当前位置: X-MOL 学术Adv. Drug Deliver. Rev. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Fluorescence anisotropy imaging in drug discovery.
Advanced Drug Delivery Reviews ( IF 16.1 ) Pub Date : 2018-02-02 , DOI: 10.1016/j.addr.2018.01.019
Claudio Vinegoni 1 , Paolo Fumene Feruglio 2 , Ignacy Gryczynski 3 , Ralph Mazitschek 1 , Ralph Weissleder 1
Affiliation  

Non-invasive measurement of drug-target engagement can provide critical insights in the molecular pharmacology of small molecule drugs. Fluorescence polarization/fluorescence anisotropy measurements are commonly employed in protein/cell screening assays. However, the expansion of such measurements to the in vivo setting has proven difficult until recently. With the advent of high-resolution fluorescence anisotropy microscopy it is now possible to perform kinetic measurements of intracellular drug distribution and target engagement in commonly used mouse models. In this review we discuss the background, current advances and future perspectives in intravital fluorescence anisotropy measurements to derive pharmacokinetic and pharmacodynamic measurements in single cells and whole organs.

中文翻译:

药物发现中的荧光各向异性成像。

药物靶标结合的非侵入性测量可以为小分子药物的分子药理学提供重要的见解。荧光偏振/荧光各向异性测量通常用于蛋白质/细胞筛选测定。然而,直到最近,将此类测量扩展到体内环境仍很困难。随着高分辨率荧光各向异性显微镜的出现,现在可以在常用的小鼠模型中对细胞内药物分布和靶标参与进行动力学测量。在这篇综述中,我们讨论了活体荧光各向异性测量的背景、当前进展和未来前景,以得出单细胞和整个器官的药代动力学和药效学测量。
更新日期:2020-04-20
down
wechat
bug