SYMPOSIUM REPORT

The 23rd EFMC-ISMC – International Symposium in Medicinal Chemistry. Lisbon 7-11, Septmber 2014


The 23rd edition of the EFMC-ISMC has been held in Lisbon, 7-11 September 2014. The meeting, organized by the group of Medicinal Chemistry of the Portoguese Chemical Society , continued the successful tradition of these biennal meetings which are became, over the last five decades, the largest medicinal chemistry congresses in the world.
The meeting, chaired by Prof. Rui Moreira, has seen the participation of about 1,200 scientists coming from more than 55 countries. The impact that the meeting had in the community is exemplified by a few numbers. More than 100 speakers, distributed among plenary, invited and oral communications, over 600 posters, of extremely high quality covering all the major therapeutic areas, as well as technological and methodological developments and 55 exhibitors. Therefore, the meeting has been not only the occasion to get updated on the last breakthroughs in our discipline, but also the ideal place for productive and enjoyable networking.

Besides the regular scientific communications, the Meeting has also hosted several events, here summarized and fully described elsewhere in this Newsletter.
The EFMC-ISMC is the place where the community recognizes its champions, and the ideal place to present the 2014 EFMC Awards and EFMC Prizes. As already announced, the Nauta Award for Pharmacochemistry has been assigned to Dr. Paul Leeson (GSK, UK), the UCB-Erlich Award for Excellence in Medicinal Chemistry to Dr. Craig Crews (Yale University, USA) and the Prous Institute-Overton & Meyer Award for New Technologies in Drug Discovery to Dr. Gyorgy Ferenczy and Dr. Gyorgy Keseru (Hungarian Academy of Sciences, HU). The EFMC Prizes for a Young Medicinal Chemist in Industry has been awarded to Dr. Grazia Piizzi (Novartis Pharma, CH), while the EFMC Prizes for Young Medicinal Chemist in Academia to Dr. Christian A. Olsen (University of Copenhagen, DK).


Furthermore, the EFMC-ISMC has also hosted the award ceremony for the IUPAC Richter Prize, assigned to Dr. Helmut Buschmann (Pharma Consulting Aachen, DE), and the ceremony for the MedChemComm Prize, won by Dr. Christian Heins, of the Ecole Polytechnique Federale de Lausanne, Switzerland.

After the success in the previous 2010 edition, also this 23rd EFMC-ISMC meeting has hosted a EFMC session, again fully described in this issue, whose theme was ‘The Innovative Medicines Initiative and Opportunities for Medicinal Chemists’. With the EFMC Session, the Federation intends to take explicitly on its role of learned society and offers qualified views on scientific developments and opportunities to its members. Also on this line was the breakfast meeting of the EC-EFMC with representatives of SMEs across Europe. The breakfast meeting, organized by the SME and Biotech Landscape Working Group of EFMC (led by Thomas Fessard, Spirochem, CH) had the scope of align the potential offered by EFMC, in its role of scientific federation and learned society, with the rapidly changing needs (visibility, networking, training) of SMEs and Biotechs.

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The first EFMC Young Medicinal Chemist Symposium (YMCS) 2014 in Lisbon

With more than 125 scientist coming from 25 nations, the very first EFMC- Young Medicinal Chemist Symposium (YMCS 2014), held at the Faculty of Pharmacy of the University of Lisbon, September 12, 2014, has created a new inspiring stage for young researchers in medicinal chemistry.

The EFMC-YMCS 2014 was organised by an EFMC working group (which spun out of the 2012 Frankfurt EFMC brainstorm session) in connection with the XXIII EFMC International Symposium of Medicinal Chemistry (ISMC). The objectives of the YMCS are to create a network of young European investigators in Medicinal Chemistry, stimulate young European investigators in Medicinal Chemistry to share their scientific work with peers and inspiring leaders in the field and create competition and excellence in Medicinal Chemistry within Europe.

The Symposium was opened by EFMC President Uli Stilz (Novo Nordisk) and Symposium Chair Chris de Graaf (VU University Amsterdam) to start a full day conference filled with state-of-the-art medicinal chemistry: 2 keynote lectures, 8 oral communications by invited prize winners from national young medicinal chemist meetings in Europe, 4 selected oral communications, 20 oral flash poster presentations, and 80 poster presentations. The symposium sponsors Taros, Roche, RSC, AstraZeneca, and Pfizer together with important financial contributions of the EFMC, in kind contributions of LD Organisation (in particular Ly Differding and Brieuc Matagne), and organisational efforts of the University of Lisbon host (Rita Guedes, Maria Santos, Rui Moreira, and their tremendous team of post-docs and PhD students) were acknowledged for their crucial support for the first YMCS.

The inspiring opening Keynote Lecture of Kelly Chibale (University of Cape Town), leader in the field of malaria drug discovery research, set the tone for a successful symposium with interactive scientific discussions on a wide variety of medicinal chemistry research topics and disciplines. Professor Chibale gave an interesting overview of the medicinal chemistry optimization of phenotypic screening of hits from softfocus chemical libraries that target the malaria parasite Plasmodium falciparum, and showed how this work links to collaborative drug discovery projects together with the Medicines for Malaria Venture (MMV).

Eight oral communications of invited prize winners of national young medicinal chemist meetings in France, Greece, Israel, Italy, Poland, Spain, The Netherlands, and United Kingdom, and four additional communications selected from more then 60 abstracts showed the high level of the new generation of European medicinal chemistry researchers.

Duncan Hay (University of Oxford), winner of the young medicinal chemist meeting in The United Kingdom (Royal Society of Chemistry), presented the structure-based design and synthesis of a chemical probe to study the biological roles of CBP/P300 bromodomains.

Lucia Tamborini (University of Milan), winner of the young medicinal chemist meeting in Italy (Società Chimica Italiana) provided insights into the development and application of continuous flow chemistry as enabling discovery tool in medicinal chemistry.

Milon Mondal (University of Groningen), one of the four selected oral abstracts, showed how the combination of de novo structure-based design and dynamic combinatorial chemistry can lead to novel inhibitors of aspartic protease endothiapsin.

Christelle Dupouy (University of Montpelier), winner of the young medicinal chemist meeting in France (Société de Chimie Thérapeutique) presented her work on the synthesis and biological evaluation of siRNA prodrugs.

Nir Ben Chetrit (Weizmann Institute of Science), winner of the young medicinal chemist meeting in Isael (The Medicinal Chemistry Section of the Israel Chemical Society) presented high-throughput screening studies to identify novel molecules that target lipid signaling as a new therapeutic approach for breast cancer.

Karolina Pajak (Medical University of Lublin), winner of the young medicinal chemist meeting in Poland (Polish Society of Medicinal Chemistry), provided insights into molecular mechanisms of functional ligand selectivity towards the beta-2-adrenergic receptor.

Tiago Rodrigues (ETH Zürich), one of the four selected oral abstracts, showed how computational methods can be used for the de novo design of lead-like chemical entities for kinase and GPCR drug targets.

Saskia Nijmeijer (VU University Amsterdam), winner of the young medicinal chemist meeting in The Netherlands (Section Medicinal Chemistry, Royal Netherlands Chemical Society KNCV) presented her work on functional fragment screening at G Protein-Coupled Receptors for the identification of signalling-biased fragment-like GPCR ligands.

Thomas Evangelidis (University of Athens), winner of the young medicinal chemist meeting in Greece (Hellenic Society of Medicinal Chemistry) showed how the performance of consensus scoring approaches in protein-ligand docking can be optimized.

Ainhoa Mascaraque (CSIS Madrid), winner of the young medicinal chemist meeting in Spain (Sociedad Española de Química Terapéutica) presented her work glycodendropeptides as a potential vaccine against influenza A virus.

Laura Jennings (University of Oxford), one of the four selected oral abstracts, showed the optimization of in vivo probes for the BET bromodomains by structure-based design and synthesis.

Susana Dias Lucas (University of Lisbon), one of the four selected oral abstracts, presented a unified unified approach for rational discovery and optimization of neutrophil elastase inhibitors.


YMCS impressions: Concentrated auditorium audience (left), coffee break and poster session networking (middle), inspiring Keynote lecturer Alexander Mayweg (right).


Twenty flash presenters efficiently used their 1.5 minute sneak previews to invite the audience and jury to their posters during the lunch: Ewald Edink (VU University Amsterdam), Stephanie Gueret (Novartis), Rudi Oliveira (University of Lisbon), Eleni Kotsampasakou (University of Vienna), Sofia Alexandre Santos (University of Lisbon), Ana Ressureicao (University of Lisbon), Rafal Urniaz (Medical University of Lublin), Sara Cristina Covas da Silva (University of Lisbon), Ramatoulie Camara (University of Hertfordshire), Mariana Reis (University of Lisbon), Daria Goldmann (University of Vienna), Carlos Jorge Azevedo Costa Ribeiro (University of Lisbon), Andrea Unzue (University of Zurich), Agnese Chiara Pippione (University of Turin), Pedro Miguel Cal (University of Lisbon), Frans Smit (North West University), Nagore Isabel Marin Ramos (Complutense University of Madrid), Marzena Baran (Jagiellonian University Medical College Krakow), Davide Carta (University of Padova). The 79 posters created a buzzing scientific atmosphere in the hall of Faculty of Pharmacy and a challenging but rewarding task for the poster jury to select the best YMCS poster presentation.

Alexander Mayweg, Global Head of Medicinal Chemistry at Roche Pharma Research and Early Development (and winner of the EFMC Prize for a Young Medicinal Chemist in Industry 2011) gave an inspiring closing Keynote lecture on the future of medicinal chemistry. In his lecture Dr. Mayweg showed how the exploration of new chemical space and development of new drug discovery technologies can broaden the range of therapeutic modalities that can be designed and synthesized by medicinal chemists. Earlier that afternoon, Dr. Mayweg and Uli Stilz awarded EFMC Roche Studentship grants to Corentine Laurin (University of Glasgow) and Johannes Lehmann (TU München).

Not only the symposium presentations were attractive demonstrations state-of-the-art science , but also the following Q&A sessions, led by session chairs Chris de Graaf (VU University Amsterdam), Rita Guedes (University of Lisbon), and Fabrizio Giordanetto (Taros Chemicals), enabled fruitful scientific discussions between the YMCS participants. Active scientific networking was further stimulated by the Portuguese sweetened coffee breaks, delicious lunch poster session, and gastronomical drinks and networking at the roof terrace of the Faculty of Pharmacy of University of Lisbon.

During the closing Award ceremony the Taros YMCS Presentation Prize, Royal Society of Chemistry YMCS Poster Prize, and Roche YMCS Public's Choice Prize were awarded to the European Champions in Medicinal Chemistry:

Duncan Hay (University of Oxford) received the Taros YMCS Presentation Prize for his presentation on “A chemical probe for the CBP/P300 Bromodomains”. The prize was awarded by Fabrizio Giordanetto on behalf of the prize sponsor Taros Chemicals, consisting of a diploma, € 1.000 and an invitation for a short presentation at an EFMC symposium.

Ramatoulie Camara (University of Hertfordshire) received the RSC YMCS Poster Prize for her presentation on “Design, synthesis and evaluation of inhibitors of the S100P/RAGE interaction as potential anti-pancreatic cancer agents”. The prize was awarded by Richard Kelly on behalf of the prize sponsor The Royal Society of Chemistry, consisting of a diploma, € 500 and free registration for an EFMC symposium.

Laura Jennings (University of Oxford), received the Roche YMCS Public’s Choice Prize for her presentation on “Optimising in vivo proves for the BET Bromodomains”. The prize, based on the votes of YMCS participants, was awarded by Andrew Thomas on behalf of the prize sponsor Roche, consisting of a diploma and an iPad.


EFMC Young Medicinal Chemist Symposium Prize Ceremony: Left: Taros YMCS Presentation Prize awarded to Duncan Hay (University of Oxford) by Fabrizio Giordanetto (Taros Chemicals); Middle: Royal Society of Chemistry YMCS Poster Prize awarded to Ramatoulie Camara (University of Hertfordshire) by Richard Kelly (Royal Society of Chemistry); Right: Roche YMCS Public’s Choice Prize awarded to Laura Jennings (University of Oxford) by Andrew Thomas (Roche).


The outstanding scientific level and interactive scientific networking atmosphere of the first YMCS Lisbon meeting has set a promising standard for the EFMC-YMCS tradition, which will be continued in conjunction with EFMC meetings, the Frontiers in Medicinal Chemistry in Antwerp September 2015, and the XXIV EFMC-ISMC September 2016 in Manchester. The first details can be found on the regularly updated symposium website www.efmc-ymcs.org or via the EFMC website www.efmc.info.

Hope to see you at the next YMCS in Antwerp: The EFMC-YMCS offers a stage to presentations by young medicinal chemists, but is open to any scientist (of all ages) interested in medicinal chemistry!

By Chris de Graaf (VU University Amsterdam), Symposium Chairman
On behalf of the Organizing Committee of the first YMCS


Editor

Gabriele Costantino
Univ. of Parma, IT

Editorial Committee

Erden Banoglu
Gazi Univ., TR

Lucija Peterlin Masic
Univ. of Ljubljana, SLO

Leonardo Scapozza
Univ. of Geneve, CH

Wolfgang Sippl
Univ. Halle-Wittenberg, DE

Sarah Skerratt
Pfizer, Sandwich, UK

Executive Committee

Uli Stilz President
Koen Augustyns President Elect
Hein Coolen Treasurer
Gabriele Costantino Member
Phil Jones Member
Jordi Gracia Member
Pascal George Member

For more information please contact info@efmc.info

MedChemComm