Cambridge Healthtech Institute’s
GPCR-Based Drug Discovery
11th Annual Part One: Screening and Structure-based Approaches
September 20-21, 2016

4th Annual Part Two: Signaling and Pharmacological Complexities
September 21-22, 2016

Part of the 14th Annual Discovery on Target Conference

G protein-coupled receptors (GPCRs) have steadily remained an important target class for drug discovery because of the myriad of biological processes they initiate as transducers of extracellular signals to inside the cell. However, they have always been and still remain a complex target class. Their multi-membrane spanning structure makes them difficult to isolate. Their ability to couple to various intracellular messengers (G proteins and other proteins) complicates interpretation and measurement of downstream signaling.

This two-part meeting enables discovery biologists and chemists to share progress, advances and new strategies in discovering, designing and optimizing GPCR-targeted compounds as well as hear about new work from academia that sheds light on the pharmacological complexities of this receptor class. Updates and challenges of GPCR-targeted compounds advancing in the drug development pipeline will also be a part of the agenda.

Part One:

The first meeting in the set, Screening and Structure-based Approaches, will include presentations and discussions related to discovering and designing compounds that act on GPCRs. Recent advances in biophysical approaches to studying GPCRs have enabled progress in both, structure-based design of ligands for GPCRs, and new screening methods, which though not as high throughput as traditional cell-based assays, allow receptors to be studied in more relevant cellular contexts.

Topics may include but are not limited to:

  • Implications of recent GPCR crystal structures to ligand design
  • New technologies in x-ray crystallography (Xel technology; liquid cubic phase)
  • Biophysical-based secondary screens for GPCRs (label free, SPR-based, back-scattering interferometry)
  • Time of flight mass cytometry (CytoF)
  • Nuclear Magnetic Resonance (NMR)-based fragment screens
  • NMR for conformational dynamics and ligand-independent receptor structure analysis
  • Screening in primary cell lines
  • Phenotypic screening

Part Two:

The second day-and-a-half conference, Signaling and Pharmacological Complexities, explores the unique aspects of GPCR signaling which makes GPCRs such challenging targets while offering multiple ways to exploit their functioning via pharmacological modulation. Insights on receptor trafficking, modifications, desensitization and selective/biased coupling and how that impacts design of GPCR-targeted compounds will be discussed. Case studies of biased ligands and allosteric modulators will also be featured.

Topics may include, but are not limited to:

  • Bitopic ligands for class A receptors
  • Biased signaling
  • Allosteric modulators
  • Receptor desensitization
  • Receptor internalization and trafficking
  • Endosomal signaling
  • G protein-independent signaling
  • GPCR regulation by kinases and RAMPs

If you are interested in speaking, please click here.

Click here to register for a special early-bird discounted rate.

The deadline for submission is March 4, 2016.

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—247-6252

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

Call for Speakers




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The exhibit hall was sold out in 2015, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2016, contact:

Jon Stroup
Sr. Business Development Manager