G protein coupled receptors (GPCRs) are one of the most common targets of therapeutic pharmacologic interventions due to their role as transducers of signals outside the cell to the inside, resulting in a myriad of physiologically important events. Despite their fruitful history in the drug development industry, discovering or designing new therapeutic agents that modulate a GPCR in a specific way is still a challenge, and in fact is undergoing a renewal because of explosion of new knowledge about their structure and ways to more precisely control their signaling via which G protein or other receptor-associated protein they couple to (biased signaling).

Cambridge Healthtech Institute’s two-part GPCR-Based Drug Discovery meeting will cover advances that are not only illuminating GPCR structure, new ligand-discovery approaches and signaling complexities, but also providing ways to translate the increased knowledge into ‘precision’ therapeutics.

GPCR-Based Drug Discovery, Part 1 will focus on structural aspects of GPCRs and new assays, technologies and approaches for discovering and designing GPCR-targeted compounds. Part 2 will consist of case studies of lead compounds progressing in development and emerging (or recently tractable) pharmacologic complexities in the field. The back-to-back day-and-a-half meetings are part of CHI’s three day, multi-meeting track event, Discovery on Target.

Who should attend: Researchers, Scientists, Students, Post-docs, Professors, Group Leaders, Directors, Managers from Pharmaceutical companies, Biotechnology companies, Contract Research Organizations, Academic and Government Laboratories working in fields such as Biology, Discovery Biology, Medicinal Chemistry, Structural Biology, Computational Chemistry, New Lead Generation, High Throughput Screening, Assay Development, GPCR Screening, Signal Transduction, Cell Biology, Molecular Pharmacology, Drug Discovery, Neuroscience, CNS, Diabetes, Cardio-Metabolic Diseases, Inflammation, Pain, Translational Medicine

Topics will include, but are not limited to: 

Part 1: 

  • Structure-based design for GPCRs: merging theoretical/computational and experimental (crystal structure elucidation) knowledge
  • Chemical probes for various conformational states of GPCRs
  • GPCR dynamics and simulations and their drug discovery applications
  • PPI approaches for GPCRs
  • Fragment-based approaches for GPCRs
  • Macrocyclics against GPCRs
  • Label-free and biosensor-based assays
  • Live-cell assays, phenotypic screening, working with primary cells
  • Visualizing receptor complexes and/or trafficking

Part 2: 

  • Biased signaling
  • Allosteric modulators
  • CNS, inflammation, cardiovascular/diabetes and cancer - targeted compounds
  • Desensitization and internalization and implications for drug discovery
  • Pharmacologic complexities: receptor folding and trafficking
  • Arrestin-mediated and alternate signaling pathways
  • GPCR-associated proteins: GRKs, RAMPs

If you are interested in speaking, click here to submit a speaking proposal.

The deadline for submission is March 11, 2015. 

All proposals are subject to review by the Scientific Advisory Committee to ensure the highest quality of the conference program. Please note that due to limited speaking slots, preference is given to pharmaceutical and biotech companies, regulators and those from academia. Additionally, vendors/consultants who provide products and services to these biopharmaceutical companies are offered opportunities for podium presentation slots based on a variety of Corporate Sponsorships. 

For questions or suggestions about the meeting, please contact:
Anjani Shah, Ph.D.
Conference Director
Cambridge Healthtech Institute
T: (+1) 781-972-5400 headquarters; 914-723-0255 (direct)

For sponsorship and exhibit sales information including sponsored podium presentations, contact:
Jon Stroup
Sr. Business Development Manager
Cambridge Healthtech Institute
T: (+1) 781-972-5483

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2014 Discovery on Target Brochure  




Molecular Sensing




The exhibit hall was sold out in 2014, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2015, contact:

Jon Stroup
Sr. Business Development Manager

Westin Boston Waterfront


Westin Boston Waterfront
425 Summer Street
Boston, MA 02210