Techniques for Effective Lead Optimization of Candidate Molecules

GPCRs have been and arguably still are the most prolific and fertile therapeutic drug targets; this course describes the essential pharmacologic techniques and knowledge required to create a GPCR Target Program aimed at the discovery of new Drugs. The course will focus on the methods used to quantify GPCR ligand activity (agonists, antagonists, modulators) and the process of characterizing the mechanism of action of ligands to enable the prediction of activity in vivo systems. In general, registrants will receive a comprehensive understanding of the unique science of pharmacology and how it can describe drug action in system-independent ways.

Registrants will learn:

• Essentials of measuring pharmacologic activity of ligands (affinity, efficacy, co-operativity).

• Application of this knowledge to determine the mechanism of action of new

  GPCR ligands.

• The required elements of a comprehensive and effective GPCR Discovery.

Modules:

• October 3rd: GPCR Project Initiation and Design for Discovery of New Molecules.

• October 10th: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists.

• October 17th: Agonists and Efficacy: A New World of GPCR Efficacies / Biased

  Signaling.

• October 24th: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to quantify the allosteric effect.

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?

• To help registrants understand the value of Pharmacology in the drug discovery process.

What will students gain from taking this course?

• Students will gain an understanding of how pharmacology can greatly extend the ability to predict a candidate's therapeutic value in a range of different physiological conditions.

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

• Pharmacology in Drug Discovery and Development (3rd ed.) T.P. Kenakin, Elsevier 2024 or 'A Pharmacology Primer' (6th ed.) T.P. Kenakin, Elsevier, 2022.