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Novel assay development and drug screening for known and orphan GPCRs: the PathHunter® Arrestin, internalisation and heterodimerisation assays


Register now! http://tiny.cc/DDW-GPCRWebinar DATE: May 24th, 2011 TIME: 7am PST


G protein-coupled receptors (GPCRs) are the most common molecular drug targets. During early drug discovery, the design and implementation of a high-throughput GPCR functional assay is critical to facilitate screening of large compound libraries required to identify novel drug candidates.


A wide variety of assays are currently available for analysing GPCR signalling events, many of them based on second messenger analysis. PathHunter -Arrestin assays are unique in that they provide a direct measure of GPCR activation by detecting the binding of -Arrestin to the GPCR of interest. Because Arrestin recruitment occurs independent of G-protein coupling, these assays offer a powerful and universal screening platform that can be used with virtually any Gi-, Gs-, or Gq-coupled receptors making them ideal for surrogate ligand discovery, de-orphanisation and receptor profiling.


During the webinar you will learn about the features of the PathHunter technology the ease of implementation of this technology from assay development to full deck HTS screening. We will discuss the utility of the platform for receptor de-orphanisation and interrogation novel GPCR heterodimers.


What will be covered • Description of PathHunter Arrestin technology • Novel application of the technology to studying GPCR heterodimers • Utility of the G-protein independent read-out for interrogating orphan GPCR receptors


Who should attend • Scientists involved in GPCR drug discovery including assay development, high-throughput screening, lead optimisation and pre-clinical


• High-throughput screening scientists interested in ligand fishing and receptor de-orphanisation • Researchers developing novel cell-based assays for GPCRs (heterodimers, internalisation) • Medicinal chemists and biologists optimizing leads from a primary screening campaign • Pharmacologists and cell biologists working in life science laboratories


Panelists include Layton H. Smith, Director of High Throughput Screening, Sanford-Burnham Medical Research Institute Xavier Leroy, Associate Director & Project Leader, Drug Discovery Group, Actelion Pharmaceuticals Tom Wehrman, PhD Senior Research Director, DiscoveRx Corporation


Produced with support from REGISTER TODAY at http://tiny.cc/DDW-GPCRWebinar PANELISTS


Layton H. Smith, Director of High Throughput Screening, Sanford- Burnham Medical Research Institute


Xavier Leroy, Associate Director & Project Leader, Drug Discovery Group, Actelion Pharmaceuticals


Tom Wehrman, PhD, Senior Research Director, DiscoveRx Corporation


MODERATOR


Robert Jordan, Publisher and Editor-in-Chief, Drug Discovery World


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