The course objectives are to provide state-of-the-art knowledge of medicinal chemistry research achievements, in addition to knowledge of the methods used in drug design and discovery.

The introduction of new techniques in basic biological research has accelerated the disclosure of the complex mechanisms underlying cell function. Thus e.g. genetic technologies have revolutionised enzyme, receptor and ion channel research, and have made detailed mapping of subtypes of these biomolecules possible. On the basis of molecular cloning approaches, virtually all enzymes and receptors have been shown to represent families of structurally related isoforms and subtypes.

These aspects hold major therapeutic prospects and obvious challenges for medicinal chemists involved in design and synthesis of specific enzyme inhibitors and receptor ligands. Computational methods are playing a key role in structure-activity analyses, in the rapidly expanding area of structure-based drug design, and in the attempts to indirectly map out the topography of recognition sites.

A number of natural compounds and toxins have been used for the exploration of biological macromolecules. By means of advanced synthetic, stereochemical, and enzymatic techniques it has been possible to convert non-specific natural products into compounds with specific actions at key biomechanisms. There is a growing interest in combinatorial approaches in areas of drug research where naturally occurring lead compounds have not yet been identified, or where endogenous ligands are not appropriate leads for the design of novel therapeutic agents. Thus, combinatorial approaches are likely to be useful in the field of nonpeptide analogues of peptide hormones and transmitters.

The development of specific experimental tools may represent the initial steps in the conversion of bioactive compounds into therapeutic agents. Rational and systematic approaches along these lines are likely to lead to the development of novel classes of drugs against diseases which, so far, have escaped effective treatment.

During the course examples of important methods or techniques within the drug design and discovery process will be presented and discussed with special emphasis on the following topics:

• Receptors: Mechanisms and Structure-Function
• Enzymes: Mechanisms and Structure-Function
• Structure-Based Drug Design
• Bioisosteric Approaches in Drug Design
• Computational Approaches in Drug Design
• Peptidomimetic Design
• Natural Products as Leads in Drug Design
• Combinatorial Approaches in Lead Identification
• Rapid Throughput Screening in Drug Discovery
• Lead Optimisation

The 5-day course will comprise 15 to 20 lectures, group work (journal club) and participant presentations.

Study materials: Original publications.

Based on individual performance, assessed by active participation, presentation of selected articles during the course, and a short report (max. 2,500 words) or a poster on a selected subject after the course, a pass/fail is given by the course directors.

5 to 9 March 2012.

4 ECTS credit points (European Credit Transfer System).

100 working hours (40 for preparation, 30 for course, and 30 for report and evaluation).

Professor Flemming Steen Jørgensen and Professor Kristian Strømgaard, Department of Medicinal Chemistry at the Faculty of Pharmaceutical Sciences, University of Copenhagen.

Total course fee: DKK 9,400 (including lunch),

of which operating costs: DKK 1,300.

1 January 2012.

25 participants.

The course addresses PhD students with an MSc degree in biochemistry, biology, chemistry, pharmacology or pharmacy, or research scientists in the pharmaceutical industry.

The course will only be held in English.