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 HÂ
TD: 5 H
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.
Necessary prerequisites
Cell Biology Basics
Structural biochemistry
Knowledge control
Integral Continuous Control
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.
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/