EFMC-YMCS 2023 – PROGRAMME IS ANNOUNCED!
We are delighted to announce the Scientific Programme of EFMC-YMCS 2023! The programme promises a lineup of interesting research presentations, insightful discussions, and engaging poster sessions. Prepare to be inspired by the work of young medicinal chemists from around the globe!
In addition, the deadline for poster submissions has been extended until July 14 so do not miss the opportunity to showcase your research and compete for best poster prizes!
- The Facinating World of Drug Discovery
Dr Christoph BOSS (Idorsia, Switzerland)
- Druggability Beyond the Rule of Five
Dr Sanja KOSTRUN (Selvita, Croatia)
- Leveraging Natural Products to Afford New Therapeutic Leads That Can Target Resistant Tumors
Prof. Thomas POULSEN (Aarhus University, Denmark)
The programme will also include 18 oral communications by invited prize winners from national young medicinal chemist meetings in Europe, 2 Prize Lectures and 20 flash poster presentations selected from submitted abstracts.
More information & registration on www.efmc-ymcs.org.
EFMC-ISCB 2023 – ORAL COMMUNICATIONS ANNOUNCED!
The organising committee of the EFMC International Symposium on Chemical Biology (EFMC-ISCB 2023) selected the 8 oral communications who will complete the high-quality programme of 26 Plenary and Invited speakers.
- Spatiotemporally Controlled Generation of Ntps as A Versatile Tool for Single-Molecule Studies
Sebastian Deindl (Uppsala University, Uppsala, Sweden)
- Molecular Glues for the 14-3-3 Interactome
Richard Doveston (University of Leicester, Leicester, United Kingdom)
- The Hidden Activator Within the Inhibitor: Regulated Tissue-Selective Inhibition and Activation of the Sugar Tolerance Transcription Factor Chrebp
Maren Heimhalt (Ludwig Maximilian Universität, Planegg-Martinsried, Germany)
- Collectin-11 Antagonists in a Therapeutic Approach to Minimize Complement-Mediated Immune Injury
Rachel Hevey (University of Basel, Basel, Switzerland)
- Molecular Binding Studies in G Protein Coupled Receptors: Insights for Drug Discovery
Vittorio Limongelli (Università Della Svizzera Italiana USI, Lugano, Switzerland)
- Lessons for Covalent Drug Development from Deep Chemoproteomic Profiling of Approved Covalent Drugs
Micah Niphakis (Lundbeck, San Diego, CA, United States)
- Photocrot: A Precise Photo-Chemical Approach to Selectively Identify Crotonylated Proteins
Rita Petracca (Utrecht University, Utrecht, The Netherlands)
- Morphological Profiling of Small Molecules Using the Cell Painting Assay
Slava Ziegler (Max Planck Institute of Molecular Physiology, Dortmund, Germany)
Have a look at the full programme!
Want to share your research with a poster? The abstract submission is open until September 20!
2023 SYMERES PHD PRIZE FOR EXCELLENCE IN CHEMISTRY IN LIFE SCIENCES RESEARCH AWARDED
The competition was fierce between the 10 candidates who joined the second round of selection for the Symeres PhD Prize, hosted at the Symeres Facilities in Nijmegen on July 10-11, 2023.
The jury proudly announces the awardees:
- 1st Place: Jan Gabriel Felber, LMU Munich, Germany
- 2nd Place: Zhangping Xiao, Imperial College London, United Kingdom
- 3rd Place: Vanesa Nozal Garcia, University of Antwerp, Belgium
As per the regulations of the prize, the winner will be invited to deliver an oral communication at the 10th EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS).
The committee would also like to congratulate the other contestants, whose presentations were of a very high level, making the final selection difficult.
- Fabio Begnini, Aarhus University, Denmark
- Elena Detta, Aicuris Anti-Infective Cures AG, Germany
- Margarida Espadinha, University of Antwerp, Belgium
- Emma Grant, University of Strathclyde/GlaxoSmithKline, United Kingdom
- Ahmed Hazem, ETH Zurich, Switzerland
- Roberta Pacifico, University of Antwerp, Belgium
- Marta Serafini, Università Del Piemonte Orientale, Italy
Congratulations to all!
COURSE MATERIAL ON BEST PRACTICES IN MEDICINAL CHEMISTRY
Wonder how researchers work in other companies or in academia? Are there important trends or new technologies that you may have missed? Looking for general guidelines or tips and tricks on important topics in drug discovery?
EFMC is tackling this challenge with a team of experienced practitioners from industry and academia, and is sharing training and course materials in several formats: freely accessible webinars on the EFMC youtube channel, educational slide decks and case studies.
These are freely accessible for personal use or for use in further training or teaching material, so have a look and spread the news!
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.
Link to the material.
- Phenotypic Drug Discovery (PDD)
Recent years have seen a renaissance of Phenotypic drug discovery (PPD) with novel screening technologies and a track record that is thought to match or surpass that of target-centric approaches. We present a view on best practices to consider when running phenotypic drug discovery campaigns to increase the chance of success of these black box approachs.
Link to the material.
Hit Generation is a crucial step of all drug discovery campaigns that will determine the speed and chance of success of identifying drug candidates.
We cover the essential approaches for hit generation and the opportunities and challenges they come with. We then provide guidance on how to validate hits to ensure medicinal chemistry is only performed on compounds and scaffolds that engage the target of interest and have the desired mode of action. Finally, we discuss the design of integrated hit generation strategies that combine several approaches to maximize the chance of identifying high quality starting points.
Link to the material.
This contribution will focus on the recently published article on “Pan-KRAS inhibitor disables oncogenic signalling and tumour growth” by Kim et al. focusing on the development of a pan-KRAS inhibitor, which aims to target KRAS mutations, a common gain-of-function alteration found in cancer patients.
KRAS is a GTPase protein that switches between an active (GTP-bound) and an inactive (GDP-bound) state. The study focuses on non-G12C KRAS mutants that constitute the majority of KRAS alterations in cancer and are not effectively targeted by current therapies.
The researchers began by modifying an existing G12C-selective inhibitor to remove its covalent warhead, and improve its inhibitory activity against various KRAS mutants. The resulting compound, BI-2865, demonstrated potent inhibitory effects on the proliferation of cells expressing G12C, G12D, or G12V KRAS mutants. Importantly, BI-2865 showed similar efficacy to covalent G12C inhibitors in cells expressing the G12C mutant. Kim et al. conducted structural analyses to understand the binding interactions between BI-2865 and different KRAS variants.
The crystal structures revealed that BI-2865 bound to the GDP-loaded state of WT and mutant KRAS with high affinity. The inhibitor occupied a conserved binding pocket in KRAS, similar to covalent G12C inhibitors, but without relying on a covalent bond. The drug preferentially targeted the inactive state of KRAS and inhibited nucleotide exchange, which is crucial for KRAS activation. Importantly, the pan-KRAS inhibitor selectively suppressed KRAS activation and downstream signaling in cancer cells, with limited effects on HRAS and NRAS isoforms. This selectivity was attributed to specific amino acid differences between KRAS and other RAS isoforms.
Further experiments demonstrated that the pan-KRAS inhibitor effectively inhibited the growth of various cancer cell lines harboring KRAS mutations, while having minimal impact on cells with WT KRAS or upstream-activated KRAS signaling. RNA sequencing analysis revealed that the inhibitor specifically targeted the MAPK pathway, which is commonly activated by mutant KRAS. The antiproliferative effects of the pan-KRAS inhibitor correlated with the degree of KRAS dependency in different cancer cell lines.
A derivative of the pan-KRAS inhibitor, BI-2493, was used in in vivo studies and exhibited favorable pharmacokinetic properties and potent antitumor effects in mouse models with KRAS mutant tumors, without apparent toxicity.
The study provides evidence that a pan-KRAS inhibitor can effectively target a broad range of KRAS mutants, including non-G12C variants, and inhibit downstream signaling and cancer cell growth. The findings have implications for the development of KRAS-targeted therapies in various cancer types, such as lung, colorectal, and pancreatic cancers, and suggests that pan-KRAS inhibitors may offer a wider therapeutic index compared to isoform-specific inhibitors. The results also highlight the potential of further exploring different KRAS-directed therapeutics for precision oncology treatments.
Kim, D., Herdeis, L., Rudolph, D. et al. Pan-KRAS inhibitor disables oncogenic signalling and tumour growth. Nature 619, 160–166 (2023). https://doi.org/10.1038/s41586-023-06123-3
REPORT OF THE ACSMEDI-EFMC MEDICINAL CHEMISTRY FRONTIERS 2023
The ACSMEDI – EFMC Medicinal Chemistry Frontiers 2023 Symposium was held in Boston, MA, between the 10th and 13th of June and included 9 different sessions covering a selection of vital topics in medicinal chemistry.
The subjects discussed ranged from approaches in organic synthesis for drug discovery, chemical modulation of RNA and GPCR signalling to the development of probes for chemical biology research and approaches for hit identification. The conference also covered the advances in proximity-inducing modalities and targeted protein degradation and overall highlighted the leaps made in drug discovery and their importance in developing the next generation of therapeutics.
The organising committee prepared a truly exciting event, which featured a number of distinguished scientists who delivered inspiring talks, encouraged fruitful discussions, and highlighted the importance of interdisciplinary collaboration.
The scientific programme provided the attendees with a broader perspective on the challenges faced by medicinal chemists, which will undoubtedly contribute to their own research projects.
In addition, a poster session of 105 posters allowed fruitful exchanges between the participants, who could present their research to peers in a relaxed and informal atmosphere.
The EFMC Young Scientists Network and ACSMEDI Young Medicinal Chemists Committee organised a series of networking activities to facilitate the exchanges between students and early career researchers, especially those for whom attending a conference abroad was a first experience. The programme was completed by a round table discussion on the tips to “Getting a Job in Industry”, with panellists from US and Europe sharing their experience to an eager audience.
Finally, the conference was also the occasion to meet more informally during the social programme, whether it was during the welcome reception, at the conference dinner in the beautiful restaurant Rochambeau, or during a Boston Red Sox baseball game!
We invite you all to the next edition of the meeting, scheduled to take place in Utrecht, The Netherlands on April 8-14, 2023.
EFMC PHOTO CONTEST 2023 – DEADLINE POSTPONED!
"Illuminating Reality" is the topic of our 2023 Photo Competition. We invite researchers from any level (eg. students to expert professionals) and affiliation (eg. academia and industry), to submit a picture showing how their work contributes to “illuminating reality”, why it is important and what it represents in your everyday life.
The submitted pictures will be judged by a first round of online voting and the 20 best shots will be showcased at the EFMC-ASMC 2023 for attendees to vote live!
Submit your best picture, and win up to €50! Two runners-up will also be acknowledged and will receive 25€ each.
Submission deadline: July 10, 2022 July 17, 2023!
GET TO KNOW DAVID DAVIES (ANTABIO & O2H, UNITED KINGDOM)
In this edition, our MedChemBioConversations is with David Davis from Antabio and o2h, United Kingdom. Get to know him better by reading the interview below:
How did you get interested in Medicinal Chemistry?
I was always interested in nature and science from an early age. I took Biology, Chemistry and English at A-level (I never liked Maths of Physics) and did an undergraduate degree in Chemistry with Biological Chemistry, with a PhD project on Synthesis of Anthracyclinones.
Where are you currently working and what is your current position?
I have been Head of Medicinal Chemistry for a French biotech called Antabio for around 12 years. This is no longer a full time position and now I also manage medicinal chemistry projects for an Indian CRO called o2h. Previously I worked as a medicinal chemist at GSK and heritage companies, but since leaving around 15 years ago I mainly work from home (near London), working on site for meetings as and when.
What are your current research interests?
I work in antibacterials, Cystic Fibrosis, oncology, Parkinsons Disease plus some novel antiaging projects.
How would you explain what your research area is to non-scientists?
I do drug design for new medicines (and no, I don’t make pills).
What do you like best about your work?
I love having an idea about how to change a molecule to affect some biological activity or property, and see it work out. Ii doesn’t happen that often, most good ideas fail.
What kind of skills does your work require?
Medicinal chemistry skill and synthetic chemistry skills, organisational, communication and people skills plus a love of science and the desire to learn more every day. Plus the determination to carry on when things look difficult.
What do you consider your greatest achievement in your scientific career?
From my GSK days we have a drug which is being launched this year and from my Antabio days we have a drug going into Phase 1 this year. I am most proud of the J Med Chem paper describing the Antabio Phase 1 drug, because we achieved an asset in a crowded area with 6 chemists in 6 months.
What are the features of a successful PhD student or postdoc?
You have to enjoy doing research. Don’t be afraid to change things if your work is going badly – success is your responsibility as much as your supervisor’s. Read the literature. Every day.
What advice would you give to someone who wants to know more about your field?
Depends on what level they are at. If a synthetic chemistry PhD student, try reading med chem journals like ACS Med Chem Lett.
Have you experienced any unfair situations during your scientific career? How would you advise scientists facing similar situations?
Absolutely. From poor organisational culture, through poor managers, to unfair funding body decisions. Life is unfair, but don’t worry, no situation is permanent. Try to take control.
What is the most embarrassing thing you have done in the lab while doing experiments, e.g. explosions?
During my PhD I had a friend who got a job selling life insurance, so I said I would buy a policy from him and he could meet me at the lab. As he walked in, I dropped a Winchester of conc. HCl which smashed and the HCl began to react with a metal container next to it containing sodium. I screamed “Get out” to him while I sorted the problem out. (He still sold me the life insurance, though.)
Which scientist do you admire the most and why?
It has to be Watson and Crick. Changed the world.
What would you expect to be the next major breakthrough in medicinal chemistry?
I am close to the end of my career now, so I will leave that question for the next generation, but I don’t think it will be due to AI.
SUMMER SCHOOL ON PHARMACEUTICAL ANALYSIS 2023 (SSPA2023)
The SSPA is an international School which is addressed to PhD students, young researchers, and professionals from private companies. The 2023 edition will focus on “Analytical methods for drug manufacturing and quality control” and will take place on September 11-13, 2023 in Rimini, Italy.
- Pharmacopeias, Guidelines, GMP regulation et al.
- Structural Analytical Chemistry: NMR, spectroscopy
- Analytical aspects related to API development and manufacturing
- Analytical aspects related to Drug Product development and manufacturing
- In Process Control & Cleaning Verification
- Analytical Method Development and Phase-Appropriate Method Validation
- Analytical Aspects for Inhalation products
- Physical Properties and Solid State Characterization
- Stability Studies
- Microbiology Testing and Environmental monitoring
- Case studies: eparine and nitrosamine
Lectures will be delivered by recognised experts from the industrial and academic sectors. The School social activities are planned to promote networking and favor interactivity between participants and lecturers. To maximize these aspects the number of participants in presence is limited to 80 but the school is also offered as hybrid event.
More information and registrations on https://www.sspaweb.com/index.asp.
Contact: Marina Rinaldi (email@example.com)
EUCHEMS COMPCHEM 2023 – EXPLORING MOLECULAR SPACE
The EuChemS CompChem is the flagship event of the European Chemical Society Division of Computational and Theoretical Chemistry (DCTC). It will take place in Thessaloniki, Greece on August 27-31, 2023.
As a platform for scientists in industry and academia to showcase recent advances, developments and trends in theoretical and computational chemistry, the 14th edition of the conference series focuses on Electronic Structure Theory and Applications, Artificial Intelligence in Chemical Research, Materials Design, Biomolecular Systems, and Computational Chemistry in Industry.
More information and registration on https://euchems-compchem.eu/.
Deadline for abstract submission: July 20, 2023.
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is pleased to announce its upcoming events.
- SCI/RSC 22nd Medicinal Chemistry Symposium
- 6th RSC-BMCS/RSC-CICAG Artificial Intelligence in Chemistry
- Hot Topics: Targeting RNA
- RSC-BMCS Postgraduate symposium XVII
- 9th RSC-BMCS Fragment-based Drug Discovery Meeting
- The BMCS Mastering MedChem VIII: 8th RSC-BMCS Symposium on Mastering Medicinal Chemistry
- 35th Medicinal Chemistry in Eastern England (Hatfield symposium)
- 3rd RSC / SCI / SEQT New Therapeutics for Global Health
SCI/RSC 22nd Medicinal Chemistry Symposium
10th – 13th September, 2023, Churchill College, Cambridge, UK
Registration is open!
Synopsis: The organisers invite you to the 22nd SCI-RSC Medicinal Chemistry symposium, Europe’s premier biennial Medicinal Chemistry event, focusing on first disclosures and new strategies in Medicinal Chemistry
6th RSC-BMCS/RSC-CICAG Artificial Intelligence in Chemistry
4th – 5th September, 2023, Churchill College, Cambridge, UK
RSC BMCS/RSC CICAG
Registration is now open!
Synopsis: Artificial Intelligence is experiencing a renaissance in the development of new methods and practical applications to ongoing challenges in Chemistry. Following the successes of five 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 advances in AI and machine learning in Chemistry. The meeting will be held over two days and combine aspects of artificial intelligence and deep machine learning methods to applications in chemistry. The programme will include a mixture of keynote talks, panel discussion, oral presentations, flash presentations, posters and opportunities for open debate, networking and discussion.
Hot Topics: Targeting RNA
30th November 2023, Virtual
Registration is now open!
Synopsis: The BMCS Hot Topics online meetings are intended to highlight breaking areas of research in fields of science relevant to drug discovery. They will run as stand-alone half-day virtual events, 2-3 times per year. The programme will be targeted towards researchers working in academia or industry who would like to enhance their understanding of these nascent or developing fields. The inaugural meeting will cover relevant methods and modes of targeting RNA in drug discovery and will focus on how small molecules can accomplish this, including RNA binding and degradation, splicing modulation, and enzymes modifying RNA. There will be presentations from leading academics and industry.
RSC-BMCS Postgraduate symposium XVII
7th December 2023, University of Oxford, Oxford, UK
Abstract submissions are now open!
Registrations are now open!
Synopsis: This face to face meeting will comprise an oral and poster presentations from PhD students and post-doctoral workers researching in biological or medicinal chemistry. In addition, the agenda will feature invited keynote speakers from industry and academia.
9th RSC-BMCS Fragment-based Drug Discovery Meeting
4th – 5th March, 2024, Hinxton Hall Conference Centre, welcome Genome Campus, Cambridge, UK
Abstract submissions are now open!
Registrations are now open!
Synopsis: The aim of the 9th RSC-BMCS Fragment-based Drug Discovery meeting will be to continue the focus on case studies in Fragment-based Drug Discovery that have delivered compounds to late stage medicinal chemistry, preclinical or clinical programmes. The Fragment series was started in 2007 and continues with this theme in having over three-quarters of the presentations focused on case studies. This will be complemented by technology progress in high concentration, NMR, SPR and X-ray screening.
The BMCS Mastering MedChem VIII: 8th RSC-BMCS Symposium on Mastering Medicinal Chemistry
15th March, 2024, Burlington House, London, UK
Registration will be open soon! Keep checking website for updates!
Synopsis: Mastering Medicinal Chemistry VIII is the latest in an ongoing series of conferences intended to provide expert advice and guidance to new practitioners in the field of drug discovery. It has been said that “there are two types of drug discovery programmes: those that hit serious problems and those that are going to hit serious problems”. Anticipating and preparing for such problems thus accelerates the delivery of new medicines: this event will feature presentations from experienced ‘drug-hunters’ in both industry and academia, who will talk about the challenges faced in modern drug discovery, and will share best practice common to all successful medicinal chemists.
35th Medicinal Chemistry in Eastern England (Hatfield symposium)
25th April 2024, Fielder Centre, Hatfield, UK
Date for your diary!
Synopsis: Known colloquially as the “Hatfield MedChem” meeting, this is a highly successful, long-standing, one-day meeting that runs annually. The scientific program will comprise presentations showcasing medicinal chemistry case studies from tools to candidates, across a range of modalities, therapeutic areas and target classes, as well as covering more general topics at the forefront of drug discovery. The meeting aims to be informal and interactive, and is ideal for all those working in medicinal chemistry and drug discovery more widely.
3rd RSC / SCI / SEQT New Therapeutics for Global Health
19th – 21st June 2024, GSK TresCantos, Madrid
Registration will be open soon! Keep checking website for updates!
Synopsis: Tuberculosis, malaria and diseases caused by a diverse range of pathogens, including flaviviruses (eg dengue, West Nile), kinetoplastids (causative agents of Chagas disease, leishmaniasis, etc) and gut pathogens (worms, bacteria, parasites), remain a cause of high mortality across the globe. Fortunately, an ever-improving understanding of the complex life-cycles of these disease-causing pathogens is presenting increasing opportunities for those seeking to tackle these global health problems.
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EFMC ORGANISED EVENTS
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
September 17-20, 2023
National Meeting on Medicinal Chemistry (NMMC28)
September 20-22, 2023
Vila Real, Portugal
I International Meeting Molecules4Life
December 7, 2023
Oxford, United Kingdom
RSC-BMCS Postgraduate Symposium XVII
January 28-February 1, 2024
St. Anton, Austria
4th Alpine Winter Conference on Medicinal and Synthetic Chemistry
September 10-15, 2023
Vienna Summer School Drug Design
September 11-13, 2023
Summer School on Pharmaceutical Analysis 2023
PhD candidate cancer theranostics, Antwerp, BELGIUM
Postdoctoral Researcher Radiotracer Development, Antwerp, BELGIUM