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环氧化酶的传感与成像剂

Sensing and Imaging Agents for Cyclooxygenase Enzyme.

作者信息

Rao Cheekatla Subba, Murale Dhiraj P, Gopala Lavanya, Lee Jun-Seok

机构信息

Department of Pharmacology, Korea University, 73 Goryeodae-ro, Seongbuk-gu, Seoul, 02841, South Korea.

Chemical and Biological Integrative Research Center, Korea Institute of Science and Technology, 5 Hwarang-ro 14-gil, Seoul, South Korea.

出版信息

ChemMedChem. 2025 Feb 1;20(3):e202400636. doi: 10.1002/cmdc.202400636. Epub 2024 Nov 20.

Abstract

In this concept, we present a comprehensive study on the development and application of COX-2-specific fluorescent probes for cancer imaging and diagnosis. To target cancer cells and measuring cancer-related activities in specific organelles quickly and accurately are crucial factors for early diagnosis and research on cancer pathology and treatment. This concept explores a variety of probes based on indomethacin (IMC), celecoxib, rofecoxib as well as CoxFluor and each one demonstrates unique mechanisms and high selectivity towards COX-2 enzymes. These probes were designed to enhance fluorescence upon binding to COX-2 which enable precise visualization of tumor and inflamed tissues. The research emphasizes the importance of COX-2 as a biomarker in cancer diagnostics, particularly in identifying cancer stem cells and inflamed tissues. This concept highlights the potentiality of these probes in non-invasive imaging techniques which offering significant advancements in cancer diagnosis and monitoring. The in vivo and in vitro experiments, including applications in mouse models and human tissue samples, confirm the efficacy of these probes in providing detailed imaging for clinical and research applications.

摘要

在本概念中,我们对用于癌症成像和诊断的COX-2特异性荧光探针的开发与应用进行了全面研究。靶向癌细胞并快速准确地测量特定细胞器中与癌症相关的活性,是癌症早期诊断以及癌症病理学与治疗研究的关键因素。本概念探索了基于吲哚美辛(IMC)、塞来昔布、罗非昔布以及CoxFluor的多种探针,每一种都展现出独特的作用机制以及对COX-2酶的高选择性。这些探针经设计可在与COX-2结合时增强荧光,从而实现对肿瘤组织和炎症组织的精确可视化。该研究强调了COX-2作为癌症诊断生物标志物的重要性,特别是在识别癌症干细胞和炎症组织方面。本概念突出了这些探针在非侵入性成像技术中的潜力,这为癌症诊断和监测带来了重大进展。体内和体外实验,包括在小鼠模型和人体组织样本中的应用,证实了这些探针在为临床和研究应用提供详细成像方面的有效性。

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