文章：

荧光激酶抑制剂的设计原理及其在癌症同步生物成像与治疗中的应用

Design Principles and Applications of Fluorescent Kinase Inhibitors for Simultaneous Cancer Bioimaging and Therapy

原文发布日期：30 October 2024

DOI: 10.3390/cancers16213667

类型: Article

开放获取: 是

英文摘要：

Kinase inhibitors are potent therapeutic agents in cancer treatment, but their effectiveness is frequently restricted by the inability to image the tumor microenvironment. To address this constraint, kinase inhibitor–fluorophore conjugates have emerged as promising theranostic agents, allowing for simultaneous cancer diagnosis and treatment. These conjugates are gaining attention for their ability to visualize malignant tissues and concurrently enhance therapeutic interventions. This review explores the design principles governing the development of multimodal inhibitors, highlighting their potential as platforms for kinase tracking and inhibition via bioimaging. The structural aspects of constructing such theranostic agents are critically analyzed. This work could shed light on this intriguing field and provide adequate impetus for developing novel theranostic compounds based on small molecule inhibitors and fluorophores.

摘要翻译： 

激酶抑制剂是癌症治疗中的强效治疗剂，但其疗效常因无法对肿瘤微环境进行成像而受限。为突破这一限制，激酶抑制剂-荧光团偶联物已成为前景广阔的治疗诊断剂，可实现癌症的同步诊断与治疗。这类偶联物因其可视化恶性组织并同步增强治疗干预的能力而备受关注。本综述探讨了多模态抑制剂开发的设计原则，重点阐述了其作为通过生物成像实现激酶追踪与抑制平台的潜力。文章对构建此类诊疗剂的结构要素进行了批判性分析，有望为该前沿领域提供新的见解，并为基于小分子抑制剂和荧光团开发新型诊疗化合物提供充分动力。

原文链接：

Design Principles and Applications of Fluorescent Kinase Inhibitors for Simultaneous Cancer Bioimaging and Therapy