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APR 05, 2017 9:00 AM PDT

Sense and Sensitivity: Screening and Characterization of fragment binders against WT GPCR drug targets using highly sensitive Biacore S200

Speaker
  • Functional Leader, Biacore at GE Healthcare
    Biography
      Dr. Belcher is the Functional Leader, Biacore at GE Healthcare. He received his Ph.D. in organic chemistry from the University of Newcastle upon Tyne in the United Kingdom in 2003. During his postdoctoral training, he worked under George Pettit at Arizona State University working on the first total synthesis of the natural product dolastatin 16, a potential cancer therapeutic. While at Arizona State, Paul established a label-free screening program for screening/characterization of large libraries of compounds to enable the development of synthetic probes to challenging targets. At GE his focus has been on the value of drug-target binding kinetics for investigating structure-activity relationships and drug efficacy. He also works on fragment-based lead discovery, interacting predominately with small molecule screening groups within academia and industry to implement and optimize label-free methods for drug discovery. He is a frequent speaker and has given over 500 lectures at conferences and pharma/biotech industry sites and Universities globally.

    Abstract

    G protein coupled receptors (GPCRs) are the targets of 30-40% of all approved drugs. However many approaches successfully applied to drug discovery for soluble protein targets have made a limited impact on GPCR’s due to challenges in obtaining pure, active, membrane free receptors for structural and biophysical investigation. Biophysical techniques in combination with improvements in protein engineering and handling have advanced to face the challenges of studying membrane bound GPCR’s with SPR in particular becoming increasingly utilized in the study of GPCR’s as the sensitivity of the detections systems has improved. Here we present the results from a collaboration with the Hopkins-Navratilova lab at the University of Dundee highlighting the importance of instrument sensitivity characterizing GPCR’s with the Biacore™ S200.


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