Keywords: Hts, Ikkβ, Tr-Fret, Z′ Factor, Dimethyl Sulfoxide, Glutathione Transferase, Histidine, I Kappa B Kinase Beta, I Kappa B Kinase Inhibitor, Article, Controlled Study, Enzyme Activity, Enzyme Assay, Fluorescence Resonance Energy Transfer, High Throughput Screening, Priority Journal, High-Throughput Screening Assays, I-Kappa B Kinase, I-Kappa B Proteins, Time Factors, Z Factor, Methods, Metabolism,
Affiliations: *** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini, CNR, Via Mezzocannone, 16, 80134, Napoli, Italy
Dipartimento Delle Scienze Biologiche, Università di Napoli, Federico II, Napoli, Italy
References: Strnad, J., Burke, J.R., IkappaB kinase inhibitors for treating autoimmune and inflammatory disorders: Potential and challenges (2007) Trends Pharmacol Sci, 28, pp. 142-14
Goldstein, D.M., Gray, N.S., Zarrinkar, P.P., High-throughput kinase profiling as a platform for drug discovery (2008) Nat Rev Drug Discov, 7, pp. 391-397
Oliver Von Ahsen, U.B., High-throughput screening for kinase inhibitors (2005) ChemBioChem, 6, pp. 481-490
Sera, T., Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors (2007) Tanpakushitsu Kakusan Koso, 52 (SUPPL.), pp. 1812-1813
Thaimattam, R., Banerjee, R., Miglani, R., Iqbal, J., Protein kinase inhibitors: Structural insights into selectivity (2007) Curr Pharm des, 13, pp. 2751-2765
Klumpp, M., Boettcher, A., Becker, D., Meder, G., Blank, J., Leder, L., Readout technologies for highly miniaturized kinase assays applicable to high-throughput screening in a 1536-well format (2006) J Biomol Screen, 11, pp. 617-633
Xu, Q.H., Wang, S., Korystov, D., Mikhailovsky, A., Bazan, G.C., Moses, D., The fluorescence resonance energy transfer (FRET) gate: A time-resolved study (2005) Proc Natl Acad Sci USA, 102, pp. 530-535
Moshinsky, D.J., Ruslim, L., Blake, R.A., Tang, F., Widely applicable, high-throughput TR-FRET assay for the measurement of kinase autophosphorylation: VEGFR-2 as a prototype (2003) J Biomol Screen, 8, pp. 447-452
Bazin, H., Trinquet, E., Mathis, G., Time resolved amplification of cryptate emission: A versatile technology to trace biomolecular interactions (2002) J Biotechnol, 82, pp. 233-250
Zhang, J.H., Chung, T.D., Oldenburg, K.R., A simple statistical parameter for use in evaluation and validation of high throughput screening assays (1999) J Biomol Screen, 4, pp. 67-73
Podolin, P.L., Callahan, J.F., Bolognese, B.J., Li, Y.H., Carlson, K., Davis, T.G., Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of Iκb kinase 2, TPCA-1 (2-[(aminocarbonyl) amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell proliferation (2005) J Pharmacol Exp Ther, 312, pp. 373-381
Goldstein, D. M., Gray, N. S., Zarrinkar, P. P., High-throughput kinase profiling as a platform for drug discovery (2008) Nat Rev Drug Discov, 7, pp. 391-397
Xu, Q. H., Wang, S., Korystov, D., Mikhailovsky, A., Bazan, G. C., Moses, D., The fluorescence resonance energy transfer (FRET) gate: A time-resolved study (2005) Proc Natl Acad Sci USA, 102, pp. 530-535
Moshinsky, D. J., Ruslim, L., Blake, R. A., Tang, F., Widely applicable, high-throughput TR-FRET assay for the measurement of kinase autophosphorylation: VEGFR-2 as a prototype (2003) J Biomol Screen, 8, pp. 447-452
Zhang, J. H., Chung, T. D., Oldenburg, K. R., A simple statistical parameter for use in evaluation and validation of high throughput screening assays (1999) J Biomol Screen, 4, pp. 67-73
Podolin, P. L., Callahan, J. F., Bolognese, B. J., Li, Y. H., Carlson, K., Davis, T. G., Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of I b kinase 2, TPCA-1 (2- [(aminocarbonyl) amino] -5- (4-fluorophenyl) -3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell proliferation (2005) J Pharmacol Exp Ther, 312, pp. 373-381
Optimizing A Kinase Assay For Ikkbeta On An Hts Station