Cambridge Healthtech Institute’s 15th Annual

GPCR-Based Drug Discovery

Targeting G Protein-Coupled Receptors for New Therapeutic Options

September 17-18, 2020


G protein-coupled receptors (GPCRs) have been a medically relevant drug target for decades because of the central roles they play in a variety of physiological processes. At least 25% of the drugs on the market achieve their effect via GPCRs. The receptors are a challenging target class to work with, however, because they are embedded in the membrane and have complex signaling properties (a single type of GPCR can couple to and activate or inhibit a variety of G proteins). Recent advances in biophysical screening approaches though are facilitating GPCR-targeted drug discovery. Cryo-electron microscopy and X-ray crystallography improvements have also aided drug discovery against GPCRs. Join us at the 15th Annual GPCR-Based Drug Discovery conference, part of Discovery on Target, to hear about examples of early drug discovery work with newer approaches and GPCR-targeted candidates progressing in the pipeline.

Preliminary Agenda

GPCRs in Disease

Keynote Presentation

Terry Kenakin, PhD, Professor, Department of Pharmacology, University of North Carolina School of Medicine

Structural or Biophysical Tools for GPCR-Targeted Drug Discovery

Beyond Soluble Targets: Applying CETSA to Multipass Transmembrane Proteins

Aarti Kawatkar, MS, Senior Scientist, Chemical Biology and Proteomics, AstraZeneca

NMR and Weak Affinity Chromatography for Small Molecule and Fragment Screening against GPCRs 

Isabelle Krimm, PhD, Principal Investigator, CNRS, University of Lyon

Talk Title to be Announced

Huixian Wu, PhD, Structural Biology Lab Head, Discovery Sciences, Medicine Design, Pfizer Worldwide Research & Development


GPCR Signaling Complexities

GPCR Heteromers as Targets for Drug Development

Ajay Yekkirala, PhD, Co-Founder & Chief Scientific Officer, Blue Therapeutics

Subcellular Localization of GPCRs and Drug Discovery Implications

Aylin Hanyaloglu, PhD, Reader, Cell Biology, Imperial College London

Dissecting Molecular Recognition Mechanisms of GPCR Phospho-Barcodes by Arrestin

Jinpeng Sun, PhD Professor, Physiology Department, Peking University School of Medicine

Targeting and Exploring the Sodium Binding Pocket of the μ-Opioid Receptor

Abdelfattah Faouzi, PhD, Postdoctoral Fellow, Department of Clinical Pharmacology, Laboratory of Susruta Majumdar, St. Louis College of Pharmacy and Washington University School of Medicine

For more details on the conference, please contact:

Anjani Shah, PhD

Senior Conference Director

Cambridge Healthtech Institute

Phone: (+1) 781-247-6252



For partnering and sponsorship information, please contact:

Rod Eymael

Manager, Business Development

Cambridge Healthtech Institute

Phone: (+1) 781-247-6286