Advanced Methods for the Optimization of Candidate Selection

This course continues with the basics learned in Course 1 and extends the ideas to apply GPCR utilization in drug therapy. Specifically, the ideas discussed cover the complex pleiotropic behaviors of GPCRs and how these may be exploited for new drug discovery.

Receptor data shows how GPCR control of cellular function goes far beyond simple second messenger production (i.e., calcium, cAMP), and these new behaviors are being used to create novel GPCR therapies. The five-lecture series describes essential additional elements to GPCR discovery programs that extend the discovery process and increase therapeutic opportunity.

Registrants will learn:

• The powerful applications of new cellular assays to determine GPCR ligand

  behavior in different functional systems.

• Understanding real-time kinetics to predict activity and in vivo target coverage.

• New ligands and new GPCR behaviors that produce unique drug profiles (i.e.

  intracellular ligands and signaling, location bias, signaling bias).

Modules

• October 31st: The Eyes to See- The Importance of Pharmacologic Assays.

• November 7th: Drug Disposition in Physiological Tissues as a Therapeutic Variable.

• November 14th: The Application of GPCR Ligand Kinetics to Candidate Design.

• November 21st: Unconventional GPCR Ligands as Drugs.

• December 5th: Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit.

Registrations start on Monday, July 15th, 2024

• Classes will be live from Zoom on Thursdays from 10 am to 11:30 am EST.

• Sessions will include a 1-hour live lecture plus 30 minutes of Q&A.

• Participants who complete the course will get an online certification signed by the professor and the Dr.GPCR Team.

A splendid time is guaranteed for all.

What are the main objectives of the course?

• Allow registrants to appreciate the great versatility of GPCRs and how small molecules can affect their behavior for therapeutic benefit.

What will students gain from taking this course?

• Learn how to therapeutically exploit GPCRs (Physiology’s ‘Swiss Army Knife’) wide repertoire of ways to control cell function.

• Apply unique pharmacologic assays and unconventional ligands to unveil GPCR activities.

• Adjust ligand kinetics and tissue disposition for optimal therapeutic activity.

Are there any specific textbooks or readings students should be aware of?

• Pharmacology in Drug Discovery and Development (3rd ed.) T>P> Kenakin, Elsevier or ''A Pharmacology Primer' (6th ed.) T.P. Kenakin, Elsevier.