This intensive course is intended for scientists working in the field, and the presentations will be given by senior scientists from industry and academia. The number of participants is limited to 35, to allow in depth discussion. Should the number of applications exceed the maximum, preference will be given to applicants from EFMC adhering countries and employees of EFMC corporate members. Upon special request to the organisers, only based on financial conditions and supported by an argued recommendation of the head of the department of the applicant, up to 3 applicants from academia may be admitted at a reduced fee.

Confirmed Speakers:

• Dr Xavier BARRIL (GAIN THERAPEUTICS, Mataro)
• Dr Ben DAVIS (VERNALIS PLC, Cambridge, United Kingdom)
• Dr Paul ENGLAND (IOTA PHARMACEUTICALS LTD., Cambridge, United Kingdom)
• Dr Mike HANN (GLAXOSMITHKLINE, Stevenage, United Kingdom)
• Prof. Rod HUBBARD (UNIVERSITY OF YORK & VERNALIS, Cambridge, United Kingdom)
• Prof. Gyorgy KESERU (RESEARCH CENTRE FOR NATURAL SCIENCES, HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary)

Organised by: Iwan DE ESCH (VU University Amsterdam, The Netherlands) and Henk TIMMERMAN (VU University Amsterdam, The Netherlands)

Organised by Bart De Spiegeleer and Henk Timmerman

In this EFMC short course, experts in the field will provide a
firm conceptual framework for the study of target binding kinetics. Tutorials and real life examples will assist the participants in the short course to grasp not only a basic understanding but also to bring home inspiring case studies from both an academic and industrial perspective. The number of participants will be limited to 35 to assure interactive and in-depth discussions.

Organised by Ad Ijzerman, Laura Heitman and Henk Timmerman

Confirmed Speakers

• Prof. Helena DANIELSON (UPPSALA UNIVERSITY, Uppsala, Sweden)

• Dr Liesbeth DE LANGE (UNIVERSITY OF LEIDEN, Leiden, The Netherlands)

• Dr Wilbert DE WITTE (UNIVERSITY OF LEIDEN, Leiden, The Netherlands)

• Dr Matthias FRECH (MERCK, Darmstadt, Germany)

• Dr Laura HEITMAN (UNIVERSITY OF LEIDEN, Leiden, The Netherlands)

• Prof. Ad P. IJZERMAN (UNIVERSITY OF LEIDEN, Leiden, The Netherlands)

• Prof. Georges VAUQUELIN (VUB, Brussel, Belgium)

In 2009, EFMC launched a series of short courses aimed to favour cultural and scientific growth of the medicinal chemistry community and organised with affordable fees for participation.

This intensive course is intended for scientists working in the field, and the presentations will be given by senior scientists from industry and academia. The number of participants will be limited to 35, to favour in depth discussion. Should the number of applications exceed the maximum, preference will be given to applicants from EFMC adhering countries and employees of EFMC corporate members. Upon special request to the organisers, only based on financial conditions and supported by an argued recommendation of the head of the department of the applicant, a limited number of applicants from academia (maximum 3) may be admitted at a reduced fee.

Speakers

• The PDE Family and Inhibitors
  Dr Andrew BELL (Iperial College London, United Kingdom)
• Epigenetic Target Families in Medicinal Chemistry
  Prof. Paul BRENNAN (University of Oxford, United Kingdom)
• Brodomain Inhibitors - from Phenotypic Screens to Fragments
  Dr Chun-wa CHUNG (Glaxosmithkline R&D, United Kingdom)
• Fragment-Based Lead Generation
  Prof. Iwan DE ESCH (VU University Amsterdam, The Netherlands)
• Glycomimetics - an Underexplored Compound Class for Medicinal Chemistry
  Prof. Dr Beat ERNST (University of Basel, Switzerland)
• Proteasome Inhibitors
  Prof. Michael GROLL (Technische Universität Munchen, Germany)
• Basic Principles of Enzymology
  Dr Laurie LEBRUN (Celgene, United States)
• Kinases and Inhibitors
  Dr Gerhard MÜLLER (Mercachem, The Netherlands)
• The Protease Target Family
  Dr Holger SELLNER (Novartis, Switzerland)
• Parallel Hands on Tutorials - Cases Study I
  Dr Leon VAN BERKOM (Mercachem, The Netherlands)
  Dr Toine VAN DEN BERGH (Mercachem, The Netherlands)
• Parallel Hands on Tutorials - Cases Study II
  Dr Stijn GREMMEN (Mercachem, The Netherlands)
  Dr Harald ALBERS (Mercachem, The Netherlands)

Course outline

Enzymes encompass a vast number of distinct target families relevant for contemporary medicinal chemists‘ endeavor to the discovery of efficient and safe drugs. A recent analysis of about 1.000 drugs approved from 1982 – 2010 uncovered around 450 effect-mediating drug targets of which only 150 cluster into enzyme families. However, the ratio of enzyme inhibitors among all approved drugs has increased over the last 10 years; of all ‘true NCEs’ that reached the market from 2005 onwards, more than 50% exert their therapeutic effect by modulation of human and pathogenic enzymes. Many of the approved inhibitors modulate enzymes that cluster into densely populated target families that will be scrutinized in the 12^th EFMC Short Course on Medicinal Chemistry. Hence, the focus of this course will be centered on all aspects of enzyme inhibitor discovery addressing the widely unexploited potential of both, the established enzyme classes such as proteases and kinases, as well as the modern emerging enzyme families from e.g. the epigenetics area. A collection of renowned international experts in the field will highlight various methodological, technological, and enzymological aspects of medicinal chemistry aimed at the discovery of inhibitors against proteases, kinases, phosphodiesterases, as well as epigenetic targets, respectively. Lectures and discussions will be complemented by interactive hands-on sessions on selected case studies in which the participants will be challenged to pursue hit-to-lead and subsequent lead optimization campaigns, supervised by experienced medicinal chemists.

Course Organisers
Gerhard Müller (Mercachem, The Netherlands)
Anita Wegert (Mercachem, The Netherlands)

Local Organiser
Henk TIMMERMAN (VU University Amsterdam, The Netherlands)

Organised by Jesper Lau and Henk Timmerman

COURSE OUTLINE

Protein-Protein Interactions (PPIs) lie at the heart of almost every physiological process and every disease. With a recently estimated number of 300,000 in humans, the possibilities for therapeutic intervention are significantly larger compared to ‘classical’ drug targets. While this potential is up to now largely untapped, some successful examples have shown that PPIs can be modulated by drug-like small molecules, natural products and peptides.

Specific features of PPIs as drug targets - in comparison to conventionally addressing e.g. enzymes - will be discussed, followed by a broad overview of the field, techniques to discover modulators of PPIs,  and - in more detail - a number of case studies on successful PPI intervention will be presented. Speakers include a selection of top-scientists active in the field of PPI, both from industry and academia.

Organised by Luc Brunsveld, Christian Ottman and Henk Timmerman

Course outline:

The interactions between molecules govern all of the properties that determine whether a compound will be an effective drug or not. This course will present the fundamental considerations determining the thermodynamic and kinetic properties of interactions between molecules.

The first part of the course will begin with an introduction to the types of interactions that are usually considered important for drug-like compounds, including some of the less commonly considered weaker interaction types. The decomposition of these interactions into their thermodynamic components will follow. A description of the experimental and computational methods available to study intermolecular interactions and their strengths and weaknesses will follow.

The second part of the course will focus on applied aspects. This will take two forms: detailed presentations considering most key molecular properties and some hands on tutorial exercises. Both will be structured around real life case studies taken from the literature and the presenters’ own experience. The areas of application will be directly relevant to the properties of a molecule typically modulated by medicinal chemists. Interactions in the solid state and their similarities and differences with interactions in solution determine the solubility of a molecule. The interactions with a range of solvent types determine many partitioning effects. The interactions between small molecules and proteins and between different protein molecules determine the affinity of compounds for their target and antitargets as well as their ability to compete with other compounds present in biological environments. The considerations governing the kinetics of association and dissociation have come into focus in recent years; they provide confounding influences that can lead to surprising in vivo effects and more importantly to better therapeutic index.

The various presentations and tutorials will be taken by experts in the field who will present a broad historical perspective as well as cutting edge research from both academia and industrial settings. The course will take an informal approach and ought to prompt plenty of discussion among participants.

Organised by George Keseru, Andrew Leach and Henk Timmerman

Course outline:

The development of future biopharmaceuticals will depend on research at the interfaces between several scientific disciplines including organic chemistry, physical chemistry, biophysics, protein chemistry and molecular biology. The interplay between these fields will have a key role for improving our molecular understanding of peptides and proteins and thus for developing future drug candidates. This course will focus on strategies on how to design and engineer biopharmaceuticals and will provide participants with insight to this important field of bioscience, which are applicable in academic and pharmaceutical contexts. The course will cover several fundamental aspects of peptide chemistry methodologies, selective modifications of proteins, ligation chemistries and regioselective coupling reactions. The biophysical characterization of peptide and proteins will be integrated in the lectures. The course will also cover various methods of semi-synthetic and synthetic modifications of proteins with focus on the application to drug discovery. Finally the course will give an insight to therapeutic antibodies including screening, optimization an engineering aspects.

Thus, various issues of development of biopharmaceuticals as well as discussions of different strategies to improve peptide and protein properties to biopharmaceuticals will be the primary focus of the course.

Organised by Jesper Lau and Henk Timmerman

Course outline:

The interactions between molecules govern all of the properties that determine whether a compound will be an effective drug or not. This course will present the fundamental considerations determining the thermodynamic and kinetic properties of interactions between molecules.

The first part of the course will begin with an introduction to the types of interactions that are usually considered important for drug-like compounds, including some of the less commonly considered weaker interaction types. The decomposition of these interactions into their thermodynamic components will follow. A description of the experimental and computational methods available to study intermolecular interactions and their strengths and weaknesses will follow.

The second part of the course will focus on applied aspects. This will take two forms: detailed presentations considering most key molecular properties and some hands on tutorial exercises. Both will be structured around real life case studies taken from the literature and the presenters’ own experience. The areas of application will be directly relevant to the properties of a molecule typically modulated by medicinal chemists. Interactions in the solid state and their similarities and differences with interactions in solution determine the solubility of a molecule. The interactions with a range of solvent types determine many partitioning effects. The interactions between small molecules and proteins and between different protein molecules determine the affinity of compounds for their target and antitargets as well as their ability to compete with other compounds present in biological environments. The considerations governing the kinetics of association and dissociation have come into focus in recent years; they provide confounding influences that can lead to surprising in vivo effects and more importantly to better therapeutic index.

The various presentations and tutorials will be taken by experts in the field who will present a broad historical perspective as well as cutting edge research from both academia and industrial settings. The course will take an informal approach and ought to prompt plenty of discussion among participants.

Organised by George Keseru and Henk Timmerman

Course Outline

In modern drug discovery, it is important that the Medicinal Chemist understands how to balance potency and ADME properties in order to provide high quality compounds for progression to clinical studies. This short course will be a mixture of talks and worked exercises designed to further the understanding of DMPK. The course will include: Outlines of the key DMPK in vitro assays: physicochemistry for ADME; Oral drug absorption; Fundamentals of drug distribution; drug metabolizing enzymes; drug transport proteins; basic PK principles and human PK prediction; PKPD relationships.

To read the full description of the course, please follow this link.

Organised by Kevin Beaumont and Henk Timmerman

Course Outline

In recent years drug discovery shifted from a traditional target-based approach towards phenotype and patient-based approaches. This course will discuss how systems biology contributes to a better understanding of human physiology and diseases (session I) and of the cellular biological systems behind (session II). This understanding is key for the discovery of novel drugs in order to address the right targets and biological mechanism.  In addition experimental (and computational) approaches to target identification will be a topic (session III), which are key for de-convolution of the molecular target(s) of known drugs or of hits from phenotypic screens (e.g. chemical proteomics). The last session will then describe how ‘omics data can be used to identify signatures of diseases (e.g. gene expression signature) and how these signatures can foster the understanding of a disease-phenotype. These disease signatures can be mapped to signatures of drugs for modern drug discovery.  Each of the four sessions of the course will be introduced by an overview, followed by several case studies and some hands-on exercises using various modelling tools.

To read the full description of the course, please follow this link.

Organised by Thomas Klabunde, Brian Harms and Henk Timmerman

Organised by Alan Stobie and Henk Timmerman

Organised by Mike Trevethick and Henk Timmerman

Organised by Alan Stobie and Henk Timmerman

Organised by Han van den Waterbeemd and Henk Timmerman