2022 EFMC AWARDS ANNOUNCED!
The EFMC is proud to announce the names of the 2022 Awards winners.
Prof. Herbert Waldmann (Max Planck Institute of Molecular Physiology, Germany)
For his pioneering contribution to medicinal chemistry and chemical biology, and for the broad range of breakthrough concepts that laid the foundation of chemical biology as a discipline. Herbert Waldmann’s research is deeply interdisciplinary and further includes influential articles covering cell-based screening, activity-based protein profiling and chemical proteomics, genetics, and biophysics methodologies. Noteworthy, he fostered Europe’s scientific community through many partnerships across academia and industry and through his numerous scientific offspring.
Prof. Mike Waring (University of Newcastle, United Kingdom)
For his conceptual work on the role of lipophilicity and for the contribution to advance the field of covalent inhibitors in medicinal chemistry. Mike Waring has been involved in drug discovery and development projects that resulted in several drug candidates reaching clinical trials, including the EGFR inhibitor osimertinib for the treatment of non-small cell lung cancer. Overall, he has made impactful contributions to small molecule drug discovery using novel hit generation approaches such as DNA encoded libraries and fragment-based lead generation.
Prof. Alessio Ciulli (University of Dundee, United Kingdom)
For his pioneering work in the field of proteolysis-targeting chimera (PROTAC) technology for drug-induced targeted protein degradation. He has made substantial contributions to the development of new ligands of von Hippel-Lindau (VHL) E3 ligase, specifically bivalent small-molecule dimerisers of the VHL E3 ubiquitin ligase (VHL-based PROTACs) and elucidated their mechanism of action. Notably, Alessio Ciulli’s research provided a rational basis for the design and optimisation of the next generation of targeted protein degradation systems.
All three awards consist of a diploma, € 7.500, and an invitation to give a headline presentation at the EFMC International Symposium on Medicinal Chemistry.
The 2022 Awards will be presented at the XXVII EFMC "International Symposium on Medicinal Chemistry" (EFMC-ISMC), scheduled to take place in Nice, France on September 4-8, 2022.
2022 EFMC PRIZES ANNOUNCED
The EFMC is happy to announce the names of the 2022 "EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Industry" and the "EFMC Prize for a Young Medicinal Chemist or Chemical Biologis in Academia".
- 2022 EFMC Prize for Young Medicinal Chemist or Chemical Biologist in Academia
The selection committee designated Prof. Olalla Vazquez (Philipps-Universität Marburg, Germany) as the winner of the 2022 EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Academia.
Prof. Tiago Rodrigues (University of Lisbon, Portugal) and Dr Cristina Mayor Ruiz (IRB Barcelona, Spain) have been recognised as the most meritorious runners-up.
- 2022 EFMC Prize for Young Medicinal Chemist or Chemical Biologist in Industry
The selection committee designated Dr Marie-Hélène Larraufie (Almirall, Spain) as the winner of the 2022 EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Industry.
Dr Nadine Schneider (Novartis, Switzerland) has been recognised as the most meritorious runner-up.
The two prizes are given annually and consist of a diploma, € 1.000 and an invitation for a short presentation at an EFMC symposium. The 2022 prize-winners will be invited to give oral communications at the XXVII EFMC "International Symposium on Medicinal Chemistry" (EFMC-ISMC 2022).
More information about EFMC Prizes.
The “literature spotlight” section of the newsletter will bring you a summary of recently published research in a concise and accessible way. Multiple thematics from different journals will be highlighted thanks to the valuable contribution of members of the EFMC working groups.
This latest contribution will focus on the recently published article “Scaffold Hopping from Amodiaquine to Novel Nurr1 Agonist Chemotypes via Microscale Analogue Libraries” (by Daniel Merk in ChemMedChem).
Scaffold hopping is a strategy that gives access to structurally novel compounds; this method usually begins with compounds with known activity and permits the discovery of novel chemotypes by modifying the core structure of the molecule. Scaffold hopping is not only used to start projects with known ligands, it is also applied during lead optimization and may open access to new compounds with better physicochemical, and therefore PK, properties.
This strategy has been combined with microscale synthesis by Merk and co-workers to generate two libraries, the first one based on the 7-chloroquiolin-4-amine core fragment of amodiaquine, the second designed to replace this core scaffold.
The target of this study is the Nuclear receptor-related 1 (Nurr1) member of a subfamily of nuclear receptors acting as transcription factors activated by ligands, it can evolve as neuroprotective protein detected in high levels in neurons suggesting a possible therapeutic use in neurodegenerative diseases. Despite this suggestion, Nurr1 modulator molecules that can validate this therapeutic potential are rare.
This study, and the models that have been developed, indicate the important pharmacophore features of Nurr1 agonists and introduces the opportunity to run a virtual screen for the identification of further different bioactive molecules for use as Nurr1 ligands. This research also identified compound 4e, a new scaffold for structural optimization to obtain potent and selective Nurr1 agonists, that are facile to synthesize, validating microscale synthesis in plate format to enable early SAR elucidation and scaffold hopping in medicinal chemistry.
Merk, Daniel, et al. "Scaffold Hopping from Amodiaquine to Novel Nurr1 Agonist Chemotypes via Microscale Analogue Libraries" ChemMedChem (2022). https://doi.org/10.1002/cmdc.202200026
EFMC-ISMC 2022 – PROGRAMME AVAILABLE!
The programme for the XXVII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022), scheduled to take place in Nice, France is now available.
The programme will take place over 5 days, and will cover:
- advances in drug discovery in major therapeutic areas
- most recent advances in new technologies
- the interface between chemical biology and drug discovery
- first-time disclosures and recent highlights in medicinal chemistry
High level presentations by the three EFMC Award winners, as well as the Klaus Grohe Prize winner and IUPAC-Richter Prize winner will also be part of the symposium.
Abstracts for poster presentation can be submitted until June 23, 2022, with a 50€ handling fee.
- 6 Flash Poster Presentation Sessions will be organised
- 2 Poster Sessions will give ample time for discussion on-site
- 10 Best Poster Prizes will be awarded at the end of the symposium.
More information and registration www.efmc-ismc.org.
We look forward meeting you in Nice!
EFMC GRANTS 2022
EFMC is funding grants for EFMC organised events with the aim to support the participation of young academic scientists. In 2022, the following grants have been distributed:
16th EFMC Short Course in Medicinal Chemistry
- Doroteja NOVAK, University of Ljubljana, Slovenia
XXVII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022) & 9th EFMC Young Medicinal Chemists’ Symposium (EFMC-YMCS 2022)
- Gilles DEGOTTE, University of Liège, Belgium
- Elisabetta DI BELLO, Sapienza University of Rome, Italy
- Mihajlo GAJIC, Heinrich Heine Universität Düsseldorf, Germany
- Jessica GRAHAM, Newcastle University, United Kingdom
- Amalia KALAMPALIKI, National and Kapodistrian University of Athens, Greece
- Elizabeth A. LOPES, University of Lisbon, Portugal
- Carlos MAGALHAES DA SILVA, University of Aveiro, Portugal
- Maria MANEIRO REY, University of Santiago de Compostela, Spain
- Ángela MARTÍN-SERRANO ORTIZ, University of Alcalá, Spain
- Ana Teresa SILVA, University of Porto, Portugal
ONE YEAR OF THE CHEMICAL BIOLOGY INITIATIVE…AND MANY TO COME
Last year we wrote about the creation of the Chemical Biology Initiative within EFMC as a working group including eight chemical biologists representing the large field of chemical biology, belonging to different member societies and working in different countries.
The aim of the initiative is to increase the visibility of chemical biology within EFMC and describe the field of chemical biology for EFMC in order to make all researchers feel fully included and well represented. During the first year of its activities, this working group actively participated to EFMC activities and various new activities have been developed.
The working group is currently increasing its size, including new industrial members to increase inclusion and strengthen relationships between academics and the private sector in the field of chemical biology.
Activities of the Chemical Biology Initiative
THE CHEMICAL BIOLOGY-MEDICINAL CHEMISTRY CONTINUUM: EFMC’s VISION
The Chemical Biology Initiative members worked on a description of EFMC’s current understanding of chemical biology and its relation to interfacing disciplines such as medicinal chemistry, biology and biochemistry. In the editorial that the working group members published last year in ChemBioChem journal, the authors described chemical biology and medicinal chemistry as part of a scientific continuum, chemical biology being interdisciplinary and involving the development and use of chemical tools to explore and modulate biological systems in a precise and controlled approach.
You can read the articles following this link: https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cbic.202100319
ORGANIZATION OF AN E-SYMPOSIUM IN COLLABORATION WITH CHEMISTRY EUROPE
EFMC Chemical Biology Initiative organized an e-symposium in collaboration with ChemBioChem (Chemistry Europe) on October 19, 2021 in the presence of three outstanding speakers:
- Ed Tate, Imperial College London, UK
- Sascha Hoogendoorn, University of Geneva, Switzerland
- Thomas Carell, Ludwig-Maximilians-Universität München, Germany
ChemBioChem and its Editor-in-chief Ruben Ragg regularly organize virtual symposiums with a 2-hour format including three presentations from 3 pm to 5 pm (CEST), and thanks to the established collaboration between EFMC and Chemistry Europe more virtual symposiums on chemical biology will come, stay tuned!
MORE CHEMICAL BIOLOGY IN MEDCHEMBIOWATCH
As the name of MedChemWatch changes to MedChemBioWatch to participate to the evolution and inclusiveness of EFMC activities, the Chemical Biology Initiative members actively participated to the publication keeping the community updated with literature highlights, institutes presentations and national chemical biology groups news. The webpage of the Chemical Biology Initiative will soon collect these contribution for a focused news page about chemical biology in Europe.
INCREASE COOPERATION WITH OTHER NATIONAL CHEMICAL BIOLOGY GROUPS AND DIVISIONS
The working group also worked on increasing the interactions and cooperation with other national chemical biology groups and divisions with the aim to be inclusive of the entire scientific community in Europe and abroad. The Chemical Biology Initiative welcome new contacts so feel free to contact us if you wish for your chemical biology group to participate to EFMC activities!
Dr. Maria Duca, Chair of the Chemical Biology Initiative
GET TO KNOW MARIO VAN DER STELT (LEIDEN UNIVERSITY & ONCODE INSTITUTE, THE NETHERLANDS)
In this edition, our interviewee is Prof. Mario van der Stelt (Leiden University & Oncode Institute, The Netherlands). Get to know him better by reading the interview below:
Can you tell us more about your background?
I received my PhD diploma in chemistry (cum laude) from Utrecht University on April 2002. My thesis was about the metabolism and neuroprotective properties of anandamide, an endogenous ligand of the cannabinoid receptors. After a post-doctoral position in cell biology in the lab of Prof. dr. Vincenzo di Marzo, I worked for almost eight years in the Research Laboratories of Merck (former Organon) in the Netherlands. I was a group leader in the medicinal chemistry department of Prof. dr. Stan van Boeckel and served as project leader for several programs ranging from hit identification up to clinical candidate selection. In 2012, I decided to go back to academia to start my own research group, where I combine medicinal chemistry with chemical biology at Leiden University.
Where are you currently working and what is your current position? What are your current research interests?
Currently, I am a full professor and chair of Molecular Physiology at the Leiden Institute of Chemistry and a principal investigator of Oncode Institute. Our aim is to design, synthesize and apply chemical tools to study important biological and biomedical questions. We have a focus on kinase and lipid signalling. We use techniques from different fields, including chemical biology, computational chemistry, medicinal chemistry and molecular biology, to determine and predict the interaction of small molecules with proteins in physiological and disease processes.
Our long-term aim is to discover drug candidates to treat cancer, (drug-resistant) infections and brain disorders. The group consists of two assistant professors (Dr. Stephan Hacker and Dr. Anthe Janssen), 4 post-docs, 16 PhD-students & technicians and >20 M.Sc and B.Sc students. We are embedded in the Leiden Early Drug Discovery network (https://www.universiteitleiden.nl/en/science/led3). Finally, I am the workstream leader of small molecule drug discovery from Oncode-PACT, an (inter)national consortium that has recently been awarded 325 million Euros from the Netherlands government to accelerate preclinical drug discovery for oncology (https://www.oncode.nl/Oncode-PACT).
What do you consider your greatest achievement in your scientific career?
The integration of activity-based protein profiling (ABPP, chemical proteomics) in the drug discovery process has allowed us to discover and profile inhibitors of lipid and kinase signalling. For example, we have shown that BIA 10-2474, a FAAH inhibitor which killed a healthy volunteer in a phase 1 clinical trial in France in 2016, was a promiscuous lipase inhibitor that disrupted the lipid homeostasis in human cortical neurons (1). These results were used in the decision-making process by companies to resume clinical trials with other FAAH inhibitors.
Currently, we collaborate with biotech and pharmaceutical companies to apply ABPP in the hit- and lead optimisation process to guide the selection of the best clinical candidates. ABPP has also enabled us to discover the first brain active inhibitors of various biosynthetic enzymes of distinct endocannabinoids (2,3). These compounds are now widely used to study the physiological role of these signalling lipids. Furthermore, we developed a target validation strategy for kinases in which we combine ABPP with chemical genetics (4).
I am still amazed that by changing one amino acid in an endogenously expressed kinase in human cells by CRISPR-Cas9, we could visualize target engagement of this specific kinase by a complementary, fluorescently labelled covalent probe.
Which of your papers are you most proud of and why?
- Van Esbroeck et al., Science, 2017, 356, 1084
- Ogasawara et al., Proc. Natl. Acad Sci. USA, 2016, 113, 26
- Mock et al., Nature Chem. Biol., 2020,16, 667
- Van der Wel et al., Nature Comm., 2020, 11, 1
What are the features of a successful PhD student or postdoc?
To have a successful PhD, it is important that you are intrinsically motivated and are curious to learn new topics and techniques. Read the literature, go to conferences and talk to people. You are venturing into new, unknown territory; therefore, it is important to be perseverant, not to give up when something is not working the first, second or even a third time. If it was easy, then somebody else would already have done it.
I like to work on the interface between chemistry and biology, because I am convinced that new chemical tools and methods will allow us to address important biological questions. In my group chemists and biologists work closely together and they have to learn to speak each other’s language to move their projects forward. Thus, team spirit, collaboration and good communication skills are important as well. If you share success, it will become bigger.
What is the most embarrassing thing you have done in the lab while doing experiments?
At the first day of my PhD, I made use of a magnetic stirrer to dissolve some components of a buffer. I put the bottle next to a flask of a colleague. I did not know the magnetic stirrer was also a heating block. By turning it on, I accidently denatured her precious protein preparation, which had taken her several weeks to obtain…. that was quite an introduction. Fortunately, we could still get along after this embarrassing mistake.
What are your recommendations for a book, podcast, website, blog, YouTube channel or film?
Of course, everyone working in medicinal chemistry should read the blog ‘In the pipeline’ from Derek Lowe.
Which scientist do you admire the most and why?
Prof. dr. Raphael Mechoulam is an inspiration for me. He discovered the structure of THC, the psychoactive component of cannabis sativa in 1964 and almost 30 years later he also identified anandamide, the first endogenous cannabinoid in the brain. Thereby, he, as a medicinal chemist, discovered a whole new physiological system and started a novel field with great opportunities for drug discovery.
Which field of medicinal chemistry do you consider the most promising for the future?
As a medicinal chemist/chemical biologist, I think it is important to develop technologies that will allow us to predict and characterize the interaction of small molecules across the entire human proteome in a living cell. Computational chemical biology (such as machine learning) combined with chemical proteomics, metabolomics and molecular & structural biology will allow us to make a molecular encyclopaedia of ligand-protein interactions and their function. Single molecule resolution imaging techniques using specific fluorescent probes will allow us to localize where these interactions take place in cells or tissues. Together, this will provide a better molecular understanding of human biology in health and disease and will lead to more efficacious and safer drugs in an efficient manner.
NEWS FROM THE DIVISION FOR MEDICINAL CHEMISTRY & CHEMICAL BIOLOGY (DMCCB)
The DMCCB is pleased to invite you to the Swiss Summer School on Chemical Biology taking place in Les Diablerets, Switzerland, September 11-15, 2022 as well as to the International Symposium on Chemical Biology taking place in Geneva, Switzerland, from November 8-10, 2022.
Swiss Summer Schools are out-of-town seminars intended for MSc, PhD students and postdoctoral researchers with a focus on chemical synthesis or chemical biology. They offer a platform for the scientific exchange with peers and lecturers from academia and industry. The goal is that the young researchers actively participate in the scientific exchange and also present a poster or a short communication on their research. The scientific program, which received EFMC certification, will consist of speakers from industry and academia giving courses on different topics in chemical biology, sponsored industry lectures, career sessions and workshops. For more details and registration please check out the website.
Organized by the NCCR Chemical Biology, The International Symposium on Chemical Biology is one of the premier events for local and international communities of researchers interested in all aspects of chemical biology. Its 4th edition is taking place on November 8 to 10, 2022 in Geneva, Switzerland and online. The event once again boasts an impressive speaker line-up featuring 15 international leading scientists in the field covering a great diversity of topics. These talks will be set in an overall framework that is carefully crafted to provide ample opportunity for networking across the global community of academics and industrial scientists, as well as to stimulate interdisciplinary discussions. Travel awards dedicated to recognize excellent science from young researchers presenting posters, are also planned.
During the event, the EFMC and the SCS will officially announce that they will take over the organization of the Symposium in the future and provide further information on the 2023 edition in Basel, Switzerland.
Discover the full list of speakers & topics
Early bird registration to the in-person event (Geneva): June 30, 2022
Regular registration: October 18, 2022
Author: Antonia F. Stepan, Roche Pharma Research and Early Development, Roche Innovation Center Basel, F. Ho''.chr('64256').''mann-La Roche AG, 4070 Basel, Switzerland
#MedChemCASES - SEMINAR BY THE DIVISION OF MEDICINAL CHEMISTRY OF THE GERMAN CHEMICAL SOCIETY (GDCH)
The MedChem Division of the German Chemical Society (GDCh) would like to invite you to the next #MedChemCASES online seminar which will be held on May 24 by Dr Tim Owens (Principia – Sanofi, Germany).
The topic of the webinar will be "Development of Reversible Covalent Inhibitors as Chemical Probes and Clinical Candidates”
In 2013, Serafimova assessed a series of electrophilic molecules that engaged non-catalytic cysteines in a covalent manner, but with variable target residence times, driven by the various stabilizing interactions of the molecule in the protein binding site. These reversible covalent inhibitors were shown to rapidly dissociate from common thiols while maintaining sustained inhibition of a target protein even after washout. This technology, therefore, has the potential to allow medicinal chemists to fashion inhibitors with the potential for selectivity gained by inhibiting only targets with a conserved cysteine, and minimal exposure requirements inherent with covalent inhibition. The reversible covalent approach furthermore mitigates risk of irreversible binding to non-target cysteines or endogenous thiols, but also allows the potential to improve selectivity among targets sharing a common cysteine.This technology has been used to identify selective inhibitors of kinases such as BTK and FGFR as well as the LMP7 subunit of the immunoproteasome. Based on our interest in BTK inhibition for the treatment of immune-mediated disorders, we embarked on a drug development effort to identify reversible covalent inhibitors, culminating in the identification of PRN473 for topical administration and PRN1008 (rilzabrutinib) as an oral BTK inhibitor currently in multiple phase 3 studies.
Register for free here:
#GDCh (MedChem Division), #NextGenMedChem.
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is delighted to announce some upcoming events.
- AI in Chemistry: 5th RCS-BMCS /RSC-CICAG Artificial Intelligence in Chemistry
- 8th RSC/SCI symposium on GPCRs in Medicinal Chemistry
- RSC-BMCS Targeted Protein Degradation: “Three’s a crowd ?”
AI in Chemistry: 5th RCS-BMCS /RSC-CICAG Artificial Intelligence in Chemistry
1st and 2nd September 2022, Churchill College, Cambridge and virtual
The call for abstracts will close on 22nd April, 2022 (oral) and 2nd June, 2022 (poster)
Synopsis: Artificial Intelligence is presently experiencing a renaissance in development of new methods and practical applications to ongoing challenges in Chemistry. Following the successes of three annual “Artificial Intelligence in Chemistry” meetings starting in 2018, we are pleased to announce that the Biological & Medicinal Chemistry Sector (BMCS) and Chemical Information & Computer Applications Group (CICAG) of the Royal Society of Chemistry are once again organising a conference to present the current efforts in applying these new methods. The meeting will be held over two days and combine aspects of artificial intelligence and deep machine learning methods to applications in chemistry
8th RSC/SCI symposium on GPCRs in Medicinal Chemistry
5th to 7th October 2022, Verona, Italy
Delegate Registration and Exhibitor/Sponsor registration is now open
The call for poster abstracts will close on Thursday, 11th August
Closing date for bursary application is Tuesday, 23rd August
Synopsis: The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We are pleased to be holding this 8th meeting in the series on GPCR drug discovery, which will combine cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.
RSC-BMCS Targeted Protein Degradation: “Three’s a crowd ?”
16th and 17th November 2022, Virtual
Abstract submission will be open soon, please keep checking website for updates
Synopsis: Targeted protein degradation is a rapidly developing field of drug discovery which is expanding the proportion of human proteins which are tractable drug targets. Whereas conventional small molecules are designed to block the activity of a protein, targeted protein degraders act by harnessing biological pathways to remove the protein entirely. This conference will showcase presentations showing the application and development of degradation technologies such as molecular glues and heterobifunctional degraders (e.g. PROTACs)
THIS NEWSLETTER IS KINDLY SPONSORED BY
ISSUE SPONSORED BY
For over 30 years, the world’s leading life sciences companies have made Symeres part of their team. From hit generation and lead optimization, ADME-Tox via our Admescope organization, through to complex synthetic chemistry, route development and clinical supply, we help to create safe, innovative therapies. We make molecules matter. Together.
EFMC ORGANISED EVENTS
September 4-8, 2022
XXVll EFMC International Symposium on Medicinal Chemistry
September 8-9, 2022
9th EFMC Young Medicinal Chemists' Symposium
EFMC SPONSORED EVENTS
June 17, 2022
3rd Medicinal Chemistry Ireland conference
July 6-7, 2022
2nd Transatlantic ECI GPCR Symposium
July 22, 2022
VIII SEQT Young Researchers Symposium
September 11-14, 2022
27th National Meeting in Medicinal in Medicinal Chemistry
September 15-17, 2022
9th BBBB International Conference on Pharmaceutical Sciences - Pharma sciences of tomorrow
EFMC CERTIFIED SCHOOLS
July 3-7, 2022
41st Edition of the European School of Medicinal Chemistry (ESMEC 2022)
July 19-21, 2022
Medicinal Chemistry and Chemical Biology in Drug Discovery: the Pharma Perspective
September 11-15, 2022
Les Diablerets (VD), Switzerland
Swiss Summer School on Chemical Biology
October 9-14 2022
Swiss School on Medicinal Chemistry in Leysin
EFMC SPONSORED SCHOOLS
September 21-23, 2022
Summer School in Pharmaceutical Analysis (SSPA2022)
two Postdoctoral researchers, Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS) Saarbrücken, GERMANY
Post-doc positions in Medicinal Chemistry, 100%, University of Basel, Department of Biomedicine Basel, SWITZERLAND
Scientist Medicinal Chemistry, Proxygen GmbH, Chemistry Vienna, AUSTRIA
Medicinal Chemist, SpiroChem AG, Chemistry Basel, SWITZERLAND