EFMC VIRTUAL WEEK | SHORT REPORT
Now that the EFMC Virtual Week is over, we would like to thank all the participants who contributed into making this e-adventure a great success.
With a combined attendance of more than 1300 participants to the virtual EFMC-ISMC, virtual EFMC-YMCS and virtual Poster session, we showed that the spirit of endeavour and community remains defiantly undimmed by global events
We discovered first time disclosures, listened to outstanding talks, heard promising scientists presenting their research and could browse through more than 200 posters – all this from the safety of our homes.
However, we look forward to being able to meet again in person, hopefully during the future EFMC Meetings scheduled in 2021.
For now, the EFMC will continue to offer virtual events such as the EFMC-YSN MedChemBioOnline or support outside initiative with its programme of EFMC Sponsored or Certified event.
EUROMEDCHEM TALENTS 2021 SPECIAL COLLECTION ANNOUNCED
ChemMedChem, EFMC, and its Young Scientists Network (YSN) present the EuroMedChemTalents Special Collection. This collaboration is the first of its kind for the journal and the EFMC, and is also our first collection dedicated to Early-Career Researchers.
This collaborative project coincides with the EFMC‘s 50th Anniversary in 2020 and ChemMedChem‘s 15th Anniversary in 2021, and celebrates our close cooperation through the years. Taking the lead in this project are our Guest Editors Yves Auberson (current EFMC President) and Filipa Ramilo Gomes (Instituto Superior Técnico, University of Lisbon).
Both ChemMedChem and the EFMC are aware of the great contributions of younger researchers in drug discovery today and how important it is to support this generation of research leaders. This Special Collection aims to showcase the latest work from these young scientists in Europe. Contributing Authors featured here are nominated by the EFMC or the ChemMedChem editors and board members. These authors are considered figures that will shape the future of research at the interface of chemistry, biology, and medicine. To be eligible, authors must be based in an institute within Europe at the time of nomination and should have received their PhDs only within the last 12 years. If you wish to nominate a specific early-career researcher based in Europe (including yourself), please get in touch with the Editorial Office by e-mail, so that the screening committee can evaluate your nomination.
All articles will be published in regular issues of ChemMedChem (or possibly ChemBioChem for chembio-heavy work), but all collected under the EuroMedChem Talents page for easy access. Articles in the collection will also be free to read for at least a year, beginning 2021.
Finally, in the collection, you will also find interesting EFMC Anniversary Articles featuring its history, projects, and future plans.
Main nominations from the EFMC & ChemMedChem, invitations will go out in October.
Nominations are also welcome, send to firstname.lastname@example.org by September 30.
1ST MERCACHEMSYNCOM DIGITAL CONFERENCE:
EXPLORING NEW MODALITY SPACE BY PRECISION CHEMISTRY (OCTOBER 7-8, 2020)
We are increasingly breaching the barriers of what used to be considered undruggable target space, by adopting novel approaches to drug discovery, often broadly defined as ‘new modalities’. This free-to-attend symposium will showcase recent advances in new modality space, including targeted delivery, conjugates, and molecular glues, with a particular focus on the underlying, very often challenging, chemistry required to create these unconventional systems.
When looking back at how drugs were discovered in the mid-to-late nineties, it becomes apparent that the role of chemists in the endeavor of drug discovery has dramatically changed. Where they used to synthesize small organic molecules, with the aim of optimizing the biological activity, nowadays, chemists are also expected to use their organic chemistry skills to design a wide diversity of molecular constructs, often based on very challenging chemistries, to enable biologists in the unravelling and understanding of extremely complex biological systems. Thus, from being an expert in pure medicinal chemistry, the chemist’s role has now evolved to that of being an expert in chemical biology.
Since the start of this chemical biology era, MercachemSyncom has paid close attention to this evolution, by deploying its cutting-edge chemistry expertise to construct these so-called new modalities. In this first edition of our e-conference on chemical biology, namely, 'Exploring new modality space by precision chemistry', we bring together an outstanding list of international speakers to present and discuss new evolutions in the new modality space. Free registration will allow you to learn more about PROTAC design, interfering with RNA, delivery technologies, and peptide-based new modalities.
We look forward to welcoming you all on October 7-8 for inspiring discussions.
The “literature spotlight” section of the newsletter will bring you a summary of the recently published research in a concise and readable way. Multiple thematics from different journals will be highlighted thanks to the valuable contribution of Dr Clemens Zwergel (University of Rome, IT) from the communication team.
This sixth contribution will focus on the recently published article on an innovative way to synthesize histone deacetylase inhibitors (HDACi) by Sinatra et al. in Angewandte Chemie.
Today research is moving from a single and specific interaction with one target of interest toward the development of “molecular network active compounds” or a polypharmacology approach with superior therapeutic effects. Multi-target drugs often possess, almost counter-intuitively, fewer adverse effects as well as a lower risk of developing drug resistance by attacking, for example, cancer via different biological pathways.
This approach is adopted by Sinatra et al. in their an innovative paper on the design and synthetis of histone deacetylase inhibitors with other classical anticancer agents. Based on the well-known the synergistic activity of HDACi with alkylating agents, the authors chose the DNA-alkylating drugs temozolomide, mitozolomide, and chlorambucil as suitable scaffolds for a hybridization approach with potent class I / HDAC6 scaffolds.
The alkylating drugs are chemically quite challenging to work on due to stability or reactivity issues. The authors developed and used an innovative parallel synthesis approach, applying an efficient solid-phase supported protocol. They immobilized hydroxamic acids on resins (HAIRs), turning them into stable and versatile building blocks for the preparation of functionalized hybrid compounds.
The link between panobinostat and chlorambucil showed the highest antiproliferative activity via the activation of caspase 3/7, better than both compounds alone or in combination.
To further valorize the HAIR technology, the building blocks were applied to thesynthesis of a proof-of-concept HDAC degrader.
The innovative approach and the promising data will hopefully accelerate the development of polypharmacology modulators.
Sinatra, L., Bandolik, J..J., Roatsch, M., Sönnichsen, M., Schoeder, C..T., Hamacher, A., Schoeler, A., Borkhardt, A., Meiler, J., Bhatia, S., Kassack, M..U. and Hansen, F.K. (2020), Hydroxamic Acids Immobilized on Resins (HAIRs): A Toolbox for the Synthesis of Dual''.chr('8208').''Targeting HDAC Inhibitors and HDAC Degraders (PROTACs). Angew. Chem. Int. Ed. Accepted Author Manuscript. doi:10.1002/anie.202006725
EFMC-YMCS 2020 | PRESENTATION PRIZE WINNER ANNOUNCED
This year again, the competition was fierce and it was a real challenge for the jury to decide whom of the 12 promising scientists would be awarded the title of European Champion at the end of the 7th EFMC Young Medicinal Chemists' Symposium, held virtually on September 10-11, 2020.
We are pleased to announce that the 2020 winner is Ms Jessica Reynolds (University of Oxford, United Kingdom) for her presentation entitled: "Design and Synthesis of Chemical Tools to Probe the Function of Trim33". She will be invited to deliver an oral communication at the EFMC-ISMC 2021 in Basel (August 29-September 2, 2021).
Congratulations to her!
EFMC VIRTUAL POSTER SESSION | BEST POSTER PRIZES
More than 200 posters were submitted at the occasion of the EFMC-ISMC & EFMC-YMCS Virtual Poster Session. The jury took its time to screen them all and to exchange with the authors via the chatting tool activated on September 9, 2020.
The below 9 winners were awarded an "EFMC Best Poster Prizes", sponsored this year by ChemMedChem/ChemBioChem.
- P012 - Charlotte Sornay (University of Strasbourg, FR)
- P082 - Verena Kunig (TU Dortmund, DE)
- P141 - Sofia Parrasia (University of Padova, IT)
- P008 - Anna Duran-Corbera (Institute for Advanced Chemistry of Catalonia, ES)
Drug Discovery Projects
- P003 - Daniel Baillache (University of Edinburgh, UK)
- P015 - Cosmin Butnarasu (Università degli Studi di Torino, IT)
- P089 - Silvia Bonomo (Charles River Discover, UK)
- P168 - Greta Bagnolini (University of Bologna, IT)
- P206 - Daniel Kohnhäuser (Helmholtz center for Infection Research, DE)
Congratulations to all of them!
GET TO KNOW AD IJZERMAN, LEIDEN UNIVERSITY, THE NETHERLANDS
In this edition, our #Iamamedicinalchemist is the winner of the 2020 Nauta Pharmacochemistry Award for Medicinal Chemistry and Chemical Biology, Prof. Ad Ijzerman from Leiden University, The Netherlands.
How did you get interested in Medicinal Chemistry?
I studied pharmacy as the consequence of my equal interest in both chemistry and biology. In my fifth year or so (one studied endlessly back then) I did a research internship in pharmaceutical chemistry, and got fascinated by small molecule – protein interactions while studying stopped-flow kinetics of the binding of drugs to human serum albumin.
Where and when did you obtain your PhD diploma?
That was in 1985 under the supervision of Henk Timmerman, Professor of Medicinal Chemistry at the Vrije Universiteit in Amsterdam.
We wanted to sort out the molecular characteristics defining an agonist’s intrinsic activity at the beta-adrenergic receptors. No cell lines in those days for the radioligand binding studies we did, so I remember vividly visiting the slaughterhouse for a pound or two of fresh calf meat every now and then, an endless source for our membrane preparations.
Where did you have your postdoc position?
If you don’t tell anyone else: I never did a postdoc.
What are your current research interests?
G-protein coupled receptors (GPCRs) have always been my pet drug targets. When I started as a PhD student, I was overwhelmed by the available literature on GPCRs and wondered what on earth I could contribute. Some decades later – it took a while - I have come to the conclusion there is still so much to discover in this research field.
What do you like most in your job?
Being a professor is probably the most fortunate position one can have. First and foremost, the interaction with colleagues, coworkers, and students is what I cherish, and I must say the corona crisis really has a negative impact on this. Secondly, never a dull moment, every day has surprises: new findings, puzzling data, and an occasional email with the great news of being selected as the 2020 EFMC Nauta Awardee
What kind of tasks your job includes?
Well, that’s a good mix of teaching and research, and the associated management. I am fond of teaching – got a few awards for my academic lecture series and together with Henk Timmerman I shaped and organized the LACDR School on Medicinal Chemistry, a 4-days workshop/course for young medicinal chemists, than ran for 20 years. Not surprisingly I love research, discussing results and science in general with anyone who’s around, and won’t stop before the G, the P, the C, and the R are mentioned in the right order. I won’t say too much on management.
What do you consider your biggest achievement in your scientific career?
When I started in Leiden back in 1985 there was no medicinal chemistry there. Now, it’s everywhere – even the School of Medicine has fume hoods now. I think I played a role in that development.
Which scientist do you admire the most and why?
Next to medicinal chemistry I am really interested in history and art, so allow me to step back a few centuries and honor Leonardo da Vinci. I just cannot fathom how all that brilliance converged in one person.
Which paper of yours you are the proudest of and why?
Frankly, my best and most influential papers were (almost) all built on collaboration. The structure elucidation of the adenosine A2A receptor, as early as 2008, is my favorite. It was published in Science that year, and could only occur thanks to our collaboration with Ray Stevens and his team in San Diego.
Which field of medicinal chemistry do you consider the most promising in the future?
It’s always hard to predict anything, especially about the future (thanks, Niels Bohr). Although not easy territory - languages can be very different, it scours and creaks from time to time - I’ve always learned most from where disciplines meet. So, for now I think the laws of biology and artificial intelligence are influencing medicinal chemistry unprecedentedly.
What would you like to ask from other medicinal chemists?
Let’s train the next generation of medicinal chemists together, whether you are in academia or industry. That way, medicinal chemistry will always flourish, more than by anything else.
EFMC PHOTO COMPETITION 2020 - BACK TO THE LAB
The Communication Team is proud to announce the winner and runner of its annual Photo Competition, held this year entirely virtually through the EFMC Instagram Channel.
The winner is Cem Yamali (Turkey) and the second place is awarded to Pallabi Sengupta (India).
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS are pleased to announce the launch of our new website - https://www.rscbmcs.org. Please copy this into your favourites and use the link to access the latest information on BMCS activities, symposia and announcements
BMCS also remind all about the Malcolm Campbell Memorial Prize 2021 and announces various events.
REMINDER: MALCOLM CAMPBELL MEMORIAL PRIZE 2021
Nominations should be submitted no later than 31st October 2020 to:
Maggi Churchouse, RSC-BMCS Secretariat, e-mail: email@example.com
For further details, please access the activities link on https://www.rscbmcs.org
VIRTUAL MEETING - 31st MEDICINAL CHEMISTRY IN EASTERN ENGLAND (HATFIELD SYMPOSIUM)
26th November 2020
NB Please note date change from previous MedChemWatch
Synopsis: Known colloquially as the "Hatfield MedChem" meeting, this is a highly successful, long-standing, one-day annual meeting. The meeting aims to be informal and interactive, and offers excellent scientific development and networking opportunities for all those working in medicinal chemistry and drug discovery
21st RSC / SCI Medicinal Chemistry Symposium
12th to 15th September 2021, Churchill College, Cambridge, UK
The call for abstracts will close on 20th November (short talks) and 30th April (posters – first round)
Synopsis: Europe’s premier biennial Medicinal Chemistry event, focusing on first disclosures and new strategies in medicinal chemistry
THIS NEWSLETTER IS KINDLY SPONSORED BY MERCACHEMSYNCOM
ISSUE SPONSORED BY
MercachemSyncom is the leading major European drug-discovery CRO for solving your chemistry challenges, from small to medium-sized molecule hits, to the first GMP batches of identified clinical candidates. To capture a glimpse of our capabilities, please visit our webinar on October 21.
EFMC ORGANISED EVENTS
August 29-September 2, 2021
EFMC-ISMC 2021 - XXVI EFMC International Symposium on Medicinal Chemistry
September 2-3, 2021
EFMC-YMCS 2021 - 8th EFMC Young Medicinal Chemists’ Symposium
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry - New Opportunities in GPCR Drug Discovery
EFMC SPONSORED EVENTS
October 7-8, 2020
1st MercachemSyncom Digital Conference - Exploring New Modality Space by Precision Chemistry
November 5-7, 2020
18th Hellenic Symposium on Medicinal Chemistry (HSMC-18)
November 27, 2020
MedChem 2020 – Medicinal Chemistry in Belgium: Innovation and Success Stories
Tenure Track Assistant Professor at the Department of Biomedicine, Aarhus University, Department of Biomedicine Aarhus, Denmark
Associate Professor at the Department of Biomedicine, Aarhus University, Department of Biomedicine Aarhus, Denmark
Professor at the Department of Biomedicine, Aarhus University, Department of Biomedicine Aarhus, Denmark