug therapy; Cell Line, Tumor; Female; Fluorescence; Humans; Inhibitors; Photochemotherapy - methods; Photosensitizing Agents - pharmacology; Photosensitizing Agents - therapeutic use; Reagents; Tumor Microenvironment
• ISSN: 1359-7345; 1364-548X
• DOI: 10.1039/d3cc00214d

AX11890 , an inhibitor of overexpressed enzyme, KIAA1363, in some breast cancers, was conjugated with a benzo[ a ]phenothiazinium photosensitizer to develop a tumor micro-environment-responsive photosensitizer NBS-L-AX . In normal cells, the special geometry of NBS-L-AX causes the fluorescence and photodynamic therapeutic (PDT) effect of NBS-L to be quenched. In cancer cells, when allowed to interact with the enzyme KIAA1363, the geometry of NBS-L-AX changes such that it becomes fluorescent and photodynamically active. Thus, the material of NBS-L-AX serves as an activated imaging and PDT treatment agent for breast cancers. In addition, NBS-L-AX also shows a selective inhibition effect against breast cancer cells. By integrating the inhibitor of KIAA1363 enzyme, AX11890 , into a red-absorbing dye, a tumor microenvironmental-responsive photosensitizer, NBS-L-AX , was developed for selective fluorescence imaging and activatable PDT therapy for breast cancers.