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 HÂ
TD : 5 H
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.
Necessary pre-requisites
Basics of Cell Biology
Basics of Structural Biochemistry
Knowledge control
Integral Continuous Control
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.
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/