2021 EFMC HONORARY FELLOWS ANNOUNCED!
The EFMC is very proud to announce the 2021 EFMC Honorary Fellows.
EFMC Honorary Fellow is a life-long title with the aim to recognize individuals who have provided outstanding support to the EFMC and contributed in strengthening the position of medicinal chemistry, chemical biology, or related fields in Europe.
Congratulations and thanks to:
Prof. Bernd Clement is recognized worldwide for his seminal and innovative contributions to medicinal chemistry in the areas of both drug metabolism and prodrug chemistry. In addition to the impact on drug discovery and drug development, the committee also considered his contributions in strengthening the position of medicinal chemistry at European level as being particularly relevant. Prof. Clement has been always one of the most active members of EFMC; he has represented the Pharmaceutical/Medicinal Chemistry group of the German Pharmaceutical Society as a Council member since 2007. He was also co-chair of the 22nd EFMC International Symposium on Medicinal Chemistry in Berlin (2012), which was a great success. In addition, Prof. Clement has played a major role in medicinal chemistry within other major international societies.
Ly and Edmond Differding were proposed for a joint nomination to the EFMC Honorary Fellowship. While this recognition is normally meant for single individuals, the committee felt that the contribution of Ly and Edmond Differding to the EFMC, and to the advancement of medicinal chemistry in Europe, was very much intertwined. Edmond Differding held the position of EFMC secretary and vice-chair, contributing to the reorganization of the EFMC, and to the development of its new structure at a period that helped shape the Federation. More recently, he was actively involved in the celebration of EFMC’s 50th anniversary, preparing two papers that review the scientific content of all EFMC-ISMC and the development of medicinal chemistry in Europe. Ly Differding plays a pivotal role in EFMC and in the organisation of some premier EFMC conferences. She actively participates in EFMC activities and not only guarantees operational support, but also provides continual advice and an historical perspective to the president, executive committee, and conference organizers. Her dedicated contributions to the success of EFMC and medicinal chemistry in Europe is unparalleled. Furthermore, Ly fully supported the EFMC during the recent pandemic crisis, proactively searching for creative solutions and facilitating their implementation.
In addition, the committee considered the following people for posthumous recognition:
Prof. Wijbe Nauta (d. 1986) was one of the founding fathers of the EFMC. He was Secretary in the early years of EFMC, playing a key role in the internationalisation of the first national organisations and promoting medicinal chemistry as an independent chemical discipline, especially characterised by its interdisciplinary nature. As a member of the UPAC’s commission on medicinal chemistry, itself a part of the Division of Organic Chemistry, Prof. Nauta promoted the EFMC through his contributions to the IUPAC Medicinal Chemistry Newsletter. Importantly, he took the initiative to organize the fourth ISMC in1974. He also initiated the book series Pharmacochemistry Library (Elsevier), of which more than 35 volumes were published, being the first editor of this series. The EFMC Pharmacochemistry Award for medicinal chemistry and chemical biology carries his name. Prof. Nauta kept a large amount of documentation regarding the first years of the Federation, which are now in the archives of EFMC.
Dr Emilio Kyburz (d. 2005) was very active in the EFMC, as he was a member of the executive committee in 1989, vice-chair in 1991-92, elected as chairman in 1995, secretary in 1997 and re-elected in this position in 1999. During this period, Dr. Kyburz put much emphasis on internationalisation of the medicinal chemistry developed in Europe, especially in expanding the committee’s interactions with the ACS. His well-curated archives, combined with those of Prof. Nauta, allowed EFMC to accurately revisit its history for the first 30 years of existence.
The official ceremony will take place during the opening of the XXVI EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2021), scheduled to take place from August 29-September 2, 2021.
The EFMC Recognition Programme will continue awarding outstanding contributors to EFMC and sciences in the future. More information is available here: www.efmc.info/honorary-fellows.
EFMC WELCOMES HERMEN OVERKLEEFT AND INGO HARTUNG IN THE ADVISORY BOARD
Prof. Hermen Overkleeft (University of Leiden, The Netherlands) and Dr Ingo Hartung (Merck, Germany) have been accepted onto the Advisory Board of the EFMC for a period of three years, joining the current members:
- Yves P. Auberson (Novartis, Switzerland) - Chair
- Maria Laura Bolognesi (University of Bologna, Italy)
- Karin Briner (Novartis, USA)
- Herbert Waldmann (Max Planck Institute of Molecular Physiology, Germany)
The Advisory Board is an EFMC consulting body assisting in assessing the Federation's strategic goals.
More information on EFMC Advisory Board.
The “literature spotlight” section of the newsletter aims to bring you a summary of the recently published research in a concise and readable way. Papers covering a range of medicinal chemistry and chemical biology from a variety of journals will be explored by the Communication Team; today’s excerpt is brought to you by Matic Proj (University of Ljubljana, Slovenia).
This twelfth contribution will focus on the recently published article on “Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry" (by Rambabu N. Reddi, Efrat Resnick et al. in JACS).
Acrylamides and other α,β-unsaturated carbonyl compounds are the most commonly used electrophiles in the development of covalent drugs. The reactivity of acrylamides can be tuned by altering the amine precursor, but this usually affects protein binding as well, since this part of the covalent inhibitor is responsible for noncovalent interactions and warhead positioning. Furthermore, the reactivity of acrylamides can be decreased by α- or β-substitutions and increased by electron-withdrawing substituents at the α-position.
Reddi et al. have recently described a new class of tunable electrophiles with hetero-substitutions on α-methacrylamides. Surprisingly, substituted methacrylamides favour an addition−elimination reaction over the Michael addition typical of acrylamides. The reactivity is predictable and depends on the pKa of the respective leaving group. Moreover, the majority of these compounds showed reduced reactivity compared to the parent unsubstituted acrylamide, as determined by monitoring the reaction with GSH. In the context of the acrylamide BTK inhibitor ibrutinib, lowering the reactivity while maintaining protein binding resulted in improved selectivity. This new class of covalent warheads is thus useful for late stage optimization of covalent inhibitors, particularly acrylamides. More excitingly, the addition−elimination mechanism can be used for the functionalization of covalent inhibitors. The leaving group (α-methacrylamide substituent) can be a turn-on fluorescent probe, as demonstrated with ibrutinib (BTK inhibitor), afatinib (EGFR inhibitor), and AMG-510 (K-RASG12C inhibitor). In addition, the authors developed a high-throughput screen against BTK using a turn-on chemiluminescent probe attached to ibrutinib. This competition-based assay does not require substrate or enzymatic reaction optimization, unlike conventional in vitro enzymatic assays, but it does require a suitable cysteine near the target binding site. Several potential applications of the new concept, named Covalent Ligand Directed Release Chemistry (CoLDR), are discussed, e.g. the release of pro-drugs, chemotherapeutics, imaging agents, or self-immolative linkers. Overall, the substituted methacrylamides are a novel and versatile class of warheads with many possible applications for the design of targeted covalent inhibitors.
Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry
Rambabu N. Reddi, Efrat Resnick, Adi Rogel, Boddu Venkateswara Rao, Ronen Gabizon, Kim Goldenberg, Neta Gurwicz, Daniel Zaidman, Alexander Plotnikov, Haim Barr, Ziv Shulman, and Nir London
Journal of the American Chemical Society Article ASAP
MEET THE NEW EFMC PRESIDENT: RUI MOREIRA (UNIVERSITY OF LISBON, PORTUGAL)
In this edition, our #Iamamedicinalchemist is no other than the EFMC President for the next three years: Prof. Rui Moreira (University of Lisbon, Portugal). Get to know him better by reading our interview below.
How did you get interested in Medicinal Chemistry?
Chemistry and biology were my favourite topics in high school, which led me to choose pharmaceutical sciences when I entered university. When I first studied medicinal chemistry as a second-year student, I was immediately fascinated how chemistry could be used to address almost any major medical need. This passion was decisive when it came to decide how to develop my scientific career.
Where and when did you obtain your PhD diploma?
I obtained my PhD degree in pharmaceutical chemistry at the University of Lisbon in 1991, under the supervision of Professor Eduarda Rosa.
What was the topic of your PhD project?
My research topic was the design and evaluation of novel prodrugs for anticancer agents. I was particularly interested in studying the mechanisms of chemical and enzymatic activation of these prodrugs, and to determine the structure-reactivity relationships that could be used to design prodrugs with improved drug delivery. This was an exciting project that brought together medicinal chemistry and the principles of physical organic chemistry.
Where did you have your postdoc position?
While not having a formal postdoc position, I did my postdoctoral research with Professor Jim Iley, at the chemistry department, The Open University, UK.
Where are you currently working and what is your current position?
I am a full professor of medicinal chemistry at the Faculty of Pharmacy, University of Lisbon, where I run a laboratory with ca. 20 people comprising research associates, postdocs and students.
What are your current research interests?
My background in physical organic chemistry led me to be interested in the design of covalent inhibitors and activity-based probes for target identification, where understanding the intrinsic reactivity associated to this type of compounds is fundamental to modulate their selectivity. Another major research topic in my group is the development of anti-infectious agents based on dual-targeting approaches as a strategy to overcome drug resistance, with a focus on parasitic diseases (e.g. malaria) and tuberculosis. Finally, we are also interested in developing tumour-activated prodrugs that use specific cellular signatures (e.g. iron level, hypoxia and oxidative stress) as triggering mechanisms to release the parent drug.
What are the features of a successful PhD student or postdoc?
Be passionate about the research project, but always with a critical mind. Do not be afraid to ask questions, because there aren’t any silly questions in Science.
How would you describe yourself as a supervisor?
Supervising students goes beyond providing scientific guidance. Mentoring is crucial for career development and I always encourage and motivate students at a personal level when problems arise during their projects.
What are your recommendations for a book, podcast, website, blog, YouTube channel or film?
My recommendation goes to the EFMC website and EFMC YouTube channel, what else?
Which scientist do you admire the most and why?
Marie Curie comes first in my list of scientists that I admire. Not only for her contribution to the use of radiation in medicine, which set the stage for the modern cancer therapies and imaging/diagnostic tools that help to save lives every day, but, even more importantly, for her perseverance at a time when being a woman was a limitation to scientific and academic success.
What would you expect to be the next major breakthrough in medicinal chemistry?
CRISPR–Cas9 will soon become a mainstream drug discovery tool, and particularly useful in helping to identify target molecules for precision medicine. Gene editing with CRISPR–Cas provides a unique opportunity to determine which genes and proteins can cause or prevent a specific disease, thus paving the way for the development of tailor-made drugs for unmet medical needs. In addition, chemical probes that can enable a highly precise spatiotemporal control of CRISPR-Cas machinery are also expected to revolutionise the therapeutic use of this technology.
#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 18 by Prof. Cristina Nevado (University of Zurich, Switzerland).
The topic of the webinar will be Exploring the chemistry and biology of CREBBP and EP300 Bromodomains.
Expanding the chemical space and simultaneously ensuring synthetic accessibility is of upmost importance, not only for the discovery of effective binders for novel protein classes but, more importantly, for the development of compounds against hard-to-drug proteins. In this talk we will introduce AutoCouple, a de novo approach to computational ligand design focused on the diversity-oriented generation of chemical entities via virtual couplings. In a benchmark application, chemically diverse compounds with low-nanomolar potency for the CBP bromodomain and high selectivity against the BRD4(1) bromodomain were achieved by the synthesis and design of ~50 derivatives of the original fragment. The binding mode was confirmed by X-ray crystallography, target engagement in cells was demonstrated, and antiproliferative activity was showcased in three cancer cell lines.
Register for free here: https://zoom.us/webinar/register/WN_lM5GrezXSVq0K7XVXld3Dw
#GDCh (MedChem Division), #NextGenMedChem.
NEWS FROM THE CHEMICAL BIOLOGY GROUP OF THE FRENCH CHEMICAL SOCIETY (SCF)
Join the SCF-ChemBio on April 27, 3-5 PM CET (UTC+1) for their inaugural symposium together with ChemBioChem. Enjoy three exciting 20-minute presentations with interactive question-and-answer sessions.
- The ins and outs of initiating glycoconjugate biosynthesis at the membrane frontier
Barbara Imperiali (MIT, United States)
- Fluorescent probes for live-cell imaging
Kai Johnsson (MPI Heidelberg, Germany)
- Role of metals in the regulation of cell plasticity
Raphaël Rodriguez (Institut Curie, France)
The event will be moderated by SCF-ChemBio president Boris Vauzeilles (ICSN, France) and ICBS president-elect Zaneta Nikolovska-Coleska (University of Michigan, United States).
Register for free here: https://www.workcast.com/register?cpak=7054213175859028&referrer=Twitter&HootPostid="88a85a04"-2f5b-4e8e-9a8d-fa084bd9236c&Socialprofile=wiley_chemistry&Socialnetwork=twitter
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is delighted to invite nominations for the 10th Capps Green Zomaya Memorial Award in medicinal or computational chemistry. We would also like to announce and congratulate the winners of the 2021 BMCS Travel Prize. In addition, the BMCS would like to remind you about the poster deadline (April 30th) for the 21st RSC/SCI Medicinal Chemistry Symposium. You are cordiallyinvited to read the honorary Chairman’s report following the 49th BMCS Annual General Meeting.
CAPPS GREEN ZOMAYA MEMORIAL AWARD 2022
The BMCS is pleased to invite nominations for the tenth Capps Green Zomaya Memorial Award in medicinal or computational chemistry. The Award will be given to the individual judged to have made an important contribution to the discovery or development of new medicines. Nominations are invited for candidates, up to the age of 40, working in UK or international laboratories (candidates over the age of 40, who have taken career breaks, will be considered). A Royal Society of Chemistry commemorative medal and certificate will be awarded to accompany the prize of £2,000.
Nominations should be submitted no later than October 31, 2021 to:
Maggi Churchouse, RSC-BMCS Secretariat
Telephone: +44 (0)1359 221004 E-mail: email@example.com
For further details, please access the activities link on https://www.rscbmcs.org.
2021 TRAVEL PRIZE WINNERS
The RSC Biological and Medicinal Chemistry Sector (BMCS) is pleased to announce the winners of the 2021 BMCS Travel Prize:
- Arron Aatkar, University of Strathclyde
- Vihange Munasinghe, University of Oxford
- Sarah Memarzadeh, University of Glasgow
- Katherine Macfarlane, University of Strathclyde
The BMCS introduced the International Travel Prize programme in 2014 as an initiative to support, encourage, and develop the training of next-generation research leaders. The winners receive funding of up to £2000 to support their attendance at, and travel to, high impact international conferences relevant to their projects.
The diversity of projects in the 2021 applications was even greater than in previous years, and the quality of all the applications extremely impressive, making the selection of the eventual winners a hugely challenging task for the judges.
They, along with all the members of the BMCS committee, would like to congratulate the winners, and sincerely thank all the participants for the excellence of their applications.
21st RSC / SCI Medicinal Chemistry Symposium
12th to 15th September 2021, Churchill College, Cambridge, UK
The call for poster abstracts will close on April 30.
Synopsis: Europe’s premier biennial Medicinal Chemistry event, focusing on first disclosures and new strategies in medicinal chemistry
BMCS HONORARY CHAIRMAN’S REPORT FROM THE 49th ANNUAL BMCS AGM
Barely a week after the 48th AGM in March 2020 the whole of the UK went into lockdown, in response to the COVID-19 pandemic. Since then, the BMCS group have been living through a Chinese proverb, we have truly been living in interesting times.
I have been immensely impressed by the way in which the group has adapted and reacted to the rapidly evolving circumstances occurring in the wider society. Faced with tremendous uncertainties, we have nevertheless continued to drive forward with our many strands of activity, to the best of our collective abilities, demonstrating impressive flexibility, adaptability, and determination. Constrained by the pandemic, we have reformatted many of our longstanding meetings and continued to deliver a program of high-quality scientific events, educational support grants (ESG), and International Travel Prizes, under the most trying of external circumstances. Thank you to all my BMCS committee colleagues for this huge collective effort.
In response to the global pandemic situation, we took the decision to extend the deadline by which winners of 2020 International Travel Prizes should take up their prize until the end of 2021. We hope that the second half of the year will offer a realistic prospect for the resumption of some face-to-face meetings. Zoom, Teams, Meetings Now, GoToMeeting have served us well during the crisis, but feedback from delegates tells us that there is a strong appetite for face-to-face meetings. The group has experienced a significant reduction in revenue, but we have awarded 2021 Travel Prizes, albeit fewer in number than previously. The ESG have seen a significant reduction in the number of applications received, probably because of complete or partial closure of schools, but we have still been able to offer support to those applications that were received.
This year we face significant personnel changes in the committee. Elaine and Stuart will be stepping down from their long-held roles as Treasurer and Secretary respectively, and I’m sure that I speak for the whole of the committee when I say thank you for your many years of stalwart service and loyalty to the group. Replacing them, I would like to welcome Douglas as Treasure and Nadia as Secretary. We will also be saying goodbye to Steve and Mihiro, who are stepping down from the committee, thank you for all your contributions towards the activities of the group. As mentioned in the previous report, Maggi will be stepping down from her secretariat position after the Cambridge Med Chem meeting in September, and I am happy to report that the near-Herculean task of identifying a successor is proceeding well.
The pandemic-related uncertainty will continue for some time to come, but the prospects for a return to normality are good. I reflect that, in the scant year since the last AGM, multiple vaccines against the virus have been developed, approved, and in this country delivered to more than 20 million people. Through the combined efforts of hundreds of medicinal chemists and biomedical scientists, several existing medicines have been repurposed for COVID therapy and have undoubtedly saved many lives. New drugs have been discovered and are entering clinical trials now. The speed of progress has been almost as bewildering as the effects of lockdown. In recognition of these combined efforts, we have decided to award the Malcolm Campbell Award this year not to an individual or a single team, but to all the British scientists involved in coronavirus research. We hope to present the award at the Cambridge Med Chem meeting in September, to someone we feel is qualified to represent the whole of the research community.
We look forward to a return to normality in 2022, but perhaps a new normality that blends the familiar from previous years with the opportunities that virtual media allow in terms of involvement of a wider number of delegates.
A C Williams, Hon. Chairman, BMCS
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EFMC ORGANISED EVENTS
August 29-September 2, 2021
EFMC-ISMC 2021 - XXVI EFMC International Symposium on Medicinal Chemistry
September 9-10, 2021
EFMC-YMCS 2021 - 8th EFMC Young Medicinal Chemists’ Symposium
EFMC SPONSORED EVENTS
April 14-15, 2021
Kinase 2021: 9th RSC / SCI Symposium on Kinase Inhibitor Design
April 20, 2021
2nd Nucleosides and Nucleotides: Synthetic and Biological Chemistry
April 26-29, 2021
13th Young Medicinal Chemist's Symposium - Nuove Prospettive in Chimica Farmaceutica
April 29, 2021
The 3rd SCI-RSC Symposium on Transporters in Drug Discovery and Development
April 29, 2021
32nd Symposium on Medicinal Chemistry in Eastern England
June 29-30, 2021
The BMCS Mastering MedChem VI: 6th RSC-BMCS Symposium on Mastering Medicinal Chemistry
July 7-9, 2021
56th International Conference on Medicinal Chemistry (RICT 2021)
EFMC SPONSORED SCHOOLS
June 27-July 1, 2021
40th Edition of the European School of Medicinal Chemistry (ESMEC)
September 13 – 17, 2021
EUROPIN Summer School on Drug Design
September 22-24, 2021
Summer School in Pharmaceutical Analysis (SSPA2021)
October 3-10, 2021
14th Swiss Course on Medicinal Chemistry
Assistant/Associate Professor (tenure track) / Full Professor, Leiden University, Medicinal Chemistry and Drug Discovery, Leiden
Postdoctoral Researcher Pharmaceutical Sciences / Toxicity Prediction, University of Vienna, Department of Pharmaceutical Sciences - Pharmacoinformatics Research Group, Vienna
Cheminformatician (M/F) DISCNGINE, Ile de France Paris, France
Drug Hunter @Aqemia, deeptech startup leveraging AI and quantum-inspired physics for drug discovery, AQEMIA, Paris, France
Analytical Scientist, Symeres, Groningen
Analytical Chemist, Symeres, Nijmegen
(Senior) Organic Chemist, Symeres, Nijmegen