Abstract
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.
| Original language | English |
|---|---|
| Journal | Advanced Drug Delivery Reviews |
| DOIs | |
| State | Accepted/In press - 1 Jan 2018 |
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Keywords
- Drug-target engagement
- Fluorescence anisotropy imaging
- Fluorescence polarization, fluorescence anisotropy
- Fluorescently labeled drugs
- Intravital imaging
- Single-cell pharmacodynamics
- Two photon microscopy
Cite this
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Fluorescence anisotropy imaging in drug discovery. / Vinegoni, Claudio; Feruglio, Paolo Fumene; Gryczynski, Ignacy; Mazitschek, Ralph; Weissleder, Ralph.
In: Advanced Drug Delivery Reviews, 01.01.2018.Research output: Contribution to journal › Article › Research › peer-review
TY - JOUR
T1 - Fluorescence anisotropy imaging in drug discovery
AU - Vinegoni, Claudio
AU - Feruglio, Paolo Fumene
AU - Gryczynski, Ignacy
AU - Mazitschek, Ralph
AU - Weissleder, Ralph
PY - 2018/1/1
Y1 - 2018/1/1
N2 - 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.
AB - 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.
KW - Drug-target engagement
KW - Fluorescence anisotropy imaging
KW - Fluorescence polarization, fluorescence anisotropy
KW - Fluorescently labeled drugs
KW - Intravital imaging
KW - Single-cell pharmacodynamics
KW - Two photon microscopy
UR - http://www.scopus.com/inward/record.url?scp=85044723741&partnerID=8YFLogxK
U2 - 10.1016/j.addr.2018.01.019
DO - 10.1016/j.addr.2018.01.019
M3 - Article
JO - Advanced Drug Delivery Reviews
JF - Advanced Drug Delivery Reviews
SN - 0169-409X
ER -