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.
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 12th 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)
