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Reports Outline Pharmacology Study Results from Y.J. Zhu et al (Integrating High-Content Analysis into a Multiplexed Screening Approach to Identify...

September 10, 2014



Reports Outline Pharmacology Study Results from Y.J. Zhu et al (Integrating High-Content Analysis into a Multiplexed Screening Approach to Identify and Characterize GPCR Agonists)

By a News Reporter-Staff News Editor at Biotech Week -- Current study results on Pharmacology have been published. According to news reporting out of Watertown, Massachusetts, by NewsRx editors, research stated, "G protein-coupled receptors (GPCRs) are one of the most popular and proven target classes for therapeutic intervention. The increased appreciation for allosteric modulation, receptor oligomerization, and biased agonism has led to the development of new assay platforms that seek to capitalize on these aspects of GPCR biology."

Our news journalists obtained a quote from the research, "High-content screening is particularly well suited for GPCR drug discovery given the ability to image and quantify changes in multiple cellular parameters, to resolve subcellular structures, and to monitor events within a physiologically relevant environment. Focusing on the sphingosine-1-phosphate (S1P1) receptor, we evaluated the utility of high-content approaches in hit identification efforts by developing and applying assays to monitor beta-arrestin translocation, GPCR internalization, and GPCR recycling kinetics. Using these approaches in combination with more traditional GPCR screening assays, we identified compounds whose unique pharmacological profiles would have gone unnoticed if using a single platform. In addition, we identified a compound that induces an atypical pattern of beta-arrestin translocation and GPCR recycling kinetics."

According to the news editors, the research concluded: "Our results highlight the value of high-content imaging in GPCR drug discovery efforts and emphasize the value of a multiassay approach to study pharmacological properties of compounds of interest."

For more information on this research see: Integrating High-Content Analysis into a Multiplexed Screening Approach to Identify and Characterize GPCR Agonists. Journal of Biomolecular Screening, 2014;19(7):1079-1089. Journal of Biomolecular Screening can be contacted at: Sage Publications Inc, 2455 Teller Rd, Thousand Oaks, CA 91320, USA. (Sage Publications - www.sagepub.com/; Journal of Biomolecular Screening - jbx.sagepub.com)

Our news journalists report that additional information may be obtained by contacting Y.J. Zhu, Forma Therapeut, High Throughput Screening, Watertown, MA, United States. Additional authors for this research include J. Watson, M.J. Chen, D.R. Shen, M. Yarde, M. Agler, N. Burford, A. Alt, S. Jayachandra, M.E. Cvijic, L.T. Zhang, A. Dyckman, J.N. Xie, J. O'Connell, M. Banks and A. Weston (see also Pharmacology).

Keywords for this news article include: Watertown, Massachusetts, United States, North and Central America, Pharmacology, Therapy

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC


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Source: Biotech Week


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