SC1: Introduction to GPCR-Based Drug Discovery
TUESDAY, SEPTEMBER 25, 2:00 - 5:00 PM
Room: Fairfax

This course will provide an understanding of the pharmacological complexities of G protein-coupled receptors (GPCRs) as well as some of the tools used to study them in a drug discovery setting. The course is well-suited for biologists, pharmacologists and medicinal chemists who have recently started working with GPCRs or for those who need a refresher on the latest technological advances and newest paradigms.

Topics to Be Discussed:

  • GPCR pharmacology including allosteric modulation, biased signaling, persistent signaling, and accessory proteins
  • Key structural features of GPCRs relevant to rational drug design
  • Current clinical candidates targeting novel GPCRs including peptide GPCRs and orphan GPCRs
  • Advances in GPCR-targeted biologics such as erenumab for calcitonin gene-related peptide (CGRP) receptor and namacizumab for the cannabinoid 1 (CB1) receptor
  • Emerging GPCR screening methods including cellular redistribution assays, affinity mass spectrometry, and biosensors
  • Recent advances in pharmacogenomics of GPCRs

Instructor Biography:

Annette Gilchrist, PhD, Professor, Pharmacology, Midwestern University

Dr. Gilchrist works on allosteric and/or biased modulators for a number of different GPCRs including PAR1, CCR1, and FFAR2. She also serves as an International Editor for the British Journal of Clinical Pharmacology. In addition to editing the book “GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions” published by John Wiley and Sons she has written chapters on G protein signaling and CCR1 antagonists.

Dr. Gilchrist recently served with Dr. Paula Stern as a guest editor for Frontiers in Endocrinology for a themed issue on “Chemokines and Bone”. She is an Associate Professor at Midwestern University. Previously, she was with Cue Biotech and Caden Biosciences, companies she co-founded that focused on GPCRs and used a novel approach to identify allosteric compounds based on their ability to modulate GPCR/G protein coupling (US Patent Numbers 7,208,279 and 7,294,472). Prior to that Dr. Gilchrist worked as an Assistant Research Professor in the Department of Molecular Pharmacology & Biological Chemistry at Northwestern University where she developed a set of unique tools known as minigene vectors (US Patent Number 6,559,128). Minigene vectors allow one to dissect out the G protein that mediates a given physiological function and they have been widely adopted by researchers around the world. Preceding that Dr. Gilchrist was a postdoctoral fellow with Dr. Heidi Hamm. In this setting, she identified high affinity peptides that mimic the C-terminus of Ga, and were later used for crystallization of rhodopsin. Dr. Gilchrist’s work on GPCRs began with her graduate studies in which she studied signaling of chemokine receptors through tyrosine kinases and phosphatases. Dr. Gilchrist has a PhD in Immunology from the University of Connecticut Health Center and a MS in Biochemistry from the University of Connecticut.

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