Tang Chu, Wang Xinan, Jin Yushen, Wang Fu
Engineering Research Center of Molecular and Neuro Imaging, Ministry of Education, School of Life Science and Technology, Xidian University, Xi'an, Shaanxi 710126, China; Xianyang Key Laboratory of Molecular Imaging and Drug Synthesis, School of Pharmacy, School of Pharmacy, Shaanxi Institute of International Trade & Commerce, Xianyang 712046, Shaanxi, China.
Engineering Research Center of Molecular and Neuro Imaging, Ministry of Education, School of Life Science and Technology, Xidian University, Xi'an, Shaanxi 710126, China.
Biochim Biophys Acta Rev Cancer. 2022 Sep;1877(5):188788. doi: 10.1016/j.bbcan.2022.188788. Epub 2022 Aug 30.
Histone Deacetylases (HDACs) are abnormally high expressed in various cancers and play a crucial role in regulating gene expression. While HDAC-targeted inhibitors have been rapidly developed and approved in the last twenty years, noninvasive monitoring and visualizing the expression levels of HDACs in tumor tissues might help to early diagnosis in cancer and predict the response to HDAC-targeted cancer therapy. In this review, we summarize the recent advancements in the development of HDAC-targeted probes and their applications in cancer imaging and image-guided surgery. We also discuss the design strategies, advantages and disadvantages of these probes. We hope that this review will provide guidance for the design of HDAC-targeted imaging probes and clinical applications in future.
组蛋白去乙酰化酶(HDACs)在各种癌症中异常高表达,并在调节基因表达中起关键作用。虽然在过去二十年中,针对HDAC的抑制剂已迅速开发并获批,但对肿瘤组织中HDACs表达水平进行无创监测和可视化,可能有助于癌症的早期诊断并预测对HDAC靶向癌症治疗的反应。在本综述中,我们总结了HDAC靶向探针开发的最新进展及其在癌症成像和图像引导手术中的应用。我们还讨论了这些探针的设计策略、优缺点。我们希望本综述将为未来HDAC靶向成像探针的设计和临床应用提供指导。