FEB 22, 2018 01:30 PM PST

Recent Trends in GPCR Drug Discovery: Novel Targets, New Disease Indications, and an Upsurge in Biologics

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  • Associate-Professor, Pharmaceutical Sciences, Midwestern University
      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".


    GPCRs constitute the largest receptor family in the human genome. Over the years they have proven themselves to be druggable targets accounting for about 1/3 of all drugs on the market today.  Of these, approximately 15% have been approved by the US Food and Drug Administration (FDA) in the last 5 years.  Recent GPCR drug discovery efforts are expanding the range of disease indications to include polycystic ovarian syndrome, gastroparesis, pulmonary fibrosis, and smoking cessation. This talk will cover some of the novel targets, such as the calcitonin gene-related peptide (CGRP) receptor, the bile acid receptor GPBAR, the hydroxycarboxylic acid (HCA2 and HCA3) receptors, and orphan GPCRs such as GPR119.  Also covered will be the development of antibody-based therapeutics for GPCRs such as mogamulizumab for the chemokine receptor CCR4. 

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