Chimie pharmaceutique avancée et drug design [ WFARM2501 ]

organic chemistry and medicinal chemistry

The teacher(s) will discuss first the different techniques allowing the discovery of novel therapeutic targets (lipidomic ' proteomic ' deorphanization), second the methods allowing the identification of hits for a given molecular target (high-throughput screening ; computer assisted de novo drug design); finally the strategies allowing to optimize a hit ('hit to lead') will be discussed (structures-activity relationships ; docking; ')

At the end of the activity the student will be able to

• Interpret, based on what was discussed in class, the results presented in a scientific paper dealing with the development of a novel drug
• Suggest a strategy allowing to identify novel therapeutic targets
• Suggest a strategy allowing to identify novel lead compounds for a given target (enzyme, receptor, ')
• Suggest a strategy allowing to optimize the activity of a drug towards its target

a written exam and a presentation of a case-study based on a scientific paper

• Lipidomics applied to the discovery of novel targets
• Exploring the proteome looking for novel targets :  the enzymes ' the receptors
• Proteins as therapeutic target
  • Determination of their 3D structure
  • Role of protein's 3D models in drug design
• The interest of establishing structure-activity relationships in drug design