Fluorescence anisotropy imaging in drug discovery.
Drug-target engagement
Fluorescence anisotropy imaging
Fluorescence polarization, fluorescence anisotropy
Fluorescently labeled drugs
Intravital imaging
Single-cell pharmacodynamics
Two photon microscopy
Journal
Advanced drug delivery reviews
ISSN: 1872-8294
Titre abrégé: Adv Drug Deliv Rev
Pays: Netherlands
ID NLM: 8710523
Informations de publication
Date de publication:
Historique:
received:
17
07
2017
revised:
29
01
2018
accepted:
30
01
2018
pubmed:
8
2
2018
medline:
2
10
2020
entrez:
8
2
2018
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 29410158
pii: S0169-409X(18)30027-9
doi: 10.1016/j.addr.2018.01.019
pmc: PMC6072632
mid: NIHMS942534
pii:
doi:
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
262-288Subventions
Organisme : NIGMS NIH HHS
ID : P50 GM107618
Pays : United States
Organisme : NIBIB NIH HHS
ID : R01 EB010011
Pays : United States
Organisme : NHLBI NIH HHS
ID : R01 HL122208
Pays : United States
Organisme : NCI NIH HHS
ID : T32 CA079443
Pays : United States
Informations de copyright
Copyright © 2018 Elsevier B.V. All rights reserved.
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