HTRF: A Technology Tailored for Drug Discovery - A Review of Theoretical Aspects and Recent Applications
Open accessAbstract
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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Cites
Blume-Jensen, P., & Hunter, T. (2001) · Nature · doi:10.1038/35077225 · Cited by 3,738 · see citing works
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 · see citing works
SIGNALLING BY RECEPTOR TYROSINE KINASES
Fantl, W. J., Johnson, D. E., & Williams, L. T. (1993) · Annual Review of Biochemistry · doi:10.1146/annurev.bi.62.070193.002321 · Cited by 1,092 · see citing works
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 · see citing works
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 · see citing works
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 · see citing works
Rare earth cryptates and homogeneous fluoroimmunoassays with human sera
Mathis, G. (1993) · Clinical Chemistry · doi:10.1093/clinchem/39.9.1953 · Cited by 393 · see citing works
Mathis, G. (1995) · Clinical Chemistry · doi:10.1093/clinchem/41.9.1391 · Cited by 339 · see citing works
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 · see citing works
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 · see citing works
ANTENNA EFFECT IN LUMINESCENT LANTHANIDE CRYPTATES: A PHOTOPHYSICAL STUDY
Alpha‐Bazin, B., Ballardini, R., Balzani, V., Lehn, J., Perathoner, S., & Sabbatini, N. (1990) · Photochemistry and Photobiology · doi:10.1111/j.1751-1097.1990.tb04185.x · Cited by 278 · see citing works
GPR30 Does Not Mediate Estrogenic Responses in Reproductive Organs in Mice
Otto, C., Fuchs, I., Kauselmann, G., Kern, H., Zevnik, B., Andreasen, P., Schwarz, G., Altmann, H., Klewer, M., Schoor, M., et al. (2009) · Biology of Reproduction · doi:10.1095/biolreprod.108.071175 · Cited by 278 · see citing works
Jean, A., Conductier, G., Manrique, C., Bouras, C., Berta, P., Hen, R., Charnay, Y., Bockaert, J., & Compan, V. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0701471104 · Cited by 196 · see citing works
Chicoric acid, a new compound able to enhance insulin release and glucose uptake
Tousch, D., Lajoix, A., Hosy, E., Azay, J., Ferrare, K., Jahannault-Talignani, C., Cros, G. H., & Petit, P. (2008) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2008.09.088 · Cited by 177 · see citing works
Bazin, H., Trinquet, E., & Mathis, G. (2002) · Reviews in Molecular Biotechnology · doi:10.1016/s1389-0352(01)00040-x · Cited by 158 · see citing works
Lewis, H. D., Beher, D., Cookson, N., Oakley, A. E., Piggott, M. A., Morris, C. M., Jaros, E., Perry, R., Ince, P. G., Kenny, R. A., et al. (2006) · Neuropathology and Applied Neurobiology · doi:10.1111/j.1365-2990.2006.00696.x · Cited by 143 · see citing works
Bellon, S. F., Kaplan‐Lefko, P. J., Yang, Y., Zhang, Y., Moriguchi, J., Rex, K. L., Johnson, C. W., Rose, P., Long, A. M., O'Connor, A. B., et al. (2007) · Journal of Biological Chemistry · doi:10.1074/jbc.m705774200 · Cited by 140 · see citing works
Trinquet, E., Fink, M., Bazin, H., Grillet, F., Maurin, F., Bourrier, E., Ansanay, H., Leroy, C., Michaud, A., Durroux, T., et al. (2006) · Analytical Biochemistry · doi:10.1016/j.ab.2006.08.002 · Cited by 131 · see citing works
Maurel, D., Kniazeff, J., Mathis, G., Trinquet, E., Pin, J., & Ansanay, H. (2004) · Analytical Biochemistry · doi:10.1016/j.ab.2004.02.013 · Cited by 126 · see citing works
Mathis, G. (1999) · SLAS DISCOVERY · doi:10.1177/108705719900400605 · Cited by 121 · see citing works
Activation of a Dimeric Metabotropic Glutamate Receptor by Intersubunit Rearrangement
Brock, C., Oueslati, N., Soler, S., Boudier, L., Rondard, P., & Pin, J. (2007) · Journal of Biological Chemistry · doi:10.1074/jbc.m702542200 · Cited by 114 · see citing works
Osteoblast expression of an engineered G s -coupled receptor dramatically increases bone mass
Hsiao, E. C., Boudignon, B. M., Chang, W. C., Bencsik, M., Peng, J. C., Nguyen, T., Manalac, C., Halloran, B. P., Conklin, B. R., & Nissenson, R. A. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0707457105 · Cited by 109 · see citing works
Albizu, L., Balestre, M., Breton, C., Pin, J., Manning, M., Mouillac, B., Barberis, C., & Durroux, T. (2006) · Molecular Pharmacology · doi:10.1124/mol.106.025684 · Cited by 108 · see citing works
Homogeneous time-resolved fluorescence and its applications for kinase assays in drug discovery
Jia, Y., Quinn, C. M., Gagnon, A. I., & Talanian, R. V. (2006) · Analytical Biochemistry · doi:10.1016/j.ab.2006.05.006 · Cited by 102 · see citing works
Coupling of Agonist Binding to Effector Domain Activation in Metabotropic Glutamate-like Receptors
Rondard, P., Liu, J., Huang, S., Malhaire, F., Vol, C., Pinault, A., Labesse, G., & Pin, J. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m602277200 · Cited by 98 · see citing works
Ayoub, M. A., Maurel, D., Binet, V., Fink, M., Prézeau, L., Ansanay, H., & Pin, J. (2007) · Molecular Pharmacology · doi:10.1124/mol.106.030304 · Cited by 90 · see citing works
Yamamoto, W., Mikami, T., & Iwamura, H. (2008) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2008.01.010 · Cited by 89 · see citing works
Functioning of the dimeric GABAB receptor extracellular domain revealed by glycan wedge scanning
Rondard, P., Huang, S., Monnier, C., Tu, H., Blanchard, B., Oueslati, N., Malhaire, F., Li, Y., Trinquet, E., Labesse, G., et al. (2008) · The EMBO Journal · doi:10.1038/emboj.2008.64 · Cited by 84 · see citing works
Peres, C. M., Aronoff, D. M., Serezani, C. H., Flamand, N., Faccioli, L. H., & Peters-Golden, M. L. (2007) · The Journal of Immunology · doi:10.4049/jimmunol.179.8.5454 · Cited by 75 · see citing works
Delcourt, N., Thouvenot, É., Chanrion, B., Galéotti, N., Jouin, P., Bockaert, J., & Marin, P. (2007) · The EMBO Journal · doi:10.1038/sj.emboj.7601608 · Cited by 69 · see citing works
Ling, S., Pi, X., & Holoshitz, J. (2007) · The Journal of Immunology · doi:10.4049/jimmunol.179.9.6359 · Cited by 69 · see citing works
Oligomerization of Recombinant and Endogenously Expressed Human Histamine H4 Receptors
van Rijn, R. M., Chazot, P. L., Shenton, F. C., Sansuk, K., Bakker, R. A., & Leurs, R. (2006) · Molecular Pharmacology · doi:10.1124/mol.105.020818 · Cited by 67 · see citing works
Dzyakanchuk, A. A., Balázs, Z., Nashev, L. G., Amrein, K. E., & Odermatt, A. (2008) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2008.08.009 · Cited by 62 · see citing works
Protein Serine Threonine Kinases
Edelman, A. (1987) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.56.1.567 · Cited by 60 · see citing works
The Lysosomal Transmembrane Protein 9B Regulates the Activity of Inflammatory Signaling Pathways
Dodeller, F., Gottar, M., Huesken, D., Iourgenko, V., & Cenni, B. (2008) · Journal of Biological Chemistry · doi:10.1074/jbc.m801908200 · Cited by 58 · see citing works
Romero, G., Sánchez, E., Pujol, M., Pérez, P., Codony, X., Holenz, J., Buschmann, H., & Pauwels, P. J. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706827 · Cited by 57 · see citing works
Viral hijacking of human receptors through heterodimerization
Vischer, H. F., Nijmeijer, S., Smit, M. J., & Leurs, R. (2008) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2008.09.082 · Cited by 57 · see citing works
Inhibition of Early Steps of HIV-1 Replication by SNF5/Ini1
Maroun, M., Delelis, O., Coadou, G., Bader, T., Ségéral, E., Mbemba, G., Petit, C., Sonigo, P., Rain, J., Mouscadet, J. F., et al. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m604849200 · Cited by 52 · see citing works
Functional Adhesiveness of the CX3CL1 Chemokine Requires Its Aggregation
Hermand, P., Pincet, F., Carvalho, S., Ansanay, H., Trinquet, E., Daoudi, M., Combadière, C., & Déterre, P. (2008) · Journal of Biological Chemistry · doi:10.1074/jbc.m802638200 · Cited by 51 · see citing works
Adams, J. W., Wang, J., Davis, J. R., Liaw, C. W., Gaidarov, I., Gatlin, J., Dalton, N. D., Gu, Y., Ross, J., Behan, D. P., et al. (2008) · American Journal of Physiology-Heart and Circulatory Physiology · doi:10.1152/ajpheart.00368.2008 · Cited by 51 · see citing works
Lemay, J., Maidou-Peindara, P., Bader, T., Ennifar, E., Rain, J., Bénarous, R., & Liu, L. X. (2008) · Retrovirology · doi:10.1186/1742-4690-5-47 · Cited by 45 · see citing works
Newton, P., Harrison, P., & Clulow, S. (2008) · SLAS DISCOVERY · doi:10.1177/1087057108321086 · Cited by 45 · see citing works
The ubiquitin E3 ligase POSH regulates calcium homeostasis through spatial control of Herp
Tuvia, S., Taglicht, D., Erez, O., Alroy, I., Alchanati, I., Bicoviski, V., Dori-Bachash, M., Ben-Avraham, D., & Reiss, Y. (2007) · The Journal of Cell Biology · doi:10.1083/jcb.200611036 · Cited by 44 · see citing works
Wang, J., & Norcross, M. A. (2008) · Drug Discovery Today · doi:10.1016/j.drudis.2008.04.004 · Cited by 43 · see citing works
A simple and rapid assay for heparanase activity using homogeneous time-resolved fluorescence
Enomoto, K., Okamoto, H., Numata, Y., & Takemoto, H. (2006) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2006.01.032 · Cited by 42 · see citing works
Liu, K., Titus, S., Southall, N. T., Zhu, P., Inglese, J., Austin, C. P., & Zheng, W. (2008) · Current Chemical Genomics · doi:10.2174/1875397300801010070 · Cited by 42 · see citing works
Schröter, T., Minond, D., Weiser, A. M., Dao, C. T., Habel, J. E., Spicer, T., Chase, P. S., Baillargeon, P., Scampavia, L. D., Schürer, S. C., et al. (2008) · SLAS DISCOVERY · doi:10.1177/1087057107310806 · Cited by 42 · see citing works
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a
Skinner, P. J., Cherrier, M. C., Webb, P. J., Shin, Y., Gharbaoui, T., Lindstrom, A., Hong, V. T. M., Tamura, S. Y., Dang, H. T., Pride, C. C., et al. (2007) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2007.07.101 · Cited by 37 · see citing works
Novel non-steroidal inhibitors of human 11β-hydroxysteroid dehydrogenase type 1
Vicker, N., Su, X., Ganeshapillai, D., Smith, A., Purohit, A., Reed, M. J., & Potter, B. V. L. (2007) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2007.03.023 · Cited by 31 · see citing works
Bergsdorf, C., Kropp-Goerkis, C., Kaehler, I., Ketscher, L., Boemer, U., Parczyk, K., & Bader, B. (2008) · Assay and Drug Development Technologies · doi:10.1089/adt.2007.108 · Cited by 29 · see citing works
Gracias, V. J., Ji, Z., Akritopoulou‐Zanze, I., Abad‐Zapatero, C., Huth, J. R., Song, D., Hajduk, P. J., Johnson, E. F., Glaser, K. B., Marcotte, P. A., et al. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.03.021 · Cited by 29 · see citing works
Novel inhibitor for fibroblast growth factor receptor tyrosine kinase
Kammasud, N., Boonyarat, C., Tsunoda, S., Sakurai, H., Saiki, I., Grierson, D. S., & Vajragupta, O. (2007) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2007.06.058 · Cited by 28 · see citing works
Discovery of Selective Small-Molecule CD80 Inhibitors
Uvebrant, K., Thrige, D. D. G., Rosén, A., Åkesson, M., Berg, H., Walse, B., & Björk, P. (2007) · SLAS DISCOVERY · doi:10.1177/1087057107300464 · Cited by 28 · see citing works
Yabuki, N., Watanabe, S., Kudoh, T., NIHIRA, S.-I., & Miyamoto, C. (1999) · Combinatorial Chemistry & High Throughput Screening · doi:10.2174/1386207302666220204200224 · Cited by 27 · see citing works
Su, X., Vicker, N., Lawrence, H. R., Smith, A., Purohit, A., Reed, M. J., & Potter, B. V. L. (2007) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2007.03.019 · Cited by 25 · see citing works
Histamine Suppresses Fibulin-5 and Insulin-like Growth Factor-II Receptor Expression in Melanoma
Pós, Z., Wiener, Z., Pócza, P., Rácz, M., Tóth, S., Darvas, Z., Molnár, V., Hegyesi, H., & Falus, A. (2008) · Cancer Research · doi:10.1158/0008-5472.can-07-2816 · Cited by 23 · see citing works
Yabuki, N., Watanabe, S., Kudoh, T., et al. (1999) · PubMed · Cited by 22 · see citing works
Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor
Ito, S., Yoshimoto, R., Miyamoto, Y., Mitobe, Y., Nakamura, T., Ishihara, A., MacNeil, D. J., Kanatani, A., & Tokita, S. (2005) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2005.10.066 · Cited by 22 · see citing works
Discovery of thienopyridines as Src-family selective Lck inhibitors
Abbott, L., Betschmann, P., Burchat, A. F., Calderwood, D. J., Davis, H., Hrnčiar, P., Hirst, G. C., Li, B., Morytko, M. J., Mullen, K. D., et al. (2006) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2006.12.035 · Cited by 22 · see citing works
Cascio, M. G., Bisogno, T., Palazzo, E., Thomas, A., van der Stelt, M., Brizzi, A., de Novellis, V., Marabese, I., Ross, R. A., van de Doelen, T., et al. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706888 · Cited by 22 · see citing works
Jia, Y., Quinn, C. M., Clabbers, A., Talanian, R. V., Xu, Y., Wishart, N., & Allen, H. (2005) · Analytical Biochemistry · doi:10.1016/j.ab.2005.11.010 · Cited by 21 · see citing works
Kumpošt, J., Syrová, Z., Kulihova, L., Franková, D., Bologna, J., Hlaváčková, V., Prézeau, L., Králíková, M., Hruskova, B., Pin, J., et al. (2008) · Neuropharmacology · doi:10.1016/j.neuropharm.2008.06.073 · Cited by 21 · see citing works
Current status of HTRF®technology in kinase assays
Jia, Y. (2008) · Expert Opinion on Drug Discovery · doi:10.1517/17460440802518171 · Cited by 19 · see citing works
Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr
Dominguez, C., Smith, L. M., Huang, Q. Z., Yuan, C., Ouyang, X., Cai, L., Chen, P. L., Kim, J. Y., Harvey, T. S., Syed, R. S., et al. (2007) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2007.07.077 · Cited by 17 · see citing works
Leblanc, V., Delaunay, V., Lelong, J., Gas, F., Mathis, G., Grassi, J. J., & May, E. (2002) · Analytical Biochemistry · doi:10.1016/s0003-2697(02)00229-4 · Cited by 17 · see citing works
A homogeneous resonance energy transfer-based assay to monitor MutS/DNA interactions
Lopez‐Crapez, E., Malinge, J., Gatchitch, F., Casano, L., Langlois, T., Pugnière, M., Roquet, F., Mathis, G., & Bazin, H. (2008) · Analytical Biochemistry · doi:10.1016/j.ab.2008.09.004 · Cited by 16 · see citing works
Development of a HTRF® Kinase Assay for Determination of Syk Activity
Harbert, C., Marshall, J., Soh, S. C., & Steger, K. K. (2008) · Current Chemical Genomics · doi:10.2174/1875397300801010020 · Cited by 15 · see citing works
HTRF-Based Assay for Microsomal Prostaglandin E2 Synthase-1 Activity
Goedken, E. R., Gagnon, A. I., Overmeyer, G. T., Liu, J., Petrillo, R. A., Burchat, A. F., & Tomlinson, M. J. (2008) · SLAS DISCOVERY · doi:10.1177/1087057108321145 · Cited by 13 · see citing works
Wang, Y., Malkowski, M. G., Hailey, J., Turek-Etienne, T. C., Tripodi, T., & Pachter, J. A. (2004) · PubMed · Cited by 12 · see citing works
HTRF® KinEASE™ TK: a new solution for tyrosine kinase screening
Tardieu, J.-L. (2007) · Nature Methods · doi:10.1038/nmeth1082 · Cited by 11 · see citing works
Identifying Nonselective Hits from a Homogeneous Calcium Assay Screen
Cassutt, K. J., Orsini, M. J., Abousleiman, M., Colone, D., & Tang, W. (2007) · SLAS DISCOVERY · doi:10.1177/1087057106298538 · Cited by 11 · see citing works
Wang, D.-Y., Lu, Q., Walsh, S. L., Payne, L. A., Modha, S. S., Scott, M. J., Sweitzer, T. D., Ames, R. S., Krosky, D. J., & Li, H. (2008) · Molecular Biotechnology · doi:10.1007/s12033-008-9050-y · Cited by 10 · see citing works
Identification and characterization of small‐molecule inhibitors of Tie2 kinase
Liu, J., Lin, T. H., Cole, A. G., Wen, R., Zhao, L., Brescia, M., Jacob, B., Hussain, Z., Appell, K. C., Henderson, I. M., et al. (2008) · FEBS Letters · doi:10.1016/j.febslet.2008.02.003 · Cited by 8 · see citing works
Maurel, D. (2004) · Analytical Biochemistry · doi:10.1016/s0003-2697(04)00162-9 · Cited by 6 · see citing works
Cellular Ser/Thr-Kinase Assays Using Generic Peptide Substrates
Adams, D. G., Wang, Y., Mak, P. A., Chyba, J., Shalizi, O., Matzen, J., Anderson, P., Smith, T. R., Garcia, M. E., Welch, G. L., et al. (2008) · Current Chemical Genomics · doi:10.2174/1875397300801010054 · Cited by 5 · see citing works
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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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Lanthanide Luminescence for Biomedical Analyses and Imaging
Bünzli, J. G. (2010) · Chemical Reviews · doi:10.1021/cr900362e · Cited by 2,699 · see citing works
Lanthanide NIR luminescence for telecommunications, bioanalyses and solar energy conversion
Bünzli, J. G., & Eliseeva, S. V. (2010) · Journal of Rare Earths · doi:10.1016/s1002-0721(09)60208-8 · Cited by 642 · see citing works
A stable trimeric influenza hemagglutinin stem as a broadly protective immunogen
Impagliazzo, A., Milder, F. J., Kuipers, H., Wagner, M. V., Zhu, X., Hoffman, R. M. B., van Meersbergen, R., Huizingh, J., Wanningen, P., Verspuij, J. W. A., et al. (2015) · Science · doi:10.1126/science.aac7263 · Cited by 591 · see citing works
Naryshkin, N. A., Weetall, M., Dakka, A., Narasimhan, J., Zhao, X., Feng, Z., Ling, K. K. Y., Karp, G. M., Qi, H., Woll, M. G., et al. (2014) · Science · doi:10.1126/science.1250127 · Cited by 524 · see citing works
Modulators of Protein–Protein Interactions
Milroy, L.-G., Grossmann, T. N., Hennig, S., Brunsveld, L., & Ottmann, C. (2014) · Chemical Reviews · doi:10.1021/cr400698c · Cited by 497 · see citing works
Mukhopadhyay, S., Wen, X., Ratti, N., Loktev, A., Rangell, L., Scales, S. J., & Jackson, P. K. (2013) · Cell · doi:10.1016/j.cell.2012.12.026 · Cited by 486 · see citing works
Förster resonance energy transfer – A spectroscopic nanoruler: Principle and applications
Sahoo, H. (2011) · Journal of Photochemistry and Photobiology C Photochemistry Reviews · doi:10.1016/j.jphotochemrev.2011.05.001 · Cited by 409 · see citing works
High-Throughput Screening: today’s biochemical and cell-based approaches
Blay, V., Tolani, B., Ho, S. P., & Arkin, M. R. (2020) · Drug Discovery Today · doi:10.1016/j.drudis.2020.07.024 · Cited by 404 · see citing works
Hang, Y., Boryczka, J., & Wu, N. (2021) · Chemical Society Reviews · doi:10.1039/c9cs00621d · Cited by 384 · see citing works
Doumazane, E., Scholler, P., Zwier, J. M., Trinquet, E., Rondard, P., & Pin, J. (2011) · The FASEB Journal · doi:10.1096/fj.10-163147 · Cited by 324 · see citing works
Zhang, R., & Xie, X. (2012) · Acta Pharmacologica Sinica · doi:10.1038/aps.2011.173 · Cited by 318 · see citing works
Lohse, M. J., Nuber, S., & Hoffmann, C. (2012) · Pharmacological Reviews · doi:10.1124/pr.110.004309 · Cited by 306 · see citing works
Van der Perren, A., Gelders, G., Fenyi, A., Bousset, L., Brito, F., Peelaerts, W., Van den Haute, C., Gentleman, S., Melki, R., & Baekelandt, V. (2020) · Acta Neuropathologica · doi:10.1007/s00401-020-02157-3 · Cited by 277 · see citing works
High density lipoproteins: Measurement techniques and potential biomarkers of cardiovascular risk
Hafiane, A., & Genest, J. J. (2015) · BBA Clinical · doi:10.1016/j.bbacli.2015.01.005 · Cited by 195 · see citing works
Age-dependent SMN expression in disease-relevant tissue and implications for SMA treatment
Ramos, D. M., d’Ydewalle, C. V. O., Gabbeta, V., Dakka, A., Klein, S., Norris, D. A., Matson, J. E., Taylor, S. J., Zaworski, P. G., Prior, T. W., et al. (2019) · Journal of Clinical Investigation · doi:10.1172/jci124120 · Cited by 190 · see citing works
Chemoselective Electrosynthesis Using Rapid Alternating Polarity
Kawamata, Y., Hayashi, K., Carlson, E., Shaji, S., Waldmann, D., Simmons, B. J., Edwards, J. T., Zapf, C. W., Saito, M., & Baran, P. S. (2021) · Journal of the American Chemical Society · doi:10.1021/jacs.1c06572 · Cited by 185 · see citing works
Advances in anion binding and sensing using luminescent lanthanide complexes
Bodman, S. E., & Butler, S. J. (2021) · Chemical Science · doi:10.1039/d0sc05419d · Cited by 173 · see citing works
CA-170 – A Potent Small-Molecule PD-L1 Inhibitor or Not?
Musielak, B., Kocik-Krol, J., Skalniak, Ł., Magiera‐Mularz, K., Sala, D., Czub, M., Stec, M., Siedlar, M., Holak, T. A., & Plewka, J. (2019) · Molecules · doi:10.3390/molecules24152804 · Cited by 171 · see citing works
Emerging degrader technologies engaging lysosomal pathways
Ding, Y., Xing, D., Fei, Y., & Lu, B. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00624c · Cited by 162 · see citing works
Screening Technologies for Small Molecule Discovery: The State of the Art
Janzen, W. P. (2014) · Chemistry & Biology · doi:10.1016/j.chembiol.2014.07.015 · Cited by 149 · see citing works
Cunningham, L., Finckbeiner, S., Hyde, R. K., Southall, N. T., Marugán, J., Yedavalli, V. R. K., Dehdashti, S., Reinhold, W. C., Alemu, L., Zhao, L., et al. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1200037109 · Cited by 133 · see citing works
Sensing with photoluminescent semiconductor quantum dots
Chern, M., Kays, J. C., Bhuckory, S., & Dennis, A. M. (2018) · Methods and Applications in Fluorescence · doi:10.1088/2050-6120/aaf6f8 · Cited by 132 · see citing works
A Selective Luminescent Probe for the Direct Time-Gated Detection of Adenosine Triphosphate
Weitz, E. A., Chang, J. Y., Rosenfield, A. H., & Pierre, V. C. (2012) · Journal of the American Chemical Society · doi:10.1021/ja304373u · Cited by 118 · see citing works
Luminescent Lanthanide Cryptates: from the Bench to the Bedside
Zwier, J. M., Bazin, H., Lamarque, L., & Mathis, G. (2014) · Inorganic Chemistry · doi:10.1021/ic402234k · Cited by 115 · see citing works
Feng, M., Jin, J. Q., Xia, L., Xiao, T., Mei, S., Wang, X., Huang, X., Chen, J., Liu, M., Chen, C., et al. (2019) · Science Advances · doi:10.1126/sciadv.aau5240 · Cited by 111 · see citing works
Kulenkampff, K., Perez, A.-M. W., Sormanni, P., Habchi, J., & Vendruscolo, M. (2021) · Nature Reviews Chemistry · doi:10.1038/s41570-021-00254-9 · Cited by 110 · see citing works
Soulié, M., Latzko, F., Bourrier, E., Placide, V., Butler, S. J., Pál, R., Walton, J. W., Baldeck, P. L., Guennic, B. L., Andraud, C., et al. (2014) · Chemistry - A European Journal · doi:10.1002/chem.201402415 · Cited by 110 · see citing works
Basu, S., Yang, J., Xu, B., Magiera‐Mularz, K., Skalniak, Ł., Musielak, B., Kholodovych, V. V., Holak, T. A., & Hu, L. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00795 · Cited by 106 · see citing works
Insulin: a review of analytical methods
Shen, Y., Prinyawiwatkul, W., & Xu, Z. (2019) · The Analyst · doi:10.1039/c9an00112c · Cited by 102 · see citing works
Application of lanthanide luminescence in probing enzyme activity
Hewitt, S. H., & Butler, S. J. (2018) · Chemical Communications · doi:10.1039/c8cc02824a · Cited by 98 · see citing works
Grichine, A., Haefelé, A., Pascal, S., Alain Duperray, B., Michel, R., Andraud, C., & Maury, O. (2014) · Chemical Science · doi:10.1039/c4sc00473f · Cited by 97 · see citing works
Crystal structure of the human oxytocin receptor
Waltenspühl, Y., Schöppe, J., Ehrenmann, J., Kummer, L., & Plückthun, A. (2020) · Science Advances · doi:10.1126/sciadv.abb5419 · Cited by 95 · see citing works
Scholler, P., Névoltris, D., Bundel, D. D., Bossi, S., Moreno‐Delgado, D., Rovira, X., Møller, T. C., Moustaine, D. E., Mathieu, M., Blanc, É., et al. (2017) · Nature Communications · doi:10.1038/s41467-017-01489-1 · Cited by 94 · see citing works
Detailed resume of RNA m6A demethylases
Shen, D., Wang, B., Gao, Y., Zhao, L., Bi, Y., Zhang, J., Wang, N., Kang, H., Pang, J., Liu, Y., et al. (2022) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2022.01.003 · Cited by 94 · see citing works
Guo, J. L., Braun, D., Fitzgerald, G. A., Hsieh, Y.-T., Rougé, L., Litvinchuk, A., Steffek, M., Propson, N. E., Heffner, C. M., Discenza, C., et al. (2025) · Cell · doi:10.1016/j.cell.2024.10.027 · Cited by 91 · see citing works
Discovering cellular protein‐protein interactions: Technological strategies and opportunities
Titeca, K., Lemmens, I. H., Tavernier, J. H., & Eyckerman, S. (2018) · Mass Spectrometry Reviews · doi:10.1002/mas.21574 · Cited by 90 · see citing works
Prolonged Calcitonin Receptor Signaling by Salmon, but Not Human Calcitonin, Reveals Ligand Bias
Andreassen, K. V., Hjuler, S. T., Furness, S. G., Sexton, P. M., Christopoulos, A., Nosjean, O., Karsdal, M. A., & Henriksen, K. (2014) · PLoS ONE · doi:10.1371/journal.pone.0092042 · Cited by 89 · see citing works
Leyris, J.-P., Roux, T., Trinquet, E., Verdié, P., Fehrentz, J., Oueslati, N., Douzon, S., Bourrier, E., Lamarque, L., Gagne, D., et al. (2010) · Analytical Biochemistry · doi:10.1016/j.ab.2010.09.030 · Cited by 87 · see citing works
Medicinal Chemistry Strategies to Disrupt the p53–MDM2/MDMX Interaction
Lemos, A., Leão, M., Soares, J., Palmeira, A., Pinto, M. M. M., Saraiva, L., & Sousa, M. E. (2016) · Medicinal Research Reviews · doi:10.1002/med.21393 · Cited by 83 · see citing works
Lanthanide-Based Imaging of Protein–Protein Interactions in Live Cells
Rajendran, M., Yapici, E., & Miller, L. W. (2013) · Inorganic Chemistry · doi:10.1021/ic4018739 · Cited by 82 · see citing works
Stabilization of G protein-coupled receptors by point mutations
Heydenreich, F. M., Vuckovic, Z., Matkovic, M., & Veprintsev, D. B. (2015) · Frontiers in Pharmacology · doi:10.3389/fphar.2015.00082 · Cited by 80 · see citing works
McCauliff, L. A., Langan, A., Li, R., Ilnytska, O., Bose, D., Waghalter, M., Lai, K., Kahn, P. C., & Storch, J. (2019) · eLife · doi:10.7554/elife.50832 · Cited by 79 · see citing works
A Homogeneous Chemiluminescent Immunoassay Method
Akhavan-Tafti, H., Binger, D. G., Blackwood, J., Chen, Y., Creager, R. S., de Silva, R., Eickholt, R. A., Gaibor, J. E., Handley, R. S., Kapsner, K. P., et al. (2013) · Journal of the American Chemical Society · doi:10.1021/ja312039k · Cited by 78 · see citing works
Anticancer drug discovery by targeting cullin neddylation
Yu, Q., Jiang, Y., & Sun, Y. (2019) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2019.09.005 · Cited by 77 · see citing works
Cellular Models and Assays to Study NLRP3 Inflammasome Biology
Zito, G., Buscetta, M., Cimino, M., Dino, P., Bucchieri, F., & Cipollina, C. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21124294 · Cited by 77 · see citing works
Functional analysis ofTCF4missense mutations that cause Pitt-Hopkins syndrome
Forrest, M. P., Chapman, R. M., Doyle, A. M., Tinsley, C. L., Waite, A. J., & Blake, D. J. (2012) · Human Mutation · doi:10.1002/humu.22160 · Cited by 73 · see citing works
Bright and stable luminescent probes for target engagement profiling in live cells
Payne, N. C., Kalyakina, A. S., Singh, K., Tye, M. A., & Mazitschek, R. (2021) · Nature Chemical Biology · doi:10.1038/s41589-021-00877-5 · Cited by 72 · see citing works
Zhang, Q., Wu, X., Zhang, H., Wu, Q., Fu, M., Hua, L., Zhu, X., Guo, Y., Zhang, L., You, Q., et al. (2022) · Journal of the American Chemical Society · doi:10.1021/jacs.2c10759 · Cited by 72 · see citing works
Levoye, A., Zwier, J. M., Jaracz‐Ros, A., Klipfel, L., Cottet, M., Maurel, D., Bdioui, S., Balabanian, K., Prézeau, L., Trinquet, E., et al. (2015) · Frontiers in Endocrinology · doi:10.3389/fendo.2015.00167 · Cited by 72 · see citing works
Time-resolved fluorescence ligand binding for G protein–coupled receptors
Emami-Nemini, A., Roux, T., Leblay, M., Bourrier, E., Lamarque, L., Trinquet, E., & Lohse, M. J. (2013) · Nature Protocols · doi:10.1038/nprot.2013.073 · Cited by 71 · see citing works
Time-gated FRET nanoassemblies for rapid and sensitive intra- and extracellular fluorescence imaging
Afsari, H. S., Santos, M. C. D., Lindén, S., Chen, T., Qiu, X., Henegouwen, P. M. P. V. B. E., Jennings, T. L., Susumu, K., Medintz, I. L., Hildebrandt, N., et al. (2016) · Science Advances · doi:10.1126/sciadv.1600265 · Cited by 71 · see citing works
Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening
Kilchmann, F., Marcaida, M. J., Kotak, S., Schick, T., Boss, S. D., Awale, M., Gönczy, P., & Reymond, J. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00709 · Cited by 69 · see citing works
Comparative Analysis of Multiple Immunoassays for Cytokine Profiling in Drug Discovery
Platchek, M., Lu, Q., Tran, H. T., & Xie, W. (2020) · SLAS DISCOVERY · doi:10.1177/2472555220954389 · Cited by 69 · see citing works
Hoffer, L., Voitovich, Y. V., Raux, B., Carrasco, K., Muller, C., Fedorov, A. Y., Derviaux, C., Amouric, A., Betzi, S., Horvath, D., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00653 · Cited by 69 · see citing works
Arezes, J., Foy, N., McHugh, K., Quinkert, D., Benard, S., Sawant, A., Frost, J. N., Armitage, A. E., Pasricha, S., Lim, P. J., et al. (2020) · Blood · doi:10.1182/blood.2019003140 · Cited by 68 · see citing works
Jacobsen, S. E., Nørskov-Lauritsen, L., Thomsen, A. R. B., Smajilovic, S., Wellendorph, P., Larsson, N., Lehmann, A., Bhatia, V. K., & Bräuner‐Osborne, H. (2013) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.113.206276 · Cited by 67 · see citing works
Ma, W., Yang, L., Lv, Y., Fu, J., Zhang, Y., & He, L. (2017) · Journal of Chromatography A · doi:10.1016/j.chroma.2017.04.053 · Cited by 64 · see citing works
Cardiac cAMP: production, hydrolysis, modulation and detection
Boularan, C., & Galès, C. (2015) · Frontiers in Pharmacology · doi:10.3389/fphar.2015.00203 · Cited by 62 · see citing works
In vitro methods for testing antiviral drugs
Rumlová, M., & Ruml, T. (2017) · Biotechnology Advances · doi:10.1016/j.biotechadv.2017.12.016 · Cited by 62 · see citing works
Wildey, M. J., Haunsø, A., Tudor, M., Webb, M. L., & Connick, J. H. (2017) · Annual reports in medicinal chemistry · doi:10.1016/bs.armc.2017.08.004 · Cited by 61 · see citing works
A Novel Bispecific Antibody Targeting PD-L1 and VEGF With Combined Anti-Tumor Activities
Cui, X., Jia, H., Xin, H., Zhang, L. J., Chen, S., Xia, S., Li, X., Xu, W., Chen, X., Feng, Y., et al. (2021) · Frontiers in Immunology · doi:10.3389/fimmu.2021.778978 · Cited by 59 · see citing works
Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme
Maianti, J. P., Tan, G. A., Vetere, A., Welsh, A. J., Wagner, B. K., Seeliger, M. A., & Liu, D. R. (2019) · Nature Chemical Biology · doi:10.1038/s41589-019-0271-0 · Cited by 58 · see citing works
Bashore, F. M., Foley, C. A., Ong, H. W., Rectenwald, J. M., Hanley, R. P., Norris-Drouin, J. L., Cholensky, S. H., Mills, C. A., Pearce, K. H., Herring, L. E., et al. (2023) · ACS Chemical Biology · doi:10.1021/acschembio.2c00804 · Cited by 56 · see citing works
Allosteric modulation and functional selectivity of G protein-coupled receptors
Gao, Z., & Jacobson, K. A. (2012) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2012.08.004 · Cited by 55 · see citing works
Even-Desrumeaux, K., Névoltris, D., Lavaut, M. N., Alim, K., Borg, J., Audebert, S., Kerfélec, B., Baty, D., & Chames, P. (2013) · Molecular & Cellular Proteomics · doi:10.1074/mcp.o112.025486 · Cited by 55 · see citing works
Loison, S., Cottet, M., Orcel, H., Adihou, H., Rahmeh, R., Lamarque, L., Trinquet, E., Kellenberger, E., Hibert, M., Durroux, T., et al. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm3006146 · Cited by 55 · see citing works
Lebek, S., Plößl, A., Baier, M. J., Mustroph, J., Tarnowski, D., Lücht, C. M., Schopka, S., Flörchinger, B., Schmid, C., Zausig, Y. A., et al. (2018) · Journal of Molecular and Cellular Cardiology · doi:10.1016/j.yjmcc.2018.03.020 · Cited by 55 · see citing works
Imamura, T., Yanagihara, Y. T., Ohyagi, Y., Nakamura, N., Iinuma, K., Yamasaki, R., Asai, H., Maeda, M., Murakami, K., Irie, K., et al. (2020) · Neurobiology of Disease · doi:10.1016/j.nbd.2020.104739 · Cited by 55 · see citing works
A Reader-Based Assay for m6A Writers and Erasers
Wiedmer, L., Eberle, S. A., Bedi, R. K., Sledz, P., & Caflisch, A. (2019) · Analytical Chemistry · doi:10.1021/acs.analchem.8b05500 · Cited by 54 · see citing works
Toward the identification of viral cap-methyltransferase inhibitors by fluorescence screening assay
Aouadi, W., Eydoux, C., Coutard, B., Martin, B., Debart, F., Vasseur, J., Contreras, J. M., Morice, C., Quérat, G., Jung, M., et al. (2017) · Antiviral Research · doi:10.1016/j.antiviral.2017.06.021 · Cited by 54 · see citing works
Hewitt, S. H., Parris, J., Mailhot, R., & Butler, S. J. (2017) · Chemical Communications · doi:10.1039/c7cc05887j · Cited by 53 · see citing works
Couturier, C., & Deprez, B. (2012) · Frontiers in Endocrinology · doi:10.3389/fendo.2012.00100 · Cited by 52 · see citing works
Target Engagement Assays in Early Drug Discovery
John‐Campbell, S. S., & Bhalay, G. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c03115 · Cited by 53 · see citing works
Nørskov-Lauritsen, L., Thomsen, A. R. B., & Bräuner‐Osborne, H. (2014) · International Journal of Molecular Sciences · doi:10.3390/ijms15022554 · Cited by 52 · see citing works
In Vitro Expressed GPCR Inserted in Polymersome Membranes for Ligand‐Binding Studies
May, S., Ochsner, M., Fu, Z., Low, Y. X., Tan, D., de Hoog, H. M., Ritz, S., Nallani, M., & Sinner, E. (2012) · Angewandte Chemie International Edition · doi:10.1002/anie.201204645 · Cited by 52 · see citing works
Kopra, K., Vuorinen, E., Blanco, M. A., Wang, Q., Eskonen, V., Gillette, W., Pulliainen, A. T., Holderfield, M. T., & Härmä, H. (2020) · Analytical Chemistry · doi:10.1021/acs.analchem.9b05126 · Cited by 52 · see citing works
Effects of pharmacological modulators of α-synuclein and tau aggregation and internalization
Dominguez‐Meijide, A., Vasili, E., König, A., Cima‐Omori, M., de Opakua, A. I., Leonov, A., Ryazanov, S., Zweckstetter, M., Griesinger, C., & Outeiro, T. F. (2020) · Scientific Reports · doi:10.1038/s41598-020-69744-y · Cited by 51 · see citing works
Time-Gated FRET Detection for Multiplexed Biosensing
Zwier, J. M., & Hildebrandt, N. (2017) · Reviews in fluorescence · doi:10.1007/978-3-319-48260-6_3 · Cited by 50 · see citing works
Recent Advances on Luminescent Enhancement-Based Porous Silicon Biosensors
Jenie, S. N. A., Plush, S. E., & Voelcker, N. H. (2016) · Pharmaceutical Research · doi:10.1007/s11095-016-1889-1 · Cited by 50 · see citing works
Barrile, F., M’Kadmi, C., Francesco, P. N. D., Cabral, A., Romero, G. G., Mustafá, E. R., Cantel, S., Damian, M., Mary, S., Denoyelle, S., et al. (2019) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2019.110573 · Cited by 50 · see citing works
HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors
Koneru, P. C., Francis, A. C., Deng, N., Rebensburg, S. V., Hoyte, A. C., Lindenberger, J., Adu-Ampratwum, D., Larue, R. C., Wempe, M. F., Engelman, A. N., et al. (2019) · eLife · doi:10.7554/elife.46344 · Cited by 49 · see citing works
PD-L1 + neutrophils contribute to injury-induced infection susceptibility
Thanabalasuriar, A., Chiang, A. J., Morehouse, C. A., Camara, M., Hawkins, S., Keller, A. E., Koksal, A. C., Caceres, C. S., Berlin, A. A., Holoweckyj, N., et al. (2021) · Science Advances · doi:10.1126/sciadv.abd9436 · Cited by 49 · see citing works
Heeres, J. T., & Hergenrother, P. J. (2010) · Chemical Society Reviews · doi:10.1039/b923660k · Cited by 49 · see citing works
Inability of Some Commercial Assays to Measure Suppression of Glucagon Secretion
Albrechtsen, N. J. W., Veedfald, S., Plamboeck, A., Deacon, C. F., Hartmann, B., Knop, F. K., Vilsbøll, T., & Holst, J. J. (2015) · Journal of Diabetes Research · doi:10.1155/2016/8352957 · Cited by 49 · see citing works
Quantifying autophagy using novel LC3B and p62 TR-FRET assays
Bresciani, A., Spiezia, M. C., Boggio, R., Cariulo, C., Nordheim, A., Altobelli, R., Kuhlbrodt, K., Dominguez, C., Muñoz-Sanjuán, I., Wityak, J., et al. (2018) · PLoS ONE · doi:10.1371/journal.pone.0194423 · Cited by 47 · see citing works
Haas, E., Eltemur, R. D. I., Hentrich, T., Huridou, C., Schmidt, T., Casadei, N., Maringer, Y., Bahl, C., Zimmermann, F., Mills, J. D., et al. (2021) · Molecular Neurobiology · doi:10.1007/s12035-021-02610-8 · Cited by 47 · see citing works
Gul, S., & Hadian, K. (2014) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2014.954544 · Cited by 46 · see citing works
Fluorescence lifetime plate reader: Resolution and precision meet high-throughput
Petersen, K. J., Peterson, K. C., Muretta, J. M., Higgins, S. E., Gillispie, G. D., & Thomas, D. D. (2014) · Review of Scientific Instruments · doi:10.1063/1.4900727 · Cited by 46 · see citing works
Key role of the CCR2-CCL2 axis in disease modification in a mouse model of tauopathy
Ben-Yehuda, H., Arad, M., Ramos, J. M. P., Sharon, E., Castellani, G., Ferrera, S., Cahalon, L., Colaiuta, S. P., Salame, T., & Schwartz, M. (2021) · Molecular Neurodegeneration · doi:10.1186/s13024-021-00458-z · Cited by 46 · see citing works
Lad, L., Clancy, S., Kovalenko, M. A., Liu, C., Hui, T., Smith, V., & Pagratis, N. C. (2014) · SLAS DISCOVERY · doi:10.1177/1087057114560123 · Cited by 46 · see citing works
Grütter, C., Sreeramulu, S., Sessa, G., & Rauh, D. (2013) · Journal of Molecular Biology · doi:10.1016/j.jmb.2013.07.034 · Cited by 45 · see citing works
The power of combining phenotypic and target-focused drug discovery
Heilker, R., Lessel, U. F., & Bischoff, D. (2018) · Drug Discovery Today · doi:10.1016/j.drudis.2018.10.009 · Cited by 45 · see citing works
A cell-free approach to accelerate the study of protein–protein interactions in vitro
Sierecki, E., Giles, N., Polinkovsky, M. E., Moustaqil, M. D., Alexandrov, K. A., & Gambin, Y. (2013) · Interface Focus · doi:10.1098/rsfs.2013.0018 · Cited by 44 · see citing works
Conley, J. M., Brand, C. S., Bogard, A. S., Pratt, E. P. S., Xu, R., Hockerman, G. H., Ostrom, R. S., Dessauer, C. W., & Watts, V. J. (2013) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.113.207449 · Cited by 41 · see citing works
Fodale, V., Kegulian, N. C., Verani, M., Cariulo, C., Azzollini, L., Petricca, L., Daldin, M., Boggio, R., Padova, A., Kuhn, R. R., et al. (2014) · PLoS ONE · doi:10.1371/journal.pone.0112262 · Cited by 41 · see citing works
Protein–Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery
Milhas, S., Raux, B., Betzi, S., Derviaux, C., Roche, P., Restouin, A., Basse, M.-J., Rebuffet, E., Lugari, A., Badol, M., et al. (2016) · ACS Chemical Biology · doi:10.1021/acschembio.6b00286 · Cited by 41 · see citing works
Studies Pertaining to the Emerging Cannabinoid Hexahydrocannabinol (HHC)
Nasrallah, D. J., & Garg, N. K. (2023) · ACS Chemical Biology · doi:10.1021/acschembio.3c00254 · Cited by 40 · see citing works
Characterization of 12 GnRH peptide agonists – a kinetic perspective
Nederpelt, I., Georgi, V., Schiele, F., Nowak‐Reppel, K., Fernández‐Montalván, A. E., IJzerman, A. P., & Heitman, L. H. (2015) · British Journal of Pharmacology · doi:10.1111/bph.13342 · Cited by 40 · see citing works
Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors
Kutil, Z., Mikešová, J., Zessin, M., Meleshin, M., Nováková, Z., Alquicer, G., Kozikowski, A. P., Sippl, W., Bařinka, C., & Schutkowski, M. (2019) · ACS Omega · doi:10.1021/acsomega.9b02808 · Cited by 40 · see citing works
Europium-Complex-Grafted Polymer Dots for Amplified Quenching and Cellular Imaging Applications
Li, Q., Zhang, J., Sun, W., Yu, J., Wu, C., Qin, W., & Chiu, D. T. (2014) · Langmuir · doi:10.1021/la501876m · Cited by 40 · see citing works
- 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)
- 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
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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