Department of Ultrasound Medicine, Second Affiliated Hospital of Anhui Medical University, Hefei, 230601, P. R. China.
South China Advanced Institute for Soft Matter Science and Technology, School of Emergent Soft Matter, South China University of Technology, Guangzhou, 510640, P. R. China.
Macromol Biosci. 2023 Jul;23(7):e2300048. doi: 10.1002/mabi.202300048. Epub 2023 Mar 25.
Fluorous tagged peptides have shown promising features for biomedical applications such as drug delivery and multimodal imaging. The bioconjugation of fluoroalkyl ligands onto cargo peptides greatly enhances their proteolytic stability and membrane penetration via a proposed "fluorine effect". The tagged peptides also efficiently deliver other biomolecules such as DNA and siRNA into cells via a co-assembly strategy. The fluoroalkyl chains on peptides with antifouling properties enable efficient gene delivery in the presence of serum proteins. Besides intracellular biomolecule delivery, the amphiphilic peptides can be used to stabilized perfluorocarbon-filled microbubbles for ultrasound imaging. The fluorine nucleus on fluoroalkyls provides intrinsic probes for background-free magnetic resonance imaging. Labeling of fluorous tags with radionuclide F also allows tracing the biodistribution of peptides via positron emission tomography imaging. This mini-review will discuss properties and mechanism of the fluorous tagged peptides in these applications.
氟标记肽在药物输送和多模态成像等生物医学应用中显示出有前景的特性。通过所谓的“氟效应”，将氟烷基配体与货物肽缀合可极大地提高其蛋白水解稳定性和膜穿透性。标记肽还可以通过共组装策略将其他生物分子（如 DNA 和 siRNA）有效地递送到细胞中。具有抗污性质的肽上的氟烷基链可在存在血清蛋白的情况下有效进行基因传递。除了细胞内生物分子的递送外，两亲性肽还可用于稳定含全氟碳的微泡以进行超声成像。氟烷基上的氟核为无背景磁共振成像提供了固有探针。放射性核素 F 对氟标记的标记也允许通过正电子发射断层扫描成像追踪肽的生物分布。这篇迷你综述将讨论这些应用中氟标记肽的特性和机制。
