Cited by 522Advanced Biosensing Techniques and ApplicationsAdvanced Fluorescence Microscopy TechniquesReceptor Mechanisms and Signaling

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HTRF: A Technology Tailored for Drug Discovery - A Review of Theoretical Aspects and Recent Applications

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Degorce, Francois·2009·Current Chemical Genomics

DOI 10.2174/1875397300903010022PMC PMC2802762

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Abstract

HTRF (Homogeneous Time Resolved Fluorescence) is the most frequently used generic assay technology to measure analytes in a homogenous format, which is the ideal platform used for drug target studies in high-throughput screening (HTS). This technology combines fluorescence resonance energy transfer technology (FRET) with time-resolved measurement (TR). In TR-FRET assays, a signal is generated through fluorescent resonance energy transfer between a donor and an acceptor molecule when in close proximity to each other. Buffer and media interference is dramatically reduced by dual-wavelength detection, and the final signal is proportional to the extent of product formation. The HTRF assay is usually sensitive and robust that can be miniaturized into the 384 and 1536-well plate formats. This assay technology has been applied to many antibody-based assays including GPCR signaling (cAMP and IP-One), kinases, cytokines and biomarkers, bioprocess (antibody and protein production), as well as the assays for protein-protein, proteinpeptide, and protein-DNA/RNA interactions.Since its introduction to the drug-screening world over ten years ago, researchers have used HTRF to expedite the study of GPCRs, kinases, new biomarkers, protein-protein interactions, and other targets of interest. HTRF has also been utilized as an alternative method for bioprocess monitoring. The first-generation HTRF technology, which uses Europium cryptate as a fluorescence donor to monitor reactions between biomolecules, was extended in 2008 through the introduction of a second-generation donor, Terbium cryptate (Tb), enhancing screening performance. Terbium cryptate possesses different photophysical properties compared to Europium, including increased quantum yield and a higher molar extinction coefficient. In addition to being compatible with the same acceptor fluorophors used with Europium, it can serve as a donor fluorophore to green-emitting fluors because it has multiple emission peaks including one at 490 nm. Moreover, all Terbium HTRF assays can be read on the same HTRF-compatible instruments as Europium HTRF assays.Overall, HTRF is a highly sensitive, robust technology for the detection of molecular interactions in vitro and is widely used for primary and secondary screening phases of drug development. This review addresses the general principles of HTRF and its current applications in drug discovery.

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Oncogenic kinase signalling.
Blume-Jensen, P., & Hunter, T. (2001) · Nature · doi:10.1038/35077225 · Cited by 3,738
PROTEIN SERINE/THREONINE KINASES
Edelman, A. M., Blumenthal, D., & Krebs, E. G. (1987) · Annual Review of Biochemistry · doi:10.1146/annurev.bi.56.070187.003031 · Cited by 1,435
SIGNALLING BY RECEPTOR TYROSINE KINASES
Fantl, W. J., Johnson, D. E., & Williams, L. T. (1993) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.62.1.453 · Cited by 1,118
Presynaptic Control of Striatal Glutamatergic Neurotransmission by Adenosine A 1 –A 2A Receptor Heteromers
Ciruela, F., Casadó, V., Rodrigues, R. J., Luján, R., Burgueño, J., Canals, M., Borycz, J., Rebola, N., Goldberg, S. R., Mallol, J., et al. (2006) · Journal of Neuroscience · doi:10.1523/jneurosci.3574-05.2006 · Cited by 591
Principles and Biophysical Applications of Lanthanide-Based Probes
Selvin, P. R. (2002) · Annual Review of Biophysics and Biomolecular Structure · doi:10.1146/annurev.biophys.31.101101.140927 · Cited by 549
Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to GPCR oligomerization
Maurel, D., Comps‐Agrar, L., Brock, C., Rives, M., Bourrier, E., Ayoub, M. A., Bazin, H., Tinel, N., Durroux, T., Prézeau, L., et al. (2008) · Nature Methods · doi:10.1038/nmeth.1213 · Cited by 500
Rare earth cryptates and homogeneous fluoroimmunoassays with human sera
Mathis, G. (1993) · Clinical Chemistry · doi:10.1093/clinchem/39.9.1953 · Cited by 393
Probing molecular interactions with homogeneous techniques based on rare earth cryptates and fluorescence energy transfer
Mathis, G. (1995) · Clinical Chemistry · doi:10.1093/clinchem/41.9.1391 · Cited by 339
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Levoye, A., Dam, J., Ayoub, M. A., Guillaume, J., Couturier, C., Delagrange, P., & Jockers, R. (2006) · The EMBO Journal · doi:10.1038/sj.emboj.7601193 · Cited by 335
Dopamine D2 receptors form higher order oligomers at physiological expression levels
Guo, W. X., Urizar, E., Králíková, M., Mobarec, J. C., Shi, L., Filizola, M., & Javitch, J. A. (2008) · The EMBO Journal · doi:10.1038/emboj.2008.153 · Cited by 334

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[23]Amoravain M Lyotard S Jaga D Lebreton ML Servent F Bomer U Introduction of a new HTRF acceptor, d2: Development of a complete GPCR platform for a Gs, Gi and Gq screening SBS 2005 11th Annual Conference Geneva

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Authors: Degorce, F.
Venue: Current Chemical Genomics
Publisher: Bentham Science Publishers Ltd.
Published: 2009-03-17
Volume: 3
Issue: 1
Pages: 22-32
ISSN: 1875-3973 (ISSN-L)
DOI: 10.2174/1875397300903010022
PMC: PMC2802762
OpenAlex: W2073113196
Cited by: 501
References: 74
Citations by year: 2026: 29 · 2025: 31 · 2024: 35 · 2023: 37 · 2022: 31 · 2021: 53 · 2020: 35 · 2019: 29 · 2018: 34 · 2017: 28 · 2016: 23 · 2015: 25 · 2014: 39 · 2013: 28 · 2012: 26
FWCI: 5.90
Type: journal article
Language: en
Open access: diamond
doi.org
Licence: cc-by
Locations: Current Chemical Genomics (publishedVersion, cc-by)
PubMed Central (publishedVersion, cc-by-nc)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Advanced Biosensing Techniques and Applications
Life Sciences › Biochemistry, Genetics and Molecular Biology › Biophysics › Advanced Fluorescence Microscopy Techniques
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords: homogeneous time-resolved fluorescence, time-resolved fluorescence resonance energy transfer, drug discovery, high-throughput screening, fluorescence resonance energy transfer, europium cryptate, G protein-coupled receptor signaling, kinase activity assay, protein-protein interaction, bioprocess monitoring, antibody-based assays, biomarkers

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