EFMC-ISMC 2022 – STILL POSSIBLE TO REGISTER!
Do not miss the opportunity to join the 945 participants already registered for the XXVII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022), scheduled to take place in Nice, France.
The programme will take place over 5 days, and will cover:
- advances in drug discovery in major therapeutic areas
- most recent advances in new technologies
- the interface between chemical biology and drug discovery
- first-time disclosures and recent highlights in medicinal chemistry
High level presentations by the three EFMC Award winners, as well as the Klaus Grohe Prize winner and IUPAC-Richter Prize winner will also be part of the symposium.
More information and registration www.efmc-ismc.org.
We look forward meeting you in Nice!
REPORT OF THE 16TH EFMC SHORT COURSE ON MEDICINAL CHEMISTRY
After several postponements due to the coronavirus outbreak, the 16th EFMC Short Course “New Opportunities in GPCR Drug Discovery” finally took place on May 8-11, 2022 and was followed by 16 participants.
The course leaders, Prof. Gyorgy Keseru (Hungarian Academy of Science, Hungary) and Prof. Rob Leurs (VU Amsterdam, The Netherlands) composed an attractive programme with 10 world-renowned experts. The speakers, Iwan de Esch, Chris de Graaf, Laura Heitman, Raimond Heukers, Albert Kooistra, Rob Lane, Aurélien Rizk and Moran Shalev-Benami covered all aspects of GPCR Drug Discovery.
Most of the participants rated the course as very good; the remaining participants scored the course as good. The participants also scored the different teachers, for the content of their presentation and the way of presentation of it both. Using a score from 0 to 5, five being the highest, the average figure reached 4.5.
Part of the success of the course is due to the pleasant venue in the midst of a beautiful park in the outskirts of Leyden, a city known for its rich history in arts and sciences.
The EFMC plans the next course on “Protein Degradation” for April 23-26, 2023. The course will be organized by Profs Alessio Ciulli and and Suzanne O'Connor, University of Dundee (UK). Details on this course will be available on the site of the EFMC soon.
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 Covalent Allosteric Inhibitors of Akt Generated Using a Click Fragment Approach, published in ChemMedChem, the official journal of the EFMC.
Akt is a serine/threonine kinase of the phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) signalling pathway and is involved in many cellular processes, including cell growth, proliferation and glucose metabolism.
Recently, there has been a renewed interest in covalent inhibitors as therapeutic agents and borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt. This irreversible compound served as inspiration for the design and synthesis of further potential covalent allosteric inhibitors of Akt, accessible through a modular approach with click chemistry. van der Westhuizen et. al. generated a small library of covalent allosteric imidazopyridine-based inhibitors. Firstly, the authors focused on the preparation of regioisomeric analogues of a previously synthesized meta-acrylamide. Secondly, they prepared methylated versions of the covalent molecules to assess the “methyl effect” on biological activity and physical properties. Thirdly, they investigated hybrid structures to further expand the chemical space. Covalent docking allowed to elucidate the binding mode and further support compound design. Using LC-MC and X-ray crystallography, novel covalent inhibitors were identified. The kinetic parameters of inactivation, namely the inhibition constant (KI), and the rate constant of enzyme inactivation (kinact) were used to characterize the irreversible inhibitors. The biochemical evaluation combined with investigation in cells allowed to pinpoint three novel covalent allosteric inhibitors of Akt1, namely compounds 11–13. The molecules showed improved potency compared to the previously synthesized compounds, even though none of them matched the potency of borussertib. This study could provide additional information for the design of future generations of irreversible Akt inhibitors.
Covalent Allosteric Inhibitors of Akt Generated Using a Click Fragment Approach. van der Westhuizen L, Weisner J, Taher A, Landel I, Quambusch L, Lindemann M, Uhlenbrock N, Müller MP, Green IR, Pelly SC, Rauh D, van Otterlo WAL. ChemMedChem. 2022 May 18; 17 (10): e202100776. doi: https://doi.org/10.1002/cmdc.202100776.
EFMC PHOTO CONTEST 2022 – DEADLINE POSTPONED!
"MedChemBio Realness" is the topic of our 2022 photo competition. We invite researchers from any level (eg. students to expert professionals) and affiliation (eg. academia and industry), to submit a picture showing the reality of Medicinal Chemistry/Chemical Biology, 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-ISMC 2022 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 15, 2022!
Enter the competition!
NEW STEERING COMMITTEE OF THE EFMC CHEMICAL BIOLOGY INITIATIVE – ACADEMIA MEETS INDUSTRY
Initiated in 2017, the Chemical Biology Initiative has now increased the number and diversity of its board.
Except for Dr Paola Arimondo from the Institut Pasteur (France), the new composition represents the industry's interests in Chemical Biology. The incoming members are Dr Andrew Zhang from Astra Zeneca (USA), Dr Ulrich Schopfer from Novartis (Switzerland), Dr Uwe Grether and Dr Arne Rufer, both from Roche (Switzerland) and Dr Sebastian Essig from Bayer (Germany). Together with the previous ones, the working group aims to reinforce the European Chemical Biology community.
For this purpose, Dr Yves P. Auberson and Prof. Maria Duca held an inaugural meeting in Basel (Switzerland), where future activities such as virtual seminars, article collections in the European Chemical Societies Publishing, conferences, etc., were discussed.
We believe such joint projects will improve collaboration among all Chemical Biology scientists in Europe.
Steering Committee of the EFMC Chemical Biology Initiative in Basel
GET TO KNOW TATJANA ROSS (MERCK HEALTHCARE KGAA, GERMANY)
In this edition, our interviewee is Dr Tatjana Ross from Merck, Germany. Get to know her better by reading the interview below:
How did you get interested in Medicinal Chemistry?
After my A-levels, I started my professional career with a vocational training as laboratory technician and spent two thirds in a Medicinal Chemistry laboratory at nowadays Sanofi. My female laboratory head was so inspiring to me, and I really enjoyed synthetic chemistry, so I started studying chemistry in Frankfurt after accomplishment of the training.
I did my PhD at the ETHZ in the group of Prof. Karl-Heinz Altmann on a total synthesis topic “Resorcylic Lactone L-783277 as a New Lead Structure for Kinase Inhibition - Total Synthesis and SAR Studies“ and continued my academic career with a postdoctoral stay with Prof. Steven Ley in Cambridge/UK, again working on a total synthesis project.
What is your current position?
I am co-leading the Medicinal Chemistry Department in Darmstadt as a Director Medicinal Chemistry. In addition, I am a research project leader. My research interests are Oncology/Immuno-Oncology/Fragment-based drug discovery/Chemical Biology/Degrader.
How would you explain what your research area is to non-scientists?
We develop new drugs for patients suffering from cancer. Whereas our area of expertise is at the very beginning of this process, namely identifying what goes wrong in the indication of interest and identifying chemical structures that can be used to fix the mis-functioning of proteins or other cellular targets.
What do you like best about your work?
I am a passionate researcher and people manager that enjoys helping my direct reports to grow out of their comfort zone. I love working with people especially with scientists and to do something that impacts patients’ life for the good.
What kind of tasks does your work involve?
Listen to people, understand what they need to solve their problems and help them to self-help, look at research projects and understand what the next critical step is to be investigated and enable the project teams to go for it. Read literature, attend conferences, understand what others do and come up with ideas how this could be helpful for our research.
All this requires emotional intelligence, scientific expertise, communication and influencing skills.
What do you consider your greatest achievement in your scientific career?
I am proud of being a meaningful support to brilliant scientists in order to progress projects into the clinics to meet patients’ needs.
Which of your papers are you most proud of and why?
Alexander J. Oelke, David J. France, Tatjana Hofmann, Georg Wuitschik, Steven V. Ley: Total Synthesis of Chloptosin; Angew. Chem. Int. Ed. 2010, 49 (35), 6129-6142. This was just very hard work…
What are the features of a successful PhD student or postdoc?
To believe in themselves, to be curious, to be open minded and to be really motivated and hard-working to achieve their goals.
How would you advise scientists facing unfair situations during their scientific career?
This might happen. However, be aware that you are on the driver seat, you will make it as long as you really want to achieve your goals...Never, never give up.
What is the most embarrassing thing you have done in the lab while doing experiments, e.g., explosions?
Once I tripped over a dry ice container and destroyed it. I was really embarrassed as it happened during an internship with Novartis. However, my lab head was kind and calmed me down.
What are your recommendations for a book, podcast, website, blog, YouTube channel or film?
https://drughunter.com/ and http://practicalfragments.blogspot.com/
Which field of medicinal chemistry do you consider the most promising for the future?
Identification of tools for difficult-to-drug targets and developing them onto in vivo suitable compounds for target validation is the most important area for the success of drug discovery in future.
What would you expect to be the next major breakthrough in medicinal chemistry?
Making use of AI in that sense that it really suggests new structures and creates something new.
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is delighted to announce some upcoming events.
- AI in Chemistry: 5th RCS-BMCS /RSC-CICAG Artificial Intelligence in Chemistry
- 8th RSC/SCI symposium on GPCRs in Medicinal Chemistry
- RSC-BMCS Targeted Protein Degradation: “Three’s a crowd?”
AI in Chemistry: 5th RCS-BMCS /RSC-CICAG Artificial Intelligence in Chemistry
1st and 2nd September 2022, Churchill College, Cambridge and virtual
Synopsis: Artificial Intelligence is presently experiencing a renaissance in development of new methods and practical applications to ongoing challenges in Chemistry. Following the successes of three annual “Artificial Intelligence in Chemistry” meetings starting in 2018, we are pleased to announce that the Biological & Medicinal Chemistry Sector (BMCS) and Chemical Information & Computer Applications Group (CICAG) of the Royal Society of Chemistry are once again organising a conference to present the current efforts in applying these new methods. The meeting will be held over two days and combine aspects of artificial intelligence and deep machine learning methods to applications in chemistry
8th RSC/SCI symposium on GPCRs in Medicinal Chemistry
5th to 7th October 2022, Verona, Italy
The call for poster abstracts will close on Thursday, 11th August
Closing date for bursary application is Tuesday, 23rd August
Synopsis: The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We are pleased to be holding this 8th meeting in the series on GPCR drug discovery, which will combine cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.
RSC-BMCS Targeted Protein Degradation: “Three’s a crowd ?”
16th and 17th November 2022, Virtual
Abstract submission will be open soon, please keep checking website for updates
Synopsis: Targeted protein degradation is a rapidly developing field of drug discovery which is expanding the proportion of human proteins which are tractable drug targets. Whereas conventional small molecules are designed to block the activity of a protein, targeted protein degraders act by harnessing biological pathways to remove the protein entirely. This conference will showcase presentations showing the application and development of degradation technologies such as molecular glues and heterobifunctional degraders (e.g. PROTACs)
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EFMC ORGANISED EVENTS
September 4-8, 2022
XXVll EFMC International Symposium on Medicinal Chemistry
September 8-9, 2022
9th EFMC Young Medicinal Chemists' Symposium
EFMC SPONSORED EVENTS
July 22, 2022
VIII SEQT Young Researchers Symposium
July 27-29, 2022
3rd Molecules Medicinal Chemistry Symposium (MMCS)
August 8-9, 2022
Chemical Biology Ireland Conference
September 11-14, 2022
27th National Meeting in Medicinal in Medicinal Chemistry
September 15-17, 2022
9th BBBB International Conference on Pharmaceutical Sciences - Pharma sciences of tomorrow
September 26-30, 2022
23rd European Symposium on Quantitative Structure-Activity Relationship
September 27, 2022
2nd Munich Leiden Virtual ChemBio Talks
EFMC CERTIFIED SCHOOLS
July 19-21, 2022
Medicinal Chemistry and Chemical Biology in Drug Discovery: the Pharma Perspective
September 11-15, 2022
Les Diablerets (VD), Switzerland
Swiss Summer School on Chemical Biology
October 9-14, 2022
Swiss School on Medicinal Chemistry in Leysin
EFMC SPONSORED SCHOOLS
September 21-23, 2022
Summer School in Pharmaceutical Analysis (SSPA2022)
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