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SLAS2018 Short Courses

Pharmacology in Drug Discovery and Development: New Lives for Receptors as Drug Targets Through Allostery and Biased Signaling

This course discusses new ideas about efficacy (efficacy fingerprints, biased signaling) and allosteric receptor function to improve definition and quantification of GPCR drug activity, better target drug activity (i.e. pathway vs target validation) and predict therapeutic activity profiles. Specifically, methods to guide SAR for biased signaling and allosteric ligand activity will be featured.

Who Should Attend:

  • Biologists involved in drug discovery
  • Medicinal chemists
  • Students of pharmacology
  • Academic pharmacologists

Those interested in the following tracks:

How You Will Benefit From This Course:

  • Gain new insights into state of the art ideas on efficacy and allostery
  • Learn new tools to quantify GPCR drug activity and guide med chem
  • Learn how parameters from these methods can predict activity in all systems
  • Define new vistas around old targets-better define chemical targets for receptor

Course Topics:

  • Ligand affinity
  • functional and binding studies
  • Ligand efficacy
  • multiple efficacies (efficacy fingerprints)
  • biased signaling- biased agonists/antagonists
  • allosteric theory and practice- how allostery can be exploited therapeutically
  • allosteric screening
  • understanding and use of the current functional allosteric model
  • quantifying allosteric ligand constants and predicting behavior in different systems
  • application of pharmacological concepts to drug discovery
  • studying PAMs / NAMs- induced biased through allosteric modulation


Terry Kenakin

Terry Kenakin
UNC School of Medicine, Chapel Hill, NC

After obtaining a BSc in chemistry and Ph.D. in Pharmacology at the University of Alberta, Dr. Kenakin worked for 3 years at University College London UK with Prof. Sir James Black. From there he spent 32 years in industry (7 Burroughs-Wellcome ,25 GlaxoSmithKline). He currently is Professor at the University of North Carolina School of Medicine. His interests have always been in quantitative pharmacodynamics and the discovery of new drugs and he has worked on projects for AIDs, heart failure and metabolic diseases. He is editor and chief of Journal of Receptors and Signal Transduction, and co-Editor in Chief of Current Opinion in Pharmacology. He has written 10 books on pharmacology.

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