Content

• Molecular basis of disease and mode of action (MOA) for various drug classes
• Overview of properties, structure and function of biological macromolecules
• Drug target identification: molecular physiology, genomics, proteomics and bioinformatics
• Drug target validation and animal models
• Techniques of high-throughput screening in vitro, in cell culture and in vivo
• Fragment-based approaches
• In silico approaches including molecular modelling, drug-ability evaluation, qualitative structure-activity relationship (QSAR) and structure-based design
• Optimization of the lead compounds

+ Link with Drug Discovery content in the OPO ‘Levenscyclus van een geneesmiddel’ (‘Drug life cycle’)

Course material

• Lecture handouts
• Review articles and textbooks (e.g. Textbook of Drug Design and Discovery, Stromgaard K. et al, 5th Edition)

Language of instruction: more information

English is by far the common language used in pharmaceutical industry, often even on a local scale, but certainly on a global scale. Translation of drug development terminology to Dutch can be challenging and may prevent thorough understanding and swift discussions.

Format: more information

Interactive lectures

Content

Through working on this practical assignment, students will get hands-on experience with:

• Searching online resources (Protein Data Bank, DrugBank, Pubmed,...) for a particular drug/target complex
• Using interactive molecular graphics in pymol to view and analyze the drug-target interactions

Popular software pymol will be used.  

Course material

• The students should install pymol and optionally other free academic software on their laptops
• Detailed assignement and instructions on the use of software will be provided

Language of instruction: more information

English is by far the common language used in pharmaceutical industry, often even on a local scale, but certainly on a global scale. Translation of drug development terminology to Dutch can be challenging and may prevent thorough understanding and swift discussions.

Format: more information

Hands-on session

Content

The task is to prepare a short (10’) presentation outlining the discovery of a particular drug, its mechanism of action, challenges and outlook.

Course material

• Lecture handouts
• Review articles and textbooks
• Software free for academic use (to be used on students’ laptops)
• Online databases (Pubmed, Protein Data Bank,...)

Language of instruction: more information

English is by far the common language used in pharmaceutical industry, often even on a local scale, but certainly on a global scale. Translation of drug development terminology to Dutch can be challenging and may prevent thorough understanding and swift discussions.

Format: more information

The students are divided in small groups. Each group focuses on one of the existing drugs (chosen independently or from the provided list). The task is to prepare a short (10’) presentation outlining the discovery of a particular drug, its mechanism of action, challenges and outlook.

• In the course of preparation, the students consult the available literature and database resources.
• They must employ the molecular graphics and analysis software (that they have been exposed through the previous OLA) towards preparing suitable figures and/or use the molecular graphics interactively during their presentations. A presentation only using figures from publications will not be accepted!

Each presentation is followed by a short discussion.