A MESSAGE FROM EFMC
The current pandemic has repercussions through the entire world, and of course EFMC also endures its consequences. While postponing several events, we however kept in mind that challenges create opportunities, and we are now developing an online offer to keep our community dynamic and well-connected. You will find some initial information about the next steps in this newsletter. Stay tuned to EFMC over the next few months, and take advantage of our upcoming activities and virtual symposia.
We are not at the end of the pandemic, not yet, and we learned a few good lessons already. We learned that even though good hygiene can bend an epidemic effectively, medicinal chemistry and chemical biology will remain critical in discovering these badly needed drugs and vaccines. We saw that our community is flexible in difficult times, and that academia and pharmaceutical industries can come together to make science progress very fast. I hope we will remember that after the pandemic. Looking back at how fast our knowledge of the disease has progressed, it is worth ensuring that we collaborate better in the future. We have also learned new ways to work and interact while staying at home. Will it influence our travelling, work and consumption habits, and help reduce stress and environmental impact in the long term? It is up to us. I hope we will all take the opportunity of this experience to pause, think, and implement solutions for a better future.
For now, please keep leading by example and actively spread science-based information about the pandemic. Our scientific community can contribute help and guidance through the first steps of de-confinement. It is important to show patience and do it right as we do not want to see a second wave of contamination. We also want to fight unnecessary fears, which in the long term would handicap our society. After these difficult months, let’s get ready to embrace a future that capitalizes on the new opportunities, and the best possible science.
I’m looking forward to seeing you all again soon – maybe virtually?
Stay healthy and confident,
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 third contribution will focus on the recently published review article on innovative medicinal chemistry approaches toward SARS-Coronavirus and Covid-19 (by Gosh et al. in ChemMedChem).
COVID-19 is a daily reality for all of us. We listen, read, see and in the worst cases are directly affected by the pandemic caused by SARS-CoV-2. COVID-19 has spread around the globe with such speed and virulence that it has created a health emergency not seen for 100 years and challenged the fabric of society. Right now we do not have an effective vaccine or other treatments such as small molecules against COVID-19 or other similar pathogenic coronaviruses. Thus, the development of novel, innovative antiviral agents is of uttermost importance. It is difficult to select one paper from the quantities appearing in the literature, but this month we have chosen the recent review by Gosh et al. which sets out the state of the art from a medicinal chemist’s viewpoint. First, they highlight the biochemical events crucial for SARS-CoV-2 replication which are attractive targets for drug development, such as the spike protein for binding to host cell surface receptor, proteolytic enzymes fundamental for processing polyproteins into mature viruses, and RNA polymerases for RNA replication.
The authors critically review the various design approaches as well as shed light on the various high throughput screening efforts led resulting in diverse lead structures, of both well-established drugs as well as novel potentially highly promising molecules. The present review is a concise, useful guide for the development of effective therapy against COVID-19 and other pathogenic coronaviruses certainly stimulating research in this direction. HIV is still best treated by small molecules. There are evidently plenty of opportunities for medicinal chemists to make vital contributions to overcoming SARS-CoV-2 infection and COVID-19.
Ghosh, A..K., Brindisi, M., Shahabi, D., Chapman, M..E. and Mesecar, A..D. (2020), Drug Development and Medicinal Chemistry Efforts Toward SARS''.chr('8208').''Coronavirus and Covid''.chr('8208').''19 Therapeutics. ChemMedChem. Accepted Author Manuscript. doi: 10.1002/cmdc.202000223
NEWS ABOUT THE UPCOMING EFMC EVENTS
Due to the extraordinary circumstances created by the coronavirus pandemic, the EFMC has taken the decision to postpone the XXVI EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2020) & 7th EFMC Young Medicinal Chemist Symposium (EFMC-YMCS 2020) by one year and launch a series of virtual events in the following months.
- EFMC-ISMC will take place in Basel on August 29 - September 2, 2021
- EFMC-YMCS will take place in Basel on September 2-3, 2021
We made this decision because the health and safety of all of our participants remains our primary concern, and because many scientists might not feel comfortable to participate in person.
But because we feel it is important to still be able to connect and share our sciences with each other, we will hold a series of virtual.
- A virtual EFMC-ISMC, EFMC-YMCS & online poster session will take place on Sept 7-11, 2020
In addition to this, the Young Scientist Network (EFMC-YSN) will hold a series of monthly webinars, free and open to all, which will mix science, soft-skills trainings and round table discussions. The first event of the series is scheduled for the second half of May.
More information will follow soon, so stay tuned on www.efmc.info and our various social media.
EFMC AWARDS & PRIZES
The EFMC is happy to announce the names of the 2020 Award & Prize winners.
Prof. Adriaan Ijzerman (Leiden University, The Netherlands)
For his leading contributions as a pioneer of GPCR drug discovery and structural biology, and his support of the medicinal chemistry and chemical biology community. His research led to over 450 publications, many of them achieving high international visibility. An excellent mentor and lecturer, Ad IJzerman played an active role in the International LACDR School on Medicinal Chemistry. He also chaired the medicinal chemistry division of the Royal Netherlands Chemical Society, organized many scientific symposia, and led several international research networks.
Dr Malin Lemurell (AstraZeneca, Sweden)
For her contribution to the discovery and development of several drug candidates and her leadership in medicinal chemistry. Her most recent contributions while leading a 60-strong medicinal chemistry group at AstraZeneca to deliver on pipeline projects in the Cardiovascular, Renal and Metabolism disease area across multiple modalities also includes harnessing innovation in the fields of RNA targeting with small molecules, RNA imaging with fluorescent nucleotide probes, machine learning applications in drug discovery projects and new modalities.
Prof. Gisbert Schneider (ETH Zürich, Switzerland)
For his pioneering work integrating machine learning into medicinal chemistry, drug discovery and chemical biology. His contributions spread across the whole drug discovery process, and introduced visionary concepts for concrete applications of computational methods. These are now broadly adopted in drug discovery and recognized as robust foundations for transformative advancements in the field.
All 3 awards consist of a diploma, € 7.500 and an invitation to give a headline presentation at the EFMC International Symposium on Medicinal Chemistry.
The selection committee designated Prof. Yimon Aye (EPFL, Switzerland) as the winner of the 2020 EFMC Prize for a Young Medicinal Chemist in Academia. Prof. Andrea Ablasser (EPFL, Switzerland) and Dr Christoph Rademacher (MPICI, Germany) have been recognised as the most meritorious runners-up.
The selection committee designated Dr Giuseppe Cecere (F. Hoffmann-La-Roche, Switzerland) as the winner of the 2020 EFMC Prize for a Young Medicinal Chemist in Industry. Dr Julien Lefranc (Bayer, Germany) and Dr Anneli Nordqvist (AstraZeneca, Sweden) have been recognised as the most meritorious runners-up.
The two prizes are given annually and consists of a diploma, € 1.000 and an invitation to give a short presentation at an EFMC symposium.
The selection committee designated Dr Victor Sebastian Perez (CSIC, Spain) as the winner of the 2020 EFMC-YSN PhD Prize. Mrs Marta Serafini (Università del Piemonte Orientale, Italy) is the most meritorious runner-up.
The Prize will constist of a diploma, a free registration and a 500€ travel grant to attend an EFMC Symposium.
RESULTS OF THE 2ND EFMC QUIZ & NEW QUIZ ANNOUNCED!
Congratulations to Jack Roberts (United Kingdom), Matjaz Brvar (Germany) & Kristina Pavic (Croatia) for winning the 2nd EFMC Quiz with 19 correct answers out of 20!
A third and final quiz is already out! Test your knowledge and try your luck winning an EFMC Goodiebox.
The deadline is May 31, 2020
Take the Quiz!
GET TO KNOW CAROLINA VINAGREIRO, UNIVERSITY OF COIMBRA, PORTUGAL
How did you get interested in Medicinal Chemistry?
The knowledge of the importance of Medicinal Chemistry for Public Health and the challenges that numerous diseases currently offer, both in terms of their diagnosis and treatment, have caught my interest from the first steps in university education. In 2010, I entered the pioneer degree in Medicinal Chemistry at the University of Coimbra and subsequently the master. After that, the MedChemTrain, a unique PhD program designed to train the next generation of scientists to work at the interface between chemistry and biology at various stages of pre-clinical drug discovery was designed. Aiming this ambitious and competitive program I applied for a grant and I was selected. After the first year of classes in the faculty of pharmacy of the University of Lisbon, we dealt with the elimination of some candidates with worst results and the selection for a grant to develop the PhD project of the rest. And the adventure began!
Where and when did you obtain your PhD diploma?
I am currently finishing my PhD in Chemistry, in the field of Medicinal Chemistry. As a student of this multidisciplinary program, I have two supervisors from two different institutions - University of Coimbra and University of Lisbon (IMM). As part of my PhD project, I also collaborated with the University of São Paulo, Brazil and the Jagiellonian University, Poland. I will obtain the degree during March 2020.
What is the topic of your PhD project?
The development of new effective treatments for infectious diseases is one of the biggest challenges of Medicinal Chemistry. The worldwide emergence of multidrug-resistant bacteria is considered by the World Health Organization (WHO) one of the main causes of mortality by infectious diseases. According to WHO recommendations, an urgent investment in R&D is essential for the development of new antibacterial entities with alternative mechanisms of action, to avoid that around 10 million people will die annually worldwide by 2050. Given the relevance of this problem, the main goal of the work presented in my PhD project consisted of the design, synthesis, and development of new antimicrobial chemical entities with alternative action mechanisms, in order to give a valuable contribution for the overcoming of this challenge.
What do you like most in your job?
Doing research, we are constantly challenged, something new and different happens every day and you need to deal with this, think and find different solutions. You also have time to invest in your personal growth. In my case, during these years, I participated in several courses and competitions.
Hard working, perseverance, self-motivation, creativity and grit are crucial. When you are doing something new, its normal to be faced with frustration and bad results! Generally, the good results do not appear at the first try! We must deal with that and find ways to overcome problems and have new ideas. Additionally, some improvising capacity is also needed!
What do you consider your biggest achievement in your scientific career?
I am just started my way, so I hope that my biggest achievement is still to come. At this moment, I considered my biggest achievement was the excellent results obtained against multidrug-resistant bacterial strains collected from patients from the Coimbra Hospital Center and biofilms. The designed meso-imidazolyl porphyrins of small size with positive charges surrounding the macrocycle enabled the inactivation of bacteria in biofilms by 6.9 log units at 5 nM photosensitizer concentration and an irradiation with 5 J cm−2. This was an unprecedent result and lead to a patent application and subsequently publication of the results.
What is the most embarrassing thing you did in the lab?
During these years of investigation, I watched to several situations in the lab. Vacuum pumps failing and balloons falling into the rotary evaporator baths, floods resulting from pipe rupture, a colleague got burned with a reagent etc. but the worst situation for me was an explosion of a fridge where I lost several compounds. Fortunately, there was only one guy in the lab and nobody got hurt.
Which scientist do you admire the most and why?
This is the most difficult question! Several scientists are doing very important work and contribute every day. I had the opportunity to know many scientists who I admired and inspired me. However, this time my words goes to young’s scientist, like me, that face lack of opportunities in science. Do your best every day and do not give up, an opportunity will appear sooner or later!
Which paper of yours you are the proudest of and why?
I would say it is the next one, because our focus is always do better in the next time!
But I am already proud of my last one. This is a compilation of the best results obtained in my project against multi-drug resistant bacteria and biofilms. The results are very good, without precedents. It is available on: https://dx.doi.org/10.1021/acsinfecdis.9b00379.
Which field of medicinal chemistry do you consider the most promising in the future?
I think the future of medicinal chemistry will pass through the deep teamwork between computational and medicinal chemistries. This will allow to save a reasonable quantity of money and perform a synthesis more conscient, which will reinforce the investment of pharmaceutical companies on R&D. On the other hand, the personalized medicine will also have their place in the future of medicinal chemistry.
What would you guess to be the next major breakthrough in medicinal chemistry?
I guess acquired drug-resistance is one of the biggest challenges in medicinal chemistry. Development of new therapeutics and novel drugs that can overcome the drug-resistance can be the key to a breakthrough in medicinal chemistry.
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS Committee has taken the decision to cancel the following meetings in which it is part of the organising team. We would hope to transpose meetings to the equivalent or similar dates in 2021 assuming that the situation stabilises.
A list of those symposia affected is given below - for more information please go to either of the following websites:
9th RSC / SCI Kinase Inhibitor Design
8th to 9th June 2020, The Francis Crick Institute, London, UK
BMCS Mastering MedChem VI
12th June 2020, Newcastle University, Newcastle-upon-Tyne, UK
8th RSC / SCI symposiums on GPCRs in Medicinal Chemistry
21st to 23rd September 2020, Evotec, Verona, Italy
MALCOLM CAMPBELL MEMORIAL PRIZE 2021
To continue the commemoration of his outstanding contributions in a broad range of chemistry and their application to the understanding of bioactivity, the Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is proud to invite nominations for the ninth Malcolm Campbell Memorial Prize. The prize will be awarded to the individual or team based in UK academia or industry who, in the judgement of the BMCS committee, has made the most significant scientific contribution to biological chemistry. Nominations could be from either discovery and/or process development and include medicinal, agrochemical or aromachemical research. The work should be timely and contemporaneous. A medal and certificate will be awarded to accompany the prize of £2,000
Nominations should be submitted no later than 31st October 2020 to:
Maggi Churchouse, RSC-BMCS Secretariat, e-mail: firstname.lastname@example.org
For further details, please access the activities link on www.rsc.org/bmcs
RSC-BMCS HALL OF FAME AND MEDAL 2019 ANNOUNCEMENT OF WINNER
The BMCS is delighted to announce that Sir Simon Campbell CBE FRS FMedSci will be the 2019 inductee to its Hall of Fame, and the recipient of the associated medal.
Sir Simon has made notable and long-standing contributions to the pharmaceutical industry and to the wider chemistry community in the UK with many significant scientific achievements. At Pfizer, he was a key member of the research teams that discovered Cardura, Norvasc (Istin) and Viagra which all became "best in class" with respect to therapeutic profile and commercial success. He has co-authored over 120 publications and patents and has received various national and international awards including the RSC BMCS Lifetime Achievement Award in 2016. Sir Simon served as President of the RSC 2004-06, and was appointed CBE for Services to Science in 2006 followed by a Knighthood for Services to Chemistry in 2015. His current scientific activities are largely focused on drug discovery for neglected diseases including malaria and TB.
The purpose of this award is to recognize prominent chemists for outstanding, sustained, and significant scientific impact, or contributions to any area of interest to the BMCS, e.g. medicinal chemistry, agriscience, bioorganic chemistry, chemical biology.
The formal medal presentation will be made on an occasion yet to be announced.
RSC-BMCS HALL OF FAME AND MEDAL 2020 CALL FOR NOMINATIONS
The BMCS is pleased to announce the 2020 call for nominations for its Hall of Fame and associated medal which recognises chemists for outstanding, sustained, significant contributions to any area of interest to the BMCS including medicinal chemistry, agriscience, bio-organic chemistry, and chemical biology.
Independent nominations may be submitted by e-mail outlining the justification and including the nominee’s CV and publication list. Additional independent letters of support to reinforce the nomination are strongly encouraged. Nominees should be resident in the UK or continental Europe, or have spent a considerable proportion of their career there. There is no requirement to be an RSC or BMCS member. There are no age restrictions, and nominees may have an academic or industrial background.
Nominations should be submitted by the end of September 2020 and the outcome will be communicated to nominators and nominees by mid-December 2020. Inductees will receive a medal and certificate, and will be invited to give a plenary lecture at an appropriate BMCS organized conference.
For further details, see the full list of requirements and terms and conditions on the RSC website below. Independent nominations should be sent by e-mail to email@example.com by 30th September 2020
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EFMC ORGANISED EVENTS
September 6-10, 2020 Postponed to August 29-September 2, 2021
EFMC-ISMC 2020: XXVI EFMC International Symposium on Medicinal Chemistry
September 10-11, 2020 Postponed to September 2-3, 2021
EFMC-YMCS 2020: 7th EFMC Young Medicinal Chemist Symposium
October 18-21, 2020
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry: New Opportunities in GPCR Drug Discovery
EFMC SPONSORED EVENTS
March 23-24, 2020 Postponed to October 26-27, 2020
Eindhoven, The Netherlands
A Joint Future for Medicinal Chemistry and Chemical Biology in the Netherlands
May 7-9, 2020 Postponed to November 5-7, 2020
18th Hellenic Symposium on Medicinal Chemistry (HSMC-18)
July 1-3, 2020 Postponed to July 7-9, 2021
RICT 2020: Interfacing Chemical Biology and Drug Discovery
EFMC SPONSORED SCHOOL
October 4-9, 2020
14th Swiss Course on Medicinal Chemistry