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Modern Drug Discovery: From Biology and Structure to New Chemical Entity


After a general introduction of “classical” and “modern” drug discovery, various receptors, enzymes, ion-channels, carbohydrates and nucleotides are presented which provide clues as to how novel drugs can be found. It will be demonstrated that the multidisciplinary interaction between molecular biology, pharmacology, biophysics and chemistry is of utmost importance in the drug discovery process. The course is intended for MSc and PhD students.

Program 1. Introduction: classical, mainstream and modern Drug Discovery 2. G Protein-Coupled Receptors, a friendly Target for Drug Discovery 3. Proteases: from peptide substrate to Protease Inhibitor 4. Steroid (Nuclear) Receptors as Gene Switch 5. Kinase Inhibitors competing with ATP 6. Ion-channels: controlling the currents 7. From Heparin to improved Synthetic Drugs 8. Can we make drugs from Nucleotides? 9. Ligand-based design: how to make better caffeines
10. AIDS: the life cycle of a virus and how to beat it


prof. dr. A.P. IJzerman


  • 2nd years MSc students of BPS (Bio-Pharmaceutical Sciences), Biology, Life Science & Technology;and Chemistry.


Sufficient background knowledge of Chemistry and Biology




Hand outs


Written exam on April 27


15 students


The course will be given on the following dates and times in 2011:

Day — Venue Gorlaeus — subject — speaker

March 28, 1 pm – 5 pm — Havingazaal — Introduction/G protein-coupled receptors — Van Boeckel
March 29, 9 am – 1 pm — Havingazaal — Proteases/Nuclear receptors — Van Boeckel
April 4, 1 pm – 5 pm — Havingazaal — Kinase inhibitors/Ion channels — Van Boeckel
April 5, 9 am – 1 pm — Havingazaal — Heparin/Nucleotides — Van Boeckel
April 11, 11 am – 3 pm — Havingazaal — Ligand-based design/How to combat AIDS — IJzerman/Van Vlijmen
April 27, 2 pm – 5 pm — Havingazaal — Written examination

*Please note that the times of the lectures deviate from the standard times given in the study guide!


Application by e-mail to prof. dr. A. IJzerman, e-mail:


The course objective is to learn and appreciate the multidisciplinary aspects of drug discovery with an emphasis on the identification of a biologically active molecule with optimal properties.