Principles of Pharmacology in Drug Discovery I

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:

• Lecture 1: GPCR Project Initiation and Design for Discovery of New Molecules.

• Lecture 2: Drug Affinity: Measurement of Antagonism (Binding and Function) /

  Classifying Antagonists.

• Lecture 3: Agonists and Efficacy: A New World of GPCR Efficacies / Biased

  Signaling.

• Lecture 4: 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.

• Every participant will also get the chance to have a 1:1 meeting with Dr. Kenakin during

  the four weeks, scheduled according to the professor's availability.

• 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.