氨肽酶,在人体中具有关键作用的酶,正在成为代谢过程和疾病的重要生物标志物。氨基肽酶水平异常通常与疾病有关,尤其是癌症。小分子探针,如荧光,荧光/光声,生物发光,和化学发光探针,是研究氨肽酶相关疾病的重要工具。荧光探针提供对蛋白质活动的实时见解,在特定位置提供高灵敏度,和精确的时空结果。此外,光声探针提供能够穿透更深组织的信号。生物发光和化学发光探针可以通过减少背景来增强体内成像能力。这篇全面的综述集中在对四种关键氨肽酶有反应的小分子探针:氨肽酶N,亮氨酸氨基肽酶,焦谷氨酸氨基肽酶1和丙氨酰氨基肽酶,以及它们在肿瘤和患病区域成像中的应用。在这次审查中,小分子探针的设计策略,以前研究的各种设计,并讨论了未来生物成像应用的机会,作为未来研究的路线图,引发氨肽酶响应探针开发的创新,并增强我们对这些酶在疾病诊断和治疗中的理解。
Aminopeptidases, enzymes with critical roles in human body, are emerging as vital biomarkers for metabolic processes and diseases. Aberrant
aminopeptidase levels are often associated with diseases, particularly cancer. Small-molecule probes, such as fluorescent, fluorescent/photoacoustics, bioluminescent, and chemiluminescent probes, are essential tools in the study of aminopeptidases-related diseases. The fluorescent probes provide real-time insights into protein activities, offering high sensitivity in specific locations, and precise spatiotemporal results. Additionally, photoacoustic probes offer signals that are able to penetrate deeper tissues. Bioluminescent and chemiluminescent probes can enhance in vivo imaging abilities by reducing the background. This comprehensive review is focused on small-molecule probes that respond to four key aminopeptidases:
aminopeptidase N, leucine
aminopeptidase, Pyroglutamate
aminopeptidase 1, and Prolyl
Aminopeptidase, and their utilization in imaging tumors and afflicted regions. In this review, the design strategy of small-molecule probes, the variety of designs from previous studies, and the opportunities of future bioimaging applications are discussed, serving as a roadmap for future research, sparking innovations in
aminopeptidase-responsive probe development, and enhancing our understanding of these enzymes in disease diagnostics and treatment.