• Study level

    BAC +5

  • ECTS

    2 credits

  • Component

    Faculty of Science

Description

Receptors are of major interest in medicinal chemistry and represent over 40% of current therapeutic targets. This teaching unit provides an interdisciplinary approach to the basic concepts and notions of receptology required by 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 aim of this module is to deconvolve with students theoretical notions at the interface between chemistry and biology concerning the structure/activity study of receptor proteins, the study of their ligands, conformational dynamics, and pharmacological approaches relating to the targeting of these membrane and nuclear receptors.

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

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Necessary prerequisites

Cell Biology Basics

Structural biochemistry

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Knowledge control

Integral Continuous Control

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Syllabus

Course:

 

Notion 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
  • Application examples: retinoid receptors, retinoid-related receptors as therapeutic targets
  • Rational agonist/antagonist design - Structure-activity relationships

Membrane receptors and their ligands :

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

 

 

TD: Case studies. Work on scientific publications.

 

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Further information

Teaching 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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