• Level of study

    BAC +5

  • ECTS

    2 credits

  • Component

    Faculty of Science

Description

Receptors are of major interest in medicinal chemistry and constitute more than 40% of current therapeutic targets. This course is an interdisciplinary approach to provide the basic concepts and fundamentals of receptology necessary for students pursuing their training in biomolecular chemistry at the chemistry-biology interface.

Hourly volumes* :

CM : 15 H 

TD : 5 H

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Objectives

The objective of this module is to deconvolve with the students the theoretical notions at the interface between chemistry and biology concerning the structure/activity study of receptor proteins, the study of their ligands, the conformational dynamics, and the pharmacological approaches related to the targeting of these membrane and nuclear receptors.

At the end of this course, the student will be able to analyze and access specialized scientific content (publications, conferences, etc.) in the field of medicinal chemistry on membrane and nuclear receptors.

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Necessary pre-requisites

Basics of Cell Biology

Basics of Structural Biochemistry

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Knowledge control

Integral Continuous Control

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Syllabus

Course:

 

Concept of cellular communication

Basic knowledge of receptor pharmacology

Nuclear receptors and their ligands:

  • The different families of ligands and nuclear receptors
  • Structure - Different binding domains
  • Mechanism of action: ligand-receptor interactions, receptor-DNA interaction, dimerization
  • Examples of applications: retinoid receptors, retinoid-related receptors as therapeutic targets
  • Rational agonist/antagonist design - Structure-activity relationships

Membrane receptors and their ligands:

  • Specialized study of structure/activity relationships of different classes of membrane receptors (GPCR educational support point)
    • channel receivers
    • G-protein coupled receptors
    • receptors with enzymatic activity
  • Concept of conformational selectivity of GPCRs & new model systems
  • Elements of physio/pathology in human health
  • Integration of signaling pathways

 

 

TD: Case study. Work on scientific publications.

 

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Additional information

Pedagogical team

 

Jean-Yves Winum

Jean-yves.winum@umontpellier.fr

 

Sophie Mary

Sophie.mary @ umontpellier.fr @

 

Administrative contact(s):

Secretariat Master Chemistry

https://master-chimie.edu.umontpellier.fr/

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