NOV 09, 2016 9:00 AM PST

A duplexed assay to measure GPCR-mediated calcium signaling and β-Arrestin recruitment from single well using FDSS/µCell functional screening system

Sponsored by: DiscoverX, DiscoverX
Speaker
  • Head of Molecular and Cellular Pharmacology, Bioprojet Biotech
    Biography
      Dr. Thierry Calmels is currently heading the Molecular and Cellular Pharmacology department at Bioprojet Biotech, with a focus on Neuroscience and Inflammation therapeutic areas. Dr. Calmels' main research focus is on G-protein Coupled Receptors (GPCRs) with the aim of setting up screening and secondary assays, as well as to dissect their signaling mechanisms for proposed drug targets. Dr. Calmels has specialized in implementing calcium mobilization assays for GPCRs in drug discovery as well as for human iPSC-derived cardiomyocytes in cardiac safety. Dr. Calmels got his Ph.D. in Applied Genetics at the University of Toulouse (France), after which he moved to Pittsburgh (USA) for a Post-Doc in Pharmacology with Dr. J. Lazo. After spending 3 years in Pittsburgh, Dr. Calmels joined the Molecular Oncology department with Pr. D. Stéhelin at the Pasteur Institute in Lille, France, followed by 5 years at GlaxoSmithKline (GSK) within the Cardiology Unit before joining Bioprojet in 2001.

    Abstract
    DATE: November 9th, 2016
    TIME: 9:00 AM PT, 12:00 PM ET


    The screening and functional characterization of novel ligands for G-Protein Coupled Receptors (GPCR) remains a key focus in drug discovery. Of late, an increasing awareness of the subtleties of receptor signaling and potential for ligand bias requires multiple endpoints to be monitored for the same screening campaign. In addition, efforts to reduce costs and improve efficiency of screening are always a key consideration for any screening campaign. In this webinar, we describe a duplexed assay for the Histamine H1 receptor using the PathHunter β-arrestin clonal cell line from DiscoverX. We have adapted existing assay protocols to monitor intracellular calcium signaling in real time along with the recruitment of β-arrestin to the Histamine H1 receptor, from the same well on a plate. We discuss protocol development and successful implementation of the final assay with this multiplexing approach, through data presented on Histamine H1 agonists and antagonist pharmacology. This duplexed assay clearly demonstrates an overall increase in screening efficiency and a total reduction in cost for running similar screening, lead optimization, and characterization programs for GPCR drug discovery.
     
    Learning Objective 1 : Screening approaches for GPCR drug discovery
     
    Learning Objective 2 :Creating a duplexed assay to monitor Calcium and β-arrestin in a single well
     

    Show Resources
    You May Also Like
    APR 07, 2020 8:00 AM PDT
    C.E. CREDITS
    APR 07, 2020 8:00 AM PDT
    DATE: April 7, 2020 TIME: 8:00am PT, 11:00am ET This webinar sets out to establish why quality control is key to robust, reliable, reproducible science. We will look at best practice criteri...
    JAN 23, 2020 9:00 AM PST
    C.E. CREDITS
    JAN 23, 2020 9:00 AM PST
    DATE: January 23, 2020 TIME: 9:00am PST, 12:00pm EST...
    MAY 08, 2020 10:00 AM PDT
    C.E. CREDITS
    MAY 08, 2020 10:00 AM PDT
    DATE: May 8, 2020 TIME: 10:00am PT, 11:00am MT, 1:00pm ET The application of next generation sequencing to interrogate immune repertoires and methods in which these highly complex dataset...
    MAR 24, 2020 10:00 AM PDT
    C.E. CREDITS
    MAR 24, 2020 10:00 AM PDT
    DATE: March 24, 2020 TIME: 10:00 am PDT, 1:00pm EDT The Clampfit software module is a useful tool to manipulate and analyze electrophysiological data acquired by pCLAMP™ software. Rece...
    JUN 09, 2020 3:00 PM CEST
    Add to Calendar Select one of the following: iCal Google Calendar Outlook Calendar Yahoo Calendar
    C.E. CREDITS
    JUN 09, 2020 3:00 PM CEST
    Add to Calendar Select one of the following: iCal Google Calendar Outlook Calendar Yahoo Calendar
    DATE: June 9, 2020 TIME: 6am PT, 9am ET, 3pm CEST The importance of disposable plastic consumables and their overall impact on the experimental workflow of qPCR has been taken into considera...
    MAY 13, 2020 4:00 PM CEST
    C.E. CREDITS
    MAY 13, 2020 4:00 PM CEST
    DATE: May 13, 2020 TIME: 7am PT, 10am ET, 4pm CEST Stem cells represent an important tool in a wide range of applications, including basic research, disease modeling, drug discovery, and reg...
    Loading Comments...
    Show Resources
    Attendees
    • See more