Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Department of Biochemistry and Biophysics, University of Pennsylvania, Philadelphia, PA 19104, USA.
Int J Mol Sci. 2019 Nov 19;20(22):5808. doi: 10.3390/ijms20225808.
The discovery of penicillin began the age of antibiotics, which was a turning point in human healthcare. However, to this day, microbial infections are still a concern throughout the world, and the rise of multidrug-resistant organisms is an increasing challenge. To combat this threat, diagnostic imaging tools could be used to verify the causative organism and curb inappropriate use of antimicrobial drugs. Nuclear imaging offers the sensitivity needed to detect small numbers of bacteria in situ. Among nuclear imaging tools, radiolabeled antibiotics traditionally have lacked the sensitivity or specificity necessary to diagnose bacterial infections accurately. One reason for the lack of success is that the antibiotics were often chelated to a radiometal. This was done without addressing the ramifications of how the radiolabeling would impact probe entry to the bacterial cell, or the mechanism of binding to an intracellular target. In this review, we approach bacterial infection imaging through the lens of bacterial specific molecular targets, their intracellular or extracellular location, and discuss radiochemistry strategies to guide future probe development.
青霉素的发现开启了抗生素时代,这是人类医疗保健的一个转折点。然而,时至今日,微生物感染仍然是全世界关注的问题,而多药耐药菌的出现更是带来了日益严峻的挑战。为了应对这一威胁,可以使用诊断成像工具来验证病原体,并遏制抗菌药物的不当使用。核成像技术具有检测原位少量细菌的所需的灵敏度。在核成像工具中,放射性标记的抗生素传统上缺乏准确诊断细菌感染所需的灵敏度或特异性。缺乏成功的一个原因是抗生素通常与放射性金属螯合。这样做没有考虑放射性标记如何影响探针进入细菌细胞的后果,也没有考虑与细胞内靶标结合的机制。在这篇综述中,我们通过细菌特异性分子靶标、它们在细胞内或细胞外的位置的视角来探讨细菌感染成像,并讨论放射化学策略以指导未来探针的开发。