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FEB 24, 2021 1:30 PM PST

Roundtable Panel Presentation: Recent Trends in Screening GPCRs

C.E. Credits: P.A.C.E. CE Florida CE
Speakers
  • Associate-Professor, Pharmaceutical Sciences, Midwestern University
    Biography
      An Associate Professor with Midwestern University, and adjunct faculty member at Northwestern University Dr. Annette Gilchrist has a PhD in Immunology from the University of Connecticut Health Center and a MS in Biochemistry from the University of Connecticut. Previously, she was with Cue Biotech and Caden Biosciences, companies she co-founded that focused on identifying modulators of G protein-coupled receptors (GPCRs) utilizing novel approaches (US Patent Numbers 6,559,128; 7,208,279; and 7,294,472). Her current research is on allosteric and functionally selective modulators of GPCRs with her primary receptors of interest being the chemokine receptor CCR1 and the recently deorphanized FFAR2. She is an International Editor for the British Journal of Clinical Pharmacology and recently served as a guest co-editor for a Frontiers in Endocrinology Bone Research themed issue on "Chemokines and Bone".
    • Director Biomedical Innovation, The University of Western Australia
      Biography

        Professor Pfleger is Director, Biomedical Innovation at The University of Western Australia (UWA) and the MTPConnect Western Australian Life Sciences Innovation Hub. He is also Head of Molecular Endocrinology and Pharmacology at the UWA Centre for Medical Research and Harry Perkins Institute of Medical Research, Deputy Director of the Australian Research Council Centre for Personalised Therapeutics Technologies, Chief Scientific Advisor to Dimerix and co-founder of RAGE Biotech. Professor Pfleger currently serves on the Board of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists and is a member of the British Pharmacological Society International Advisory Group. Professor Pfleger has developed extensive expertise in profiling receptor binding and function at the molecular and cellular levels over the last 20 years, particularly involving G protein-coupled receptors (GPCRs). He also has globally-recognised expertise in the bioluminescence resonance energy transfer (BRET) technology, including his patented Receptor-Heteromer Investigation Technology (Receptor-HIT) for studying heteromers.

      • Principal Scientist, GPCR Therapeutics
        Biography

          Dr. Juan José Fung is a Principal Scientist at GPCR Therapeutics, Inc, a drug discovery company focused on targeting GPCR heteromers in cancer, located in Seoul, Korea. Dr. Fung received his Ph.D. from the Stanford University School of Medicine under the mentorship of Dr. Brian Kobilka, studying dimerization of GPCRs. Dr. Fung continued his Postdoctoral training in Dr. Kobilka’s lab contributing to the elucidation of high-resolution structures of GPCRs. Dr. Fung has spent significant time in industry studying membrane proteins, antibodies and HTS methods for drug discovery. His current work is mainly focused on assay development to bridge the gap between in vitro and in vivo GPCR pharmacology.

        • Sr. Scientist, Chemical Biology and Proteomics group, AstraZeneca
          Biography

            Aarti Kawatkar was trained as an organic chemist, obtaining her M.S. from the University of Georgia at Athens in 2005 with Prof. Geert-Jan Boons. She started her industrial career as a medicinal chemist at Vertex, and in 2008, she moved to AstraZeneca as a lead chemist in both oncology and the fragment based lead generation group contributing to the discovery of several clinical candidates. In 2013 she joined AstraZeneca’s newly created Chemical Biology group, focusing on small molecule target deconvolution and target engagement, supporting multiple drug discovery projects at different stages from hit identification to lead optimization to clinical candidates selection. In the chemical biology group, Aarti has championed the application of the CEllular Thermal Shift Assay (CETSA) and in-cell Chemoproteomics to measure cellular target engagement and target validation for multipass transmembrane protein receptors. Aarti’s efforts in studying difficult targets was recognized in 2017 with AstraZeneca’s Breakthrough Scientist of the Year award for "Innovative techniques for profiling target engagement and selectivity for multipass transmembarne proteins".  Again in 2020, she was awarded for finding the target of a small molecule modulator of inflammation.

          • Founder, Dr. GPCR
            Biography

              Dr. Yamina A. Berchiche is the founder of Dr. GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors (GPCRs), that control virtually everything in the body, as drug targets. The mission of Dr. GPCR is to accelerate GPCR drug discovery by sharing the latest research and technology advances in the field and provide exposure to scientists through the Dr. GPCR podcast. Dr. Berchiche obtained her Master’s and Ph.D. in Biochemistry at the University of Montreal in Canada before training at The Rockefeller University in New York and the National Institutes of Health in Bethesda, Maryland. She developed expertise over the past 2 decades studying structure/function relationships of GPCRs using live cell bioluminescence resonance energy transfer (BRET). Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the body.

            • Co-Founder & CSO, Blue Therapeutics
              Biography

                Ajay Yekkirala is a co-founder of Blue Therapeutics, a platform company focused on utilizing the power of receptor-interactomicsTM to develop novel therapies.  He is the co-inventor of Blue’s core technology and has over 15 years of experience in GPCR and ion channel drug discovery and development. Ajay completed his doctoral studies with ACS hall of fame chemist, Dr. Philip Portoghese, at the University of Minnesota and postdoctoral training under renowned pain neurobiologist Clifford Woolf at Harvard. He has authored several papers published in high-impact, peer-reviewed journals, including book chapters and invited reviews. He is also a recipient of the Bacaner Research Award from the Minnesota Medical Foundation.


              Abstract

              G protein-coupled receptors (GPCRs) are among the most intensively studied drug targets, and account for about ~34% of all drugs approved by the FDA.  Examples of drugs targeting GPCRs include anti-histamines, β-blockers and ACE inhibitors. In the past, high-throughput methodologies for GPCR screening largely involved the measurement of second messenger production such as Ca2+, cAMP, and inositol phosphate (IP). Over the last decade there have been a number of advances in receptor pharmacology, breakthroughs in structural biology, and innovations in biotechnology, that together have led to several novel strategies to target this important receptor class. For example, since 2014, researchers have harnessed CRISPR technology to knockout (KO) GPCRs, GPCR-associated signaling proteins, or knock-in normal or mutated GPCRs. The panel will discuss some of these approaches including assays that directly quantify receptor coupling to heterotrimeric G proteins and β-arrestin, advancements using rational drug design and AI-based approaches, the increased interest in GPCR-targeting mAbs, and the increased appreciation for the role of pharmacogenomics.

              Learning Objectives:

              1. Identify some of the challenges to screening GPCRs

              2. Describe some of the emerging technologies being used for GPCRs


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