MedChemWatch
Monthly Newsletter December 2020

A MESSAGE FROM EFMC - OUR INITIATIVES TOWARDS MORE DIVERSITY

The European Federation for Medicinal Chemistry, as a learned society, is firmly committed to represent its members in a way that reflects the diversity of its community. It encourages diversity of views, and participation in its initiatives and scientific events independently of gender, nationality, personal characteristics or circumstances.

With regard gender balance, EFMC has increased the proportion of ISMC session chairs & speakers to align with the increasing percentage of women in medicinal chemistry-related disciplines, which now averages between 35% and 40% in Europe. In the programme of the 2021 EFMC-ISMC in Basel, female scientists represent 37% of the session chairs. Similarly, EFMC aims to promote and achieve gender balance in its speaker line-ups.

The representation of female delegates in the EFMC Council has followed a similar trend, with a delay largely due to the measured turnover rate of these positions. From 4% in 1985, it reached 24% in 2020. In the Executive Committee (EC), EFMC also promotes the nomination of female scientists and recently appointed Dr Kristina Goncharenko (Chair of the Young Scientists Network). She will actively participate in EC meetings and represent the voice of a younger and more gender-diverse generation.

Younger scientists are becoming more involved in shaping the medicinal chemistry community. Over the past decade, student participation in EFMC-ISMCs has grown to thirty percent, encouraged by the creation of the EFMC Prizes for Young Medicinal Chemists, the Young Medicinal Chemist Symposium (EFMC-YMCS), travel grants for young scientists, and, most recently, the Young Scientists Network (EFMC-YSN).

The EFMC-YSN membership has a 1:1 gender ratio, which reflects the demographic of the young scientist's population. Its Board is composed of 58% women and is chaired by Dr Goncharenko.

Supporting the diversity of our community goes beyond gender balance. We hope you will help and support our efforts and help us to support you.

LITERATURE SPOTLIGHT

The “literature spotlight” section of the newsletter will bring you a summary of the recently published research in a concise and readable way. Multiple themes from different journals will be highlighted thanks to the valuable contribution of Dr Clemens Zwergel (University of Rome, IT) from the communication team.

This ninth contribution will focus on the recently published article on the “Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors” (by Wagner et al. in ChemMedChem).

The C−C chemokine receptor type 2 (CCR2) is known to be involved in the trafficking of lymphocytes and monocytes/macrophages responsible for various pathophysiological processes such as inflammatory and autoimmune diseases, as well as for tumor growth and metastasis formation. In the field of positron emission tomography (PET) imaging this receptor is a promising diagnostic marker for lung inflammation, injured heart or pancreatic ductal adenocarcinoma proven in several clinical trials. Until recently, only a peptidic ligand that binds to the first extracellular loop of the CCR2 receptor ECL1i was applied in PET imaging either as 64Cu-DOTA-ECL1i or 68Ga-DOTA-ECL1i conjugate. Wagner et al. describe for the first time the development, synthesis and evaluation of a series of highly selective CCR2 antagonists as 18F-labeled PET tracers. A previously unknown structure–activity/affinity relationship between CCR2 and CCR5 led to the development of these innovative compounds. Their most promising candidates were extensively evaluated for their CCR2 activity/affinity and their off-target selectivity profile checking 47 other related receptors such as GPCRs, ion channels and transporters. A biodistribution study of the most potent and selective candidate revealed a promising profile for a further preclinical and eventual clinical development. It is the first potential nonpeptidic PET tracer for the imaging of CCR2 receptors.

Stefan Wagner, Fernando de Moura Gatti, Daniel G. Silva, Natalia V. Ortiz Zacarias, Annelien J. M. Zweemer, Sven Hermann, Monica De Maria, Michael Koch, Christina Weiss, Dirk Schepmann, Laura H. Heitman, Nuska Tschammer, Klaus Kopka, Anna Junker
Development of the First Potential Nonpeptidic PositronEmission Tomography Tracer for the Imaging of CCR2Receptors
ChemMedChem 2020, in press
https://doi.org/10.1002/cmdc.202000728

EFMC HISTORY SPECIAL ISSUE

To celebrate its golden jubilee, the EFMC written a series of articles charting its history, activities and future directions. We are most grateful to ChemMedChem for its support and publishing these articles.

With the contribution of Henk Timmerman in collecting its "Memoirs of the First 50 Years of the European Federation for Medicinal Chemistry" and the extraordinary archivist's efforts of Edmond Differding to gather and write both:

The EFMC is now able to look with pride over its history.

CALL FOR NOMINATIONS - EFMC HONORAY FELLOWS

The EFMC is pleased to announce the 2021 call for nominations for the title of "Honorary Fellows".

This life-long title and associated medal aim to recognize individuals who have provided outstanding support to the EFMC and contributed in strengthening the position of medicinal chemistry, chemical biology or related fields in Europe.

Nominations can be submitted until January 31, 2021, and should include:

  • Brief curriculum of the nominee
  • Statement of the documented facts supporting the nomination, summarizing scientific achievements and support of EFMC activities. (maximum two pages)
  • Two seconding nomination letters

Self-nominations are not accepted. There are no age restrictions, and nominees may have an academic or industrial background. Nominees should be European residents or have spent a considerable proportion of their career in Europe.

The award ceremony will take place during the opening of the XXVI EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2021), scheduled to take place in Basel, Switzerland from August 29-September 2, 2021. Appointed Honorary Fellows will be invited to attend the meeting and receive their award on stage.

More information and nominations on www.efmc.info/honorary-fellows.

CALL FOR NOMINATIONS - EFMC PRIZES 2021

To acknowledge and recognize outstanding young medicinal chemists (≤ 12 years after PhD) working in European industry and academia, EFMC established the "EFMC Prize for a Young Medicinal Chemist in Industry" and the "EFMC Prize for a Young Medicinal Chemist in Academia".

The two Prizes are given annually and consists of a diploma, € 1.000 and an invitation for a short presentation at an EFMC symposium.

The prize-winners will be invited to give oral communications at the XXVI EFMC International Symposium on Medicinal Chemistry and EFMC Young Medicinal Chemist Symposium (EFMC-ISMC 2021).

Applications and regulations can be found on www.efmc.info/prizes

Deadline for submission: January 31, 2021

GET TO KNOW CHRISTOPH RADEMACHER, UNIVERSITY OF VIENNA, AUSTRIA

In this edition, our #Iamamedicinalchemist is Dr Christoph Rademacher, University of Vienna, Austria.

 


How did you get interested in medicinal chemistry?

I was in my first semesters in Lübeck studying “Molecular Biotechnology” and walked through the library amazed by all those books. The new “Wirkstoffdesign” book by Böhm, Klebe and Kubinyi just came out in 2002 and I borrowed it and read it from A to Z in a couple of weeks. My next step was to walk into the Institute of Chemistry asking for an internship to do molecular modelling.

Where and when did you obtain your PhD diploma?
I stayed at the University of Luebeck in the Chemistry department and did my PhD (2009) on “Investigations into Viral Entry Mechanisms and Carbohydrate-Protein Interactions using NMR” in the same group.

Where did you have your postdoc position?
Department of Chemical Physiology with Prof. Dr James C. Paulson, The Scripps Research Institute, La Jolla, USA entering the field of Glycoimmunology and Targeted Delivery.

What are your current research interests?
Fragment-based drug discovery against challenging protein targets such as carbohydrate-binding proteins. Allostery in Drug Discovery. Targeted delivery to manipulate immune cells for immunotherapies.

What do you like most in your job?
It is an excellent mixture of creativity and working in smarts teams of brilliant people.

What do you consider your biggest achievement in your scientific career?
Translating basic research on carbohydrate binding proteins and the development of ligands for these challenging proteins into something that might make it into the market as a drug.

What is the most embarrassing thing you did in the lab while doing experiments?
A student thought he could get rid of left-over dry ice by pouring it into the sink. I didn't think either by assuming I could facilitate the process by adding water on top of it - which essentially let a massive amount of dry ice vapor floating the entire lab space by about 1 m heights and scaring people in the hall way.

Which scientist do you admire the most and why?
Max Delbrück, for moving from theoretical physics into revolutionizing biology.

Did you experience any unfair situations during your scientific career?
It is getting less, but I still see scientist being selected for being great thinkers, but not good leaders – and they kill the career of the next generation by promoting a hopefully-soon-to-be-extinct picture of how science works.

Which paper of yours you are the proudest of and why?
Wamhoff et al. 2019 ACS Cent Sci. 5, 808-820.
This paper summarizes our work on the development of a targeting ligand for human Langerin enabling the future development of ligand-based targeted delivery for immunomodulation. Since day one of my independent career we have been working on this and my team together with our collaborators managed in five years to design such targeting ligand from the scratch, starting from modelling, structure-based to design, over to chemistry and into primary human cells from human skin using a breath of methodology.

Which field of medicinal chemistry do you consider the most promising in the future?
Rational design of allosteric modulators of target proteins.

What would you like to ask from other medicinal chemists?
To think out of the box and develop new methodologies treating every project as a unique challenge and not do the same type of chemistry on the same type of molecules over and over again.

What would you guess to be the next major breakthrough in medicinal chemistry?
The feedback cycle between artificial intelligence suggesting solutions to old problems that we had not envisioned before and our rapid learned by deriving a rational from those suggestions.

MEET JULIEN LEFRANC, NUVISAN, GERMANY

Carried out by the holiday season, we offer you as special gift to discover another great #Iamamedicinalchemist and meet Dr Julien Lefranc, Nuvisan.

 


How did you get interested in Medicinal Chemistry?

My first contact with medicinal chemistry was as an undergraduate student in France. During that time, I had the chance to do internships with pharma companies (Sanofi and Pierre Fabre) and could discover research in industry.

Where and when did you obtain your PhD diploma?
I did my PhD at the University of Manchester under the supervision of Prof. Jonathan Clayden. I graduated in December 2011.

What was the topic of your PhD project?
Jonathan Clayden’s group is well known for organilithium chemistry and that was the topic of my PhD. I was working on the rearrangement of lithiated vinyl ureas to synthesize α-tertiary amines.

Where did you have your postdoc position?
As a postdoc I worked for two years in the group of Prof. Dirk Trauner where I worked on the total synthesis of natural products.

Where do you work at the moment and what is your current position?
I am currently working as a labhead in Bayer in Berlin in the Med Chem department.

What are your current research interests?
Over the last 6 years I have been working in oncology mainly in Lead-optimization projects. I’ve worked on different kinases inhibitors projects such as ATR and TBK1 inhibitors and now I am working on the exciting field of immuno-oncology.

What do you like most in your job?
There are so many interesting parts in my everyday job that it’s difficult to pick one. I have the chance to keep learning new things all the time by working with excellent scientists across a lot of different fields. I also really enjoy working with my lab team in order to synthesis new compounds and solve problems.
One part of my job is the management of research projects where I work with other scientists on oncology projects in order to identify new clinical candidates for oncology. In parallel I also have a chemistry lab with three coworkers. We need to design and synthesis the new compounds that will be tested by our colleagues in other departments such as pharmacology, DMPK etc.

What kind of skills your job requires?
When you work in research, I think you need to be curious and not afraid to fail or make mistakes. When you are responsible for research teams and a lab you definitely need to be organized and be able to communicate clearly. You also need to trust your team either in the lab or in the other functions.

What is the most embarrassing thing you did in the lab while doing experiments?
It was probably when I wanted to show one of my labmate how to quench BuLi safely. And at the first drop we saw very nice blue flame. Fortunately, nobody was injured, and we didn’t start a fire.

Which scientist do you admire the most and why?
That's a very difficult question to answer. There so many excellent scientists around that I can’t pick one. Among all the great chemists around I have to say that I am always really looking forward to reading the total synthesis papers from Sarah Reisman or a new methodology paper from John Hartwig.

Which paper of yours you are the proudest of and why?
I think my last paper on the discovery of BAY-985 as a highly selective TBK1/IKKε probe was definitely a very exciting story. It was my first project as a project leader and quite challenging. We managed to identify a highly selective compound that is now available for free to the scientific community so everybody can use it in their own research if they want to probe these targets.

Which field of medicinal chemistry do you consider the most promising in the future?
At the moment, we see a very strong interest in the scientific community for degraders and Protacs. The field is exciting and offers a lot of promising perspectives for treatments in the future.

What would you guess to be the next major breakthrough in medicinal chemistry?
I think small molecule RNA inhibitors are getting more and more attention in the scientific community and I won’t be surprised if this modality plays an important role in the future.

EFMC ADVENT CALENDAR – JOIN AND WIN A GOODIEBOX

Staying in the jolly atmosphere of the holiday seasons, the EFMC Communication team has launched its traditional "Advent Calendar" of festive pictures related to science.

Be sure not to miss them on our social media: Twitter, Facebook & Instagram!

If you want to join and compete to win an EFMC Goodiebox, send your pictures to us at communication@efmc.info, or directly in MP on our social media accounts.

 

NEWS FROM THE DIVISION FOR MEDICINAL CHEMISTRY & CHEMICAL BIOLOGY (DMCCB) OF THE SWISS CHEMICAL SOCIETY (SCS)

The DMCCB is happy to announce the following event: «Targeting RNA by Small Molecules», which will take place as an online event on the 4th of February 2021.

The topic of this DMCCB Basel symposium has been selected by the DMCCB members among several proposals aiming at reinforcing the links between chemical biology, medicinal and agro chemistry, while being of importance in drug discovery and optimization programs.

Discover the programme!

Illustrating the progress in the field of RNA targeting drugs the symposium will be of high interest to students in chemistry, pharmacy, biology, and to the medicinal chemistry and chemical biology community at large. The target audience is therefore composed of scientists from pharmaceutical and biotech industries, as well as colleagues from academia.

Confirmed Speakers are:

  • Kamal Azzaoui (Saverna Therapeutics, Basel, Switzerland)
  • Matthew Disney (Scripps Research Institute, Florida, United States)
  • Michaela Frye (Deutsches Krebsforschungszentrum, Heidelberg, Germany)
  • Amanda E. Hargrove (Duke University, Durham, United States)
  • TBD (Storm Therapeutics, Cambridge, United Kingdom)
  • Iris Alroy (Anima Biotech, Bernardsville, United States)

Due to the Covid-19 pandemic, a virtual meeting is planned.

For all information, please check the event website: http://dmccb21.scg.ch

NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)

The BMCS invite you to stay in touch through its new website and various social media, and announces some upcoming events.

STAY CONNECTED: NEW BMCS WEBSITE - https://www.rscbmcs.org
Please join as many of the groups below as you wish to receive the latest news from the RSC BMCS:
Twitter             @RSC-BMCS
LinkedIn           linkedin.com/company/rsc-bmcs
Facebook         @RSCBMCS
Instagram        @RSCBMCS
YouTube           youtube.com/channel/UCMEMVT-D4vHxNU-bQQw3Ifw

VIRTUAL - 7½th RSC / SCI SYMPOSIUM ON GPCRS IN MEDICINAL CHEMISTRY
24th and 25th February 2021 (two afternoon sessions)
Website: https://www.rsc.org/events/detail/41236/7-th-rsc-sci-symposium-on-gpcrs-in-medicinal-chemistry

Synopsis: The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. This series of events on GPCR drug discovery, which will combine cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.

VIRTUAL - SYNTHESIS IN DRUG DISCOVERY AND DEVELOPMENT
22nd and 23rd March 2021 (two afternoon sessions)
The call for poster abstracts will close on 29th January
Website: https://www.rsc.org/events/detail/39710/synthesis-in-drug-discovery-and-development

Synopsis: This symposium aims to highlight and celebrate the crucial role which synthetic organic chemistry plays in the success of small molecule drug discovery.

The three main themes of the symposium will be:

  • Innovative synthesis facilitating candidate discovery
  • Novel bioisosteres and methodology applicable to drug discovery
  • Overcoming challenges of scale-up and process scale chemistry.

VIRTUAL - KINASE 2021: 9th RSC / SCI SYMPOSIUM ON KINASE INHIBITOR DESIGN
14th and 15th April 2021 (two afternoon sessions)
The call for poster abstracts will close on 20th January
Website: https://www.rsc.org/events/detail/40755/kinase-2021-9th-rsc-sci-symposium-on-kinase-inhibitor-design

Synopsis: Synopsis: With more than 25 FDA-approved small molecules, the field of kinase inhibition continues to attract significant investment from the drug discovery and development community. The event will encompass case studies of ongoing programmes as well as successful past programmes.

21st RSC / SCI MEDICINAL CHEMISTRY SYMPOSIUM
12th to 15th September 2021, Churchill College, Cambridge, UK
The call for poster abstracts (first round) will close on 30th April
Website: http://www.rsc.org/events/detail/42821/21st-rsc-sci-medicinal-chemistry-symposium

Synopsis: Europe’s premier biennial Medicinal Chemistry event, focusing on first disclosures and new strategies in medicinal chemistry.

THIS NEWSLETTER IS KINDLY SPONSORED BY SYMERES


 

ISSUE SPONSORED BY

Symeres is the leading mid-sized European Contract Research Organization for your drug-discovery and development challenges. Our services span across early stage hit finding all the way to the delivery of your early clinical drug substance API. We Make Molecules Matter.

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EFMC ORGANISED EVENTS

January 28, 2021
Online
6th EFMC-YSN MedChemBioOnline

August 29-September 2, 2021
Basel, Switzerland
EFMC-ISMC 2021 - XXVI EFMC International Symposium on Medicinal Chemistry

September 2-3, 2021
Basel, Switzerland
EFMC-YMCS 2021 - 8th EFMC Young Medicinal Chemists’ Symposium

Autumn 2021
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry - New Opportunities in GPCR Drug Discovery

EFMC SPONSORED EVENTS

February 25-27, 2021
Online
18th Hellenic Symposium on Medicinal Chemistry (HSMC-18)

JOB PORTAL

Analytical Chemist (Job Code AC) for the quality control of our chemical compound collection, EU-OPENSCREEN ERIC, Compound Team, Berlin, Germany

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Postdoctoral Fellows in Chemical Biology of Ciliary Signaling, University of Geneva, Department of Organic Chemistry and NCCR Chemical Biology, Geneva, Switzerland

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Postdoc in Computational Chemistry, University of Hradec Kralove, Department of Chemistry, Hradec Kralove, Czech Republic

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Senior Research Scientist – Synthetic/Medicinal Chemistry, AstraZeneca R&D, Gothenburg, Sweden, Early R&I Medicinal Chemistry, Gothenburg, Sweden

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Senior lecturer in Medicinal Chemistry/Chemical Biology, University of Gothenburg, Department of Chemistry and Molecular Biology, Gothenburg, Sweden

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