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Kinase Inhibitor Screening Service

BioAssay Systems has developed and validated a variety of proprietory methods for follow-up study and HTS screening of kinase inhibitors.

1. IMAP Kinase Assay

This fluorescence polarization assay is based on the specific binding of the kinase reaction product, a fluorescent labeled phosphopeptide, to metal-nanoparticles, thus slowing down the rotation of the peptide in solution.

Typical assay optimization steps include enzyme (Figure A) and substrate titrations, interference by dimethyl sulfoxide (DMSO) and Z’ factor determination. For screening kinase inhibitors, the inhibitor is usually incubated with the kinase for 10 min prior to addition of ATP and substrate. Z’ factors of >0.8 are often observed in these assays.

Please contact us by email or call 1-510-782-9988 x 2 to discuss your kinase screening service needs.


2. EKIN Kinase Assay

Our proprietary, homogeneous, microplate-based EKIN kinase assay involves incubating the kinase with a single working reagent. During the kinase reaction, ATP is converted to ADP. The produced ADP is enzymatically converted to ATP and pyruvate, which is quantified using a fluorimetric (530nm/590nm) assay method.

Please contact us by email or call 1-510-782-9988 x 2 to discuss your kinase screening service needs.


Publications

Rommel Mallaria, Elissa Swearingenb, Wei Liu, Arnold Ow, Stephen W. Young and Shu-Gui Huang* (2003) “A Generic High- throughput Screening Assay for Kinases: Protein Kinase A as an Example”. J. Biomol. Screen. 8: 198-204.

Catherine A. Hong, Elissa Swearingen, Rommel Mallari, Xiong Gao, Zhaodan Cao, Anne North, Stephen W. Young and Shu-Gui Huang* (2003) “Development of A High-Throughput Time-Resolved Fluorescence Resonance Energy Transfer Assay for TRAF6 Ubiquitin Polymerization”. Assay and Drug Development Technologies 1: 175-180.

Shu-Gui Huang* (2002) “Development of A High-throughput Screening Assay for Mitochondrial Membrane Potential in Living Cells”. J. Biomol. Screen. 7: 383-389.

Ellyn Farrelly, M. Catherine Amaral, Lisa Marshall and Shu-Gui Huang* (2001) A high-throughput assay for mitochondrial membrane potential in permeabilized yeast cells. Analytical Biochemistry 293(2):269-276.

Tony Smith, John Chan, Donna Oksenberg, Roman Urfer, Dave Wexler, Arnie Ow, Liping Gao, Alanna McAlorum, and Shu-Gui Huang* (2004). A High-Throughput Turbidometric Assay for Screening Inhibitors of Protein Disulfide Isomerase Activity. J. Biomol. Screen. 9(7): 614-620.

David S. Wexler, Liping Gao, Francisco Anderson, Arnold Ow, Laszlo Nadasdi, Alanna McAlorum, Roman Urfer, and Shu-Gui Huang* (2005). “Linking Solubility and Permeability Assays for Maximum Throughput and Reproducibility”. J. Biomol. Screen. 10(4): 383-390.

Shu-Gui Huang (2005) “Progress from HTS to HTL: Current Strategies in Drug Lead Discovery” Review article in Trends in Pharmaceutical Research 1: 5-10.

David S. Wexler, Shu-Gui Huang, Roman Urfer (2004). “Replumbing the Pipeline: A small, biopharmaceutical company’s strategy for integrating lead optimization and ADMET screening”. Current Drug Discovery, May 2004: 35-38.

Shu-Gui Huang, Donna Oksenberg, Roman Urfer (2005). “High-throughput Turbidometric Assay for Screening Inhibitors of Protein Disulfide Isomerase Activity”. US 6,977,142.

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