Fluorescence anisotropy imaging in drug discovery

Claudio Vinegoni, Paolo Fumene Feruglio, Ignacy Gryczynski, Ralph Mazitschek, Ralph Weissleder

Research output: Contribution to journalReview articlepeer-review

32 Scopus citations


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 languageEnglish
Pages (from-to)262-288
Number of pages27
JournalAdvanced Drug Delivery Reviews
StatePublished - 1 Nov 2019


  • Drug-target engagement
  • Fluorescence anisotropy imaging
  • Fluorescence polarization, fluorescence anisotropy
  • Fluorescently labeled drugs
  • Intravital imaging
  • Single-cell pharmacodynamics
  • Two photon microscopy


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