IN MEMORIAM BERNARD TESTA (1941-2022)
It was with great sadness that we learnt of the death of Prof. Bernard Testa, recipient of the 2002 Nauta Award for Pharmacochemistry and speaker at the first EFMC Short Course in Medicinal Chemistry.
He was highly considered by the community for his numerous and excellent contributions to the advancement of pharmaceutical sciences and medicinal chemistry, both as teacher and as researcher. His achievements in understanding the role of physiochemical properties in drug activity, more precisely in the disposition of medicines ought to be particularly recognised.
EFMC would like to remind his efforts, joint with Henk Timmerman and Han van de Waterbeemd, to launch the successful series of EFMC Short Course in Medicinal Chemistry in 2009 with a very successful course on “Improving Compound Quality: Physical Chemistry and DMPK Properties in Drug Discovery. Principles, Assays and Predictions”.
EFMC regrets the loss of this contributor to its history, and presents its condolences to his family.
XXVII EFMC INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY (EFMC-ISMC 2022) – SHORT REPORT
The 27th edition of the EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC) took place on September 4-8th, 2022 in Nice, France.
More than 1000 scientists from all over the globe gathered to listen to the cutting-edge science presented by the 76 invited speakers, 44 Oral Communications and 384 poster presenters over the five days of the conference.
The opening ceremony was chaired by the EFMC President, Prof. Rui Moreira (University of Lisbon, Portugal), the Symposium Chair, Dr Luc Van Hijfte (Symeres, The Netherlands) and the President of the “Société de Chimie Thérapeutique”, Prof. Rebecca Deprez-Poulain (University of Lille/Institut Pasteur of Lille, France). Hosted at the Nice Acropolis Convention Center, it provided an ideal stage to host the various Awards ceremonies and the EFMC Honorary Fellows ceremony.
The patient testimonial, chaired by Dr Tatjana Ross (Merck, Germany) was a vibrant reminder of the importance of medicinal chemistry and chemical biology, and its impact on healthcare - setting the tone for an inspiring meeting. Prof. Herbert Waldmann (Max Planck Institute of Molecular Physiology, Germany), winner of the Nauta Pharmacochemistry Award for Medicinal Chemistry and Chemical Biology, delivered a lecture on “Pseudo Natural Products – Chemical Evolution of Natural Product Structure”. Dr Raphaël Rodriguez (Institut Curie, France), winner of the Klaus Grohe Prize, followed by a talk entitled “Discovery of a Druggable Copper-signaling Pathway that Drives Cell Plasticity and Inflammation”. Several musical interludes by a traditional dance group of Nice punctuated the lectures.
In the following four days, the participants attended a busy programme of 2 award lectures, 4 plenary lectures, 6 prize lectures, 25 themed sessions, two plenary first-time disclosures sessions, workshops, and poster sessions. Among the posters presented, ten were awarded an EFMC Best Poster Prize. Ten young scientists were also awarded a free subscription to the event by the EFMC.
Amongst many highlights of the programme were the award lectures by Prof. Mike Waring (Newcastle University, United Kingdom) and Prof. Alessio Ciulli (University of Dundee, United Kingdom), plenary lectures by Prof. Benoit Deprez (Institut Pasteur of Lille, France), Prof. Erik Miska (University of Cambridge, United Kingdom), Prof. Sarah E. Reisman (California Institute of Technologies, United States), and the 2022 IUPAC-Richter Prize Lecture by Prof. Michael E. Jung (UCLA Chemistry & Biochemistry, United States). The closing lecture was delivered by Dr Outi Vaarala (Orion Corporation, Finland).
Several networking opportunities were offered, and the exhibition gathered 56 exhibitors, to whom we are thankful for their support. To conclude the event in style, a conference dinner was hosted in the beautiful “Palais de la Mediterannée” – an Art Déco landmark on the famous Promenade des Anglais.
We would like to thank again all our committee members, speakers, sponsors, exhibitors, and of course participants for their support – and we look forward to warmly meeting you all in the “Eternal City” for the XXVIII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2024), which will take place on September 1-5, 2024 in Rome, Italy.
EFMC AWARD & HONORARY FELLOWS CEREMONIES
Hosted at the occasion of 27th edition of the EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC) which took place on September 4-8, 2022 in Nice, France, the EFMC Award & Honorary Fellow ceremonies were the occasion to thank the individuals who have provided outstanding support to the EFMC or contributed to strengthening the position of medicinal chemistry, chemical biology, or related fields in Europe.
Prof. Herbert Waldmann (Max Planck Institute of Molecular Physiology, Germany) received the Nauta Pharmacochemistry Award for Medicinal Chemistry and Chemical Biology 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. He has helped foster Europe’s scientific community through many partnerships across academia and industry and through his numerous scientific offspring.
Prof. Henk Timmerman, Dr Andele Nauta, Prof. Herbart Waldmann, Prof. Rui Moreira
Credits: Fabien Venturi
Prof. Mike Waring (Newcastle University, United Kingdom) received the UCB-Ehrlich Award for Excellence in Medicinal Chemistry for his conceptual work on the role of lipophilicity and for contributions to advancing the field of covalent inhibitors in medicinal chemistry. Mike Waring has been involved in drug discovery and development projects that have 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.
Dr Adrian Hall, Prof. Mike Waring, Prof. Rui Moreira
Credits: Fabien Venturi
Prof. Alessio Ciulli (University of Dundee, United Kingdom) received the Prous Institute - Overton and Meyer Award for New Technologies in Drug Discovery 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.
Dr Josep Prous, Prof. Alessio Ciulli, Prof. Rui Moreira
Credits: Fabien Venturi
The life-long title of Honorary Fellows was given to
- Dr Dave Alker for his active role within the various leading boards of the EFMC, and his extraordinary commitment to the support of the EFMC Young Medicinal Chemists’ Symposium (EFMC-YMCS). Dr Alker has been an active member of the Executive Committee, Council, and Industry Liaison committee - increasing the visibility of EFMC activities within companies which employ medicinal chemists as well as those related industries for whom medicinal chemistry is an enabling science or for whom medicinal chemists represent a significant customer base. Dr Dave Alker has significantly contributed to the Biological and Medicinal Chemistry Sector (BMCS) of the Royal Society of Chemistry (RSC) and helped in disseminating the news and activities of the EFMC to the United Kingdom communities of Medicinal Chemists and Chemical Biologists and is regarded as a strong link between his national adhering organisation and the EFMC.
- Prof. Gabriele Costantino has been a member of the Executive Committee of the EFMC from 2011 until 2014, before joining the Council of the EFMC from 2017 until 2019, and from 2021 until the present days. He strongly collaborated in the creation of the EFMC newsletter “MedChem(Bio)Watch” and acted as editor-in-chief for almost a decade. With its high-quality content composed of editorials, perspective articles and reports of EFMC events and activities, the newsletter greatly helped disseminating the EFMC brand to the scientific community – and contributed to strengthening the position of medicinal chemistry, chemical biology, and related fields in Europe. In addition, Prof. Costantino has significantly contributed to the Division of Medicinal Chemistry of the Italian Chemical Society and worked as powerful ambassador between the Italian community and the EFMC.
- Dr Kristina Goncharenko for her active participation in the creation of the EFMC Young Scientists Network. She was one of the driving forces behind in this endevour in 2019 and subsequently as chair. Her vision and sense of leadership has immensely contributed to the success of the network. Dr Goncharenko also supported the EFMC within the communication team, helping to resent our Federation to the new generation via an improved presence on social media and various branding activities such as the interviews and photo competitions. In addition, Kristina Goncharenko has contributed to the Division for Medicinal Chemistry & Chemical Biology of the Swiss Chemical Society and worked at spreading the visibility of our Federation within the Swiss community.
- Dr Peter Mohr has made substantial contributions in a wide range of medicinal chemistry areas, building on an outstanding level of scientific achievement in his career, in particular in the design of chemical probes for the unravelling of biological processes as well as in the development of several first-in-class candidates. Dr Mohr has expanded the knowledge and expertise in several important disease areas such as oncology, dermatology, psoriasis, and Type II diabetes. As well as his scientific achievements, Dr Peter Mohr has contributed significantly to the Swiss Chemical Society and to the EFMC in quality of Council Member for more than 8 years as well as active members of various EFMC initiatives and working groups until today.
Dr Luc Van Hijfte, Dr Peter Mohr, Dr Kristina Goncharenko, Prof. Gabriele Costantino, Prof. Rui Moreira
Credits: Fabien Venturi
EFMC-YSN PhD PRIZES, BEST POSTER PRIZES & ROCHE STUDENTSHIPS
Because recognising excellence and merits is important, the new generation was also celebrated during the 27th edition of the EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC).
Due to the coronavirus pandemic, the EFMC-YSN PhD Prize ceremony gathered the winners and runners-up of the 3 preceding editions.
- 2020: Dr Victor Sebastian Perez (Exscientia, United Kingdom)
- 2021: Dr Nikolaj Sten Troelsen (Amgen Research, Denmark)
- 2022: Dr Johannes Morstein (University of California, United States) who unfortunately could not be present & the two runners-up: Ms Vanesa Nozal Garcia (CIB - CISC, Spain) and Ms Eleonora Comeo (University of Nottingham, United Kingdom)
Prof. Rui Moreira, Ms Vanesa Nozal Garcia, Dr Nikolaj Sten Troelsen, Dr Victor Sebastian Perez, Ms Eleonora Comeo
The EFMC Best Poster Prizes have been granted to the following participants :
- Ben Cons (Astex)
- Blake Curtis (Australian National University)
- Evelyne Dietrich (Repare Therapeutics)
- Sandra Kovachka (Côte D’azur University)
- Caroline Lanthier (UAntwerp)
- Angela Martin Serrano Ortiz (University of Grenoble-Alpes)
- Pilar Suarez De Cepeda Fuentes (University of Santiago de Compostela)
- Julian Witt (University of Hamburg)
The EFMC-ICBS Best Poster Prizes have been granted to the following participants :
- Carlo Matera (University of Milan)
- Doroteja Novak (University of Ljubljana)
Credits: Fabien Venturi
Finally, the 2022 EFMC-Roche Studentships, hosted by Dr Hayley Binch (F. Hoffmann-La Roche, Switzerland) rewarded excellence accomplished during a medicinal chemistry internship in industry have been granted to the following participants:
- Mr Adam McGrath (Imperial College London)
- Mr Sander Folker (F.Hoffmann-La Roche)
- Ms Hannah Unsworth (University of Oxford)
Credits: Fabien Venturi
9TH EFMC YOUNG MEDICINAL CHEMISTS' SYMPOSIUM (EFMC-YMCS 2022) – SHORT REPORT
Following the EFMC-ISMC 2022 and taking place in the beautiful scenery of the Villa Arson, and Art centre located in the hills of Nice overlooking the bay, the 9th EFMC Young Medicinal Chemists' Symposium was this time again the cradle of lively exchanges and interactions for the early career researchers.
185 researchers gathered to listen to the two inspiring keynote lectures, 19 oral communications by invited prize winners from national young medicinal chemist meetings in Europe and 19 Flash Poster Presentations over the one and half day conference.
The opening ceremony was chaired by the EFMC President, Prof. Rui Moreira (University of Lisbon, Portugal) and the Symposium Chair, Dr Maria Duca (Côte d’Azur University, France) and immediately followed by the opening lecture by Prof. Benoit Deprez (Institut Pasteur of Lille, France), entitled "All Models are Wrong, Some are Useful:.The Medicinal Chemist is Never Better than the Biological Models Available to Assess Compound Properties”
The participants then attended a busy programme of oral communications, flash poster presentations and two posters’ sessions gathering a little over 100 posters. The closing lecture was given by Dr Gerhard Müller (Anavo Therapeutic, Germany), entitled “Medicinal Chemistry Today: Be Prepared for the Unexpected!”
The award ceremony recognised the following champions:
Ms Floriane Eshak (University Paris Cité, France) received the EFMC-YMCS Presentation Prize for her presentation on the "Epitope Identification, a Case Study: Nanobodies Binding to MGLU5 Receptor".
Dr Margarida Espadinha (University of Antwerp, Belgium) was awarded the EFMC-YMCS Public's Choice Prize for her presentation on "Design, Synthesis and Biological Evaluation of Novel P53 Activators by Targeting P53 Protein-Protein Interactions".
The three EFMC-YMCS Best Poster Prizes, sponsored by Chemistry Europe have been offered to:
- Poster 031: Giulia Assoni (University of Trento, Italy)
- Poster 062: Beatrice Chiew (University of Newcastle, Australia)
- Poster 095: Louna Mossino Diaz (Université Paris Cité, France)
Finally, the bravest of the attendees stayed for the very interesting optional programme hosted by the EFMC Young Scientists Network and composed of a workshop by Reaxys, given by Giulia Moncelsi and a lecture on Effective Communication and Networking for Scientists, given by David Peralta.
We would like to thank again all our committee members, speakers, sponsors, exhibitors, and of course participants for their support – and we look forward to warmly meeting you all in Zagreb, Croatia to celebrate the 10th anniversary of the EFMC Young Medicinal Chemists' Symposium. EFMC-YMCS 2023 will take place on September 7-8, 2023.
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 contribution will focus on the recently published article on Machine Learning Guided Discovery of Non-Hemolytic Membrane Disruptive Anticancer Peptides, published in ChemMedChem, the official journal of the EFMC.
First example of direct machine learning guided discovery of non-hemolytic Anticancer Peptides:
Computational chemistry is a leading area that is contributing for accelerating the discovery of new entities. Machine learning (ML) methods can provide a deep insight into chemical processes that goes beyond experimental measurements. Anticancer peptides (ACPs) fold into membrane-disruptive cationic amphiphilic α-helices, many of them unpredictably hemolytic and toxic. ML classifiers trained with sequence activity data can distinguish active from inactive and hemolytic from non-hemolytic peptides with good performance.
In this article, two ML approaches were used to discover new non-hemolytic membrane disruptive ACPs: recurrent neural networks (RNN) and Peptide Design Genetic Algorithm (PDGA). The sequences of ACPs were selected based on their novelty and their predicted α-helicity and amphiphilicity to favor the membrane disruptive mechanism of action. The peptides were synthetized and tested. Eleven active ACPs were found,four of which were classified as non-hemolytic. The authors envision that iterative rounds of ML-guided design might allow expansion of the set of non-hemolytic ACPs and lead to better understand of activity and selectivity of the class.
Read the article.
E. Zakharova, M. Orsi, A. Capecchi, J.-L. Reymond, ChemMedChem 2022, 17, e202200291
13th EFMC-YSN MEDCHEMBIOONLINE – OCTOBER 18
Now that the summer break is over, the EFMC Young Scientists Network is back with its series of webinars mixing science, soft-skills trainings, and round table discussions.
The upcoming edition, scheduled for October 18 between 17:00 and 19:15 CEST, is organised in collaboration with the EFMC Chemical Biology Initiative and will carry the thematic of “Chemical Biology as a Bridge Between Industry and Academia”.
The programme of the webinar will be as follow:
- Explorations in Chemical Biology
Prof. Boris Vauzeilles (Institut de Chimie des Substances Naturelles, France)
- Precision Chemistry applied to Chemical Biology Tools
Dr Luc Van Hijfte (Symeres, The Netherlands)
- Cross-Fertilization of Industrial Drug Discovery and Academic Research – Examples from the Discovery of Cannabinoid Receptor Type 2 Agonist RG7774
Dr Uwe Grether (F. Hoffmann-La Roche, Switzerland)
- Round Table Discussion "The Career stories of our speakers"
Registration to the event is free and open to all thanks to the generous support of Symeres.
BEST PRACTICES IN VALIDATING CHEMICAL PROBES
What are chemical probes and why are they important? Chemical probes are designed to selectively address a biological question; this is distinctly different from a drug, which is designed to produce a clinical outcome! Simple guidelines can be used to generate high-quality chemical probes and obtain reliable data to further our understanding of human biology and disease.
If you have missed the excellent webinars and slide decks by the EFMC Best Practices working group, you can still access them on www.efmc.info/validating-chemical-probes.
11TH ANNUAL CONFERENCE OF THE INTERNATIONAL CHEMICAL BIOLOGY SOCIETY (ICBS2022)
We are pleased to announce that the 11th annual conference of the International Chemical Biology Society (ICBS) will take place this December 4-7 in Brisbane, Australia. The conference will carry the broader theme of “Uncovering solutions for diseases” with a focus on academic and industrial applications of chemical biology to both fundamental and translational research.
The EFMC will host a session on “Enabling Chemical Biology with Medicinal Chemistry” and is inviting you all to join us in fostering collaborations and partnership to advance chemical biology and promote the career development of young chemical biologists.
The EFMC session on “Enabling Chemical Biology with Medicinal Chemistry”, chaired by Dr Yves P. Auberson, will take place on December 6 morning and we are happy to welcome Dr David Fairlie (University of Queensland, Australia) as our first keynote lecturer. He will deliver a very exciting lecture on chemical modulators of MAIT cells. Our second keynote lecturer will be Dr Andrea Vernall (Otago University, New Zealand).
Our third lecturer will be selected from submitted abstract, so we invite you all to take the opportunity of the extended abstract submission deadline to share your work through an oral communication at the ICBS2022.
GET TO KNOW ANNA VULPETTI, NOVARTIS, SWITZERLAND
In this edition, our #Iamamedicinalchemist is Anna Vulpetti from Novartis, Switzerland.
Get to know her better by reading our interview below.
How did you get interested in Medicinal Chemistry?
Medicinal chemistry attracted my interest because it is a discipline that integrates different expertises ranging from computational design and synthetic organic chemistry to biophysical and biological evaluation.
What was the topic of your PhD project?
I received my Ph.D. degree in Chemistry from the University of Milan, under the supervision of Prof. C. Gennari, working on the rational design of highly stereoselective boron enolates using transition-state computer modeling. The developed reagent was subsequently used to synthesize Taxol and Taxotere. Both synthetic chemistry and quantum mechanical calculations were performed during my studies.
Where are you currently working and what is your current position?
In 1995, I joined Pharmacia & Upjohn, later Pfizer, and in 2006 I moved to Novartis, where I support drug discovery projects in various therapeutic areas, from early target assessment to lead optimisation.
What are your current research interests?
My research interests include ligand-based Fluorine NMR screening in drug discovery, the investigation of the role of fluorine in drug design, the development of novel methods for describing and comparing either fluorinated molecules or protein binding sites.
How would you explain your research area to non-scientists?
My aim is to improve the efficiency of drug discovery by helping to design compounds that have a high probability of binding to the target of interest with the right molecular and physical properties to ultimately demonstrate good bioavailability and be beneficial to patients.
What do you like best about your work?
The possibility to work in multidisciplinary teams on various challenges. I like working in different disease areas with different protein families and different modalities.
What kind of skills does your work require?
Creativity with scientific rigor. Broad knowledge of all disciplines involved in drug discovery. Good communication skills and self-motivation.
What do you consider your greatest achievement in your scientific career?
Contribution to the development of drugs that have reached the clinic.
Which of your papers are you most proud of and why?
The perspective published in J. Med. Chem. (2019), 62, 2218-2224 nicely summarizes the synergy of working at the interface of different disciplines.
What would you like to ask from other medicinal chemists?
Desire to learn and apply learnings together. Motivate each other’s with constructive feedback, cooperation and mutual respect. Recognize that great science is not a one person or one discipline effort.
Which scientist do you admire the most and why?
Curious scientists with humble attitude, but with strong commitment, broad and in depth understanding of different scientific fields.
What would you expect to be the next major breakthrough in medicinal chemistry?
Ability to combine precise atomic design with big-data-driven approaches. Design methods will heavily rely on artificial intelligence and advanced computational methods such as quantum chemistry.
#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 October 26 by Dr Kai Schiemann (Merck KGaA).
The topic of the webinar will be “Discovery of M1069, a highly selective dual inhibitor of adenosine A2a/A2b receptors”
While the A2A adenosine receptor has been considered a major contributor to adenosine mediated tumor immunosuppression, the A2B receptor has recently emerged as another potential therapeutic target. Considering the importance of both targets, we developed M1069 as a selective dual antagonist of the A2A and A2B adenosine receptors to counteract the immunosuppressive effects of adenosine signaling and stimulate anti-tumor immune responses in patients with advanced malignancies.
M1069 was discovered through the medicinal chemistry optimization of a thiazolo[4,5-c]pyridin-2-amine scaffold. The binding mode was confirmed by X-ray structure analysis of close derivatives of M1069 in a complex with the A2A receptor domain. Initial cellular optimization resulted in a very high A2AR potency and a low potency for A2BR. Homology models of the A2BR, along with docking into the published A1R, supported further optimization. Increasing the potency on A2BR was a major challenge, which required some fine-tuning of the substituents, while keeping a high split ratio to the A1R, which was defined as an exclusion criterion to avoid unwanted side-effects. Finally, potent dual and selective A2A/A2B antagonists were further profiled. Surprisingly, some of these showed species’ differences in human and murine T cells, as well as myeloid cells at high (10 µM) NECA (stable analog of adenosine) concentrations and needed to be excluded from the evaluation of in vivo pharmacology using murine tumor models. In contrast, M1069 demonstrated dual A2A and A2B antagonist activity in assays with both human and murine immune cells, favorable physchem/ADME properties, good PK in various species and predicted minimal brain penetration in humans.
Preclinically, M1069 has demonstrated superior activity in comparison to A2A-selective reference antagonists in high (10uM) NECA/adenosine settings in vitro, which translated into superior anti-tumor activity for M1069 in vivo in the 4T1 tumor model. In addition, M1069 showed combination activity with the chemotherapeutic agents’ cisplatin and paclitaxel in the 4T1 tumor model. These preclinical data are consistent with a primary mechanism of action of M1069 that involves the reversal of immune suppression via dual antagonism of pro-tumorigenic A2A and A2B adenosine receptors in an adenosine rich TME, where A2B could act complementary, or compensatory to A2A. Together, this data suggests higher potential for dual A2A/A2B antagonism of M1069 compared to A2A antagonism to block the immune-suppressive/pro-tumorigenic impact of adenosine.
M1069 is currently being evaluated as a monotherapy in a Phase I, first-in-human clinical trial in patients with advanced solid tumors (NCT05198349).
Register for free here: https://us06web.zoom.us/webinar/register/WN_FcNEiMiqTB-R0wZiMdoCIw
#GDCh (MedChem Division), #NextGenMedChem
EFMC SPONSORED EVENT REPORT: 3RD MOLECULES MEDICINAL CHEMISTRY SYMPOSIUM (MMCS): SHAPING MEDICINAL CHEMISTRY FOR THE NEW DECADE
It is with great pleasure that we officially close the 3rd Molecules Medicinal Chemistry Symposium—Shaping Medicinal Chemistry for the New Decade (MMCS2022), which was held in Rome, from 2729 July 2022.
We received more than 150 submissions from which we accepted 104. The program for the 3 day-event was composed of 12 keynotes speakers and 38 selected talks. The rest of excellent submissions were divided in two poster sessions, held during the lunch breaks. With more than 140 attendants from 41 countries, we celebrated a fruitful and exciting conference covering particularly challenging diseases, novel and revisited drug discovery approaches, and medicinal chemistry stories about recently implemented projects.
Thank you to our chairs, committee members, speakers, sponsors, and all the attendees for making such a great meeting!
EFMC SPONSORED EVENT REPORT: 27th NATIONAL MEETING ON MEDICINAL CHEMISTRY (NMMC27)
The XXVII edition of the National Meeting on Medicinal Chemistry (NMMC27), joint with the 14th Young Medicinal Chemists’ Symposium “New perspectives in Medicinal Chemistry” (NPCF14), organised by the Medicinal Chemistry Division of the Italian Chemical Society, in collaboration with the Department of Pharmacy & Pharmaceutical Sciences of the University of Bari Aldo Moro, has been held in Bari (Italy) in September 11-14, 2022.
About 300 delegates from academia and industry (more than fifty under-35 young people, about twenty from other European countries) attended the meeting, with 5 plenary lectures of European leading scientists, 5 parallel sessions with 10keynotes, 50 oral/flash communications and 120 poster presentations, has covered the advances in drug discovery in major therapeutic areas, including the treatment of bacterial and viral infections, with a focus to the emerging COVID-19 pandemics, but also neurodegenerative and cardiovascular diseases, cancer, and rare diseases.
From September 11 to 14, 2022, the University of Bari Aldo Moro hosted the 27th edition of the Italian National Meeting on Medicinal Chemistry (NMMC27), joint with the 14th Young Medicinal Chemists’ Symposium “New perspectives in Medicinal Chemistry” (NPCF14), which was the first face-to-face meeting after two years of virtual conferences.
About 300 delegates from academia and industry, including many under-35 young people even coming from other European countries, attended the meeting. On the first day, the scientific committee awarded Prof. Gabriele Costantino (University of Parma) with the Musajo Medal of the Medicinal Chemistry Division, Dr. Francesco Merlino (University of Naples Federico II) and Laura Scalvini (University of Parma) with the Division of Medicinal Chemistry Young Scientist awards. Two best doctoral thesis awards were assigned to Marco Maspero (University of Milan), for a thesis on “Design and synthesis of new PET radiotracers in drug discovery”, and to Filippo Basagni (University of Bologna), for a thesis on “Design and synthesis of (pro)electrophilic compounds for investigating the multifactorial nature of neurodegenerative diseases: focus on inflammation-driven events”.
The opening lecture was given by pProfessor Jurgen Bajorath (University of Bonn, Germany), dealing with the role of Artificial Intelligence in drug discovery. In the following days, the plenary lectures were given by eminent European scientists: Oliver Kappe (Graz University), Maria Duca (Université Côte d'Azur Nice, France), Laura Heitman (Leiden University, The Netherlands), Vincenzo Summa (University of Naples Federico II, Italy). The meeting has covered advances in drug discovery in major therapeutic areas, including neurodegenerative and cardiovascular diseases, rare diseases, and cancer, and the treatment of bacterial and viral infections, with a particular focus on COVID-19 pandemics. The artificial intelligence and machine learning techniques as applied to drug discovery, the so-called “new modalities in medicinal chemistry” and the most recent advances in sustainable, chemical and biophysical technologies have been featured. More importantly, some initiatives of networking and public engagement, with a round table on Lafora rare disease, complemented the scientific sessions, where the participants had the opportunity to establish and strengthen collaborative networks, as is necessary for successful research.
The meeting was also the occasion to commemorate Professor Vincenzo Tortorella who passed away in July 2022. Professor Tortorella, besides being the Dean of the Faculty of Pharmacy of the University of Bari for more than 30 years, served as president of the Division of Medicinal Chemistry of the Italian Chemical Society and was a co-founder and previous chairman of the European Federation of Medicinal Chemistry.
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is delighted to announce the upcoming events.
- RSC-BMCS Targeted Protein Degradation: “Three’s a crowd?”
- 7th RSC-BMCS / SCI Symposium on Ion Channels as Therapeutic Targets
- 10th SCI/RSC Kinase Symposium on Inhibitor Design
RSC-BMCS Targeted Protein Degradation: “Three’s a crowd ?”
16th and 17th November 2022, Virtual
Delegate Registration and Exhibitor/Sponsor registration is now open
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)
7th RSC-BMCS / SCI Symposium on Ion Channels as Therapeutic Targets
27th and 28th March 2023, Wellcome Genome Campus, Cambridge
Closing date for poster abstracts is 31st December
Synopsis: Ion channels are important targets for therapeutic intervention due to their extensive roles in human physiology and the pathophysiology of disease. Many successful drugs targeting this gene family have been discovered for diseases such as hypertension, epilepsy and neuropathic pain.
This symposium, the 7th in an ongoing series, will showcase the most recent advances to aid the design of new ion channel therapeutics and promote interaction between scientists with a shared interest in the field of ion channel drug discovery.
10th SCI/RSC Kinase Symposium on Inhibitor Design
9thand 10th May 2023, SCI, London, UK
Abstract submissions are now open!
Synopsis: With more than 70 FDA-approved small molecules, the field of kinase inhibition continues to attract significant investment from the drug discovery and development community. The 10th SCI/RSC symposium on kinases will encompass plenary lectures on emergent topics and case studies of ongoing programmes as well as successful past programmes. A range of topics including new screening approaches, brain penetrant kinase inhibitors, induced protein degradation, allosteric inhibitors and kinase inhibition for immuno-oncology will be covered, along with views and perspectives on the future of kinase inhibitor research.
THIS NEWSLETTER IS KINDLY SPONSORED BY
Over the last two decades, traditional small molecules and antibody drugs have provided tremendous benefits to cancer patients. Due to the complexity of the disease, incomplete response and drug resistance ultimately emerge.
In this webinar, we will discuss the opportunity of new modalities for treating KRAS mutant cancers, as well as various modality toolboxes to support drug discovery programs.
ISSUE SPONSORED BY
"Every drug can be made and every disease can be treated."
EFMC ORGANISED EVENTS
April 23-26, 2023
Oegstgeest, The Netherlands
17th EFMC Short Course on Medicinal Chemistry
June 10-13, 2023
Boston, United States
ACSMEDI-EFMC Medicinal Chemistry Frontiers
September 3-7, 2023
IX International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC)
September 7-8, 2023
10th EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS)
November 16-18, 2023
EFMC International Symposium on Chemical Biology (EFMC-ISCB)
EFMC SPONSORED EVENTS
November 23-26, 2022
12th Joint Meeting on Medicinal Chemistry 2022
Various jobs opportunities, Sygnature Discovery, UNITED KINGDOM
Various jobs opportunities, Peak Proteins, Peak Proteins Macclesfield, UNITED KINGDOM
Postdoc in Chemical Biology, University of Geneva, Geneva, SWITZERLAND
Postdoctoral Research Fellow, The University of British Columbia, Vancouver, CANADA
PhD in Medicinal Chemistry, Institut de Chimie de Nice UMR7272 CNRS, Nice, FRANCE