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

Organised by Luc Brunsveld, Christian Ottman and Henk Timmerman

Organised by George Keseru, Andrew Leach and Henk Timmerman

Organised by Jesper Lau and Henk Timmerman

Organised by George Keseru and Henk Timmerman

Organised by Kevin Beaumont and Henk Timmerman

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