A novel porphyrin-based theranostic agent activated by cysteine over-expressed in cancer cells shows promise for tumour-targeted monitoring and phototherapy
{"title":"A novel porphyrin-based theranostic agent activated by cysteine over-expressed in cancer cells shows promise for tumour-targeted monitoring and phototherapy","authors":"Fumihisa Ishida, Satoe Moriya, Daisuke Takahashi, Kazunobu Toshima","doi":"10.1016/j.bmc.2025.118131","DOIUrl":null,"url":null,"abstract":"<div><div><span>l</span>-Cysteine (Cys) is a tumor-related biomarker. The photo- and Cys-activatable theranostic agent <strong>4</strong> was designed and synthesized based on 5,10,15,20-tetrakis(4-hydroxyphenyl)porphyrin (<strong>3</strong>). Compound <strong>4</strong> exhibited negligible fluorescence and photosensitizing activity in the absence of Cys. However, when activated by Cys, <strong>3</strong> was released, resulting in fluorescence and photosensitization. Moreover, upon irradiation with 660 nm light, <strong>4</strong> displayed selective and effective fluorescence and photo-cytotoxicity exclusively against cancer cells, such as HeLa and A549 cells, which express high levels of Cys. This wavelength of light falls within the phototherapeutic window.</div></div>","PeriodicalId":255,"journal":{"name":"Bioorganic & Medicinal Chemistry","volume":"121 ","pages":"Article 118131"},"PeriodicalIF":3.0000,"publicationDate":"2025-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0968089625000720","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/2/23 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
l-Cysteine (Cys) is a tumor-related biomarker. The photo- and Cys-activatable theranostic agent 4 was designed and synthesized based on 5,10,15,20-tetrakis(4-hydroxyphenyl)porphyrin (3). Compound 4 exhibited negligible fluorescence and photosensitizing activity in the absence of Cys. However, when activated by Cys, 3 was released, resulting in fluorescence and photosensitization. Moreover, upon irradiation with 660 nm light, 4 displayed selective and effective fluorescence and photo-cytotoxicity exclusively against cancer cells, such as HeLa and A549 cells, which express high levels of Cys. This wavelength of light falls within the phototherapeutic window.
期刊介绍：
Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides.
The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
