MedChemWatch
Monthly Newsletter March 2023

EFMC-YSN MENTORING PROGRAMME 2023 – DEADLINE POSTPONED (MARCH 10)

The one year mentoring programme is shaped for PhDs (up to 18 months before the end PhD) and Post-docs, who are seeking a career in medicinal chemistry, chemical biology or related fields, either in industry or academia. The main objective is to support their transition into the job market by providing feedback, soft-skill training, and overall guidance. 

To meet the demand, we decided to postpone the registration deadline to March 10. All the material will have to be submitted by March 12, so do not miss this unique opportunity to connect with experienced professionals, gain valuable insights and achieve your career goals.

More information and application on www.efmc.info/mentoring-programme.

IX EFMC INTERNATIONAL SYMPOSIUM ON ADVANCES IN SYNTHETIC AND MEDICINAL CHEMISTRY (EFMC-ASMC 2023) – CALL FOR ABSTRACTS

The IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC 2023) will take place in Zagreb, Croatia on September 3-7, 2023.

The symposium programme will feature an opening lecture by Prof. Jeffrey Bode (ETH Zurich, Switzerland), followed by 26 invited lectures equally selected from industry and academia, as well as 10 oral communications selected from submitted abstracts.

Submit your abstract before April 13, 2023 to be considered for one of the Oral Communications.

SYMERES PHD PRIZE FOR EXCELLENCE IN CHEMISTRY IN LIFE SCIENCES RESEARCH – DEADLINE IS APPROACHING

The deadline to apply for the Symeres PhD Prize for Excellence in Chemistry in Life Sciences Research is quickly approaching!

Upon application, the submission will be peer reviewed and the 10 best candidates will be invited to the Symeres facilities in Nijmegen, The Netherlands to present their work. The prizes will consist of a diploma and a cash prize of 1000€ for the winner, 600€ for the runner-up and 400€ for the third place. The winner will also be invited to deliver an oral communication at the EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS).

The 2023 winner will also receive a free registration and a 500€ travel grant to attend both the IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC 2023) and the 10th EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS 2023) which will take place in Zagreb, Croatia on September 3-7 & September 7-8, 2023.

Application deadline is March 15, 2023!

LITERATURE SPOTLIGHT

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 “Scouting in silico different chemo-types of PDE4 inhibitors to guide the design of new anti-inflammatory/antioxidant agents” by Elena Cichero et al., published in ChemMedChem.

Phosphodiesterase-4 (PDE4) regulates inflammation through degradation of the intracellular signalling molecule, cAMP. Inhibition of PDE4 has been recognised as a method for treating a variety of conditions, including chronic obstructive pulmonary disease. Cichero et al., iterating upon recent developments in cathechol-, naphthyridinone- and toddacoumalone-based PDE4 inhibitors, used in silico methods to rationalise a series of novel PDE4 inhibitors and predict their ADMET properties.

The authors prepared a library of compounds featuring a scaffold-merged benzodihydro-1,4-oxazine conjugated to a basic terminus via an oxime-based linker. The novel design was rationalised to combine desirable interactions and vectors from previously reported inhibitors, while offering additional engagement with aromatic residues.  The library was evaluated by MOE Dock and the top-scoring compounds were selected for synthesis.

The authors tested two of these compounds in vitro, measuring the compounds’ effect on reactive oxygen species (ROS) accumulation as a marker of inflammatory response. In endothelial cells, the novel compounds proved to have an antioxidant effect comparable to a previously reported PDE4 inhibitor, while little antioxidant activity was detected in human platelets.

In silico evaluation of the library’s ADMET properties indicated that these novel PDE4 inhibitors satisfied both Lipinski’s and Veber’s rules for orally bioavailable compounds, while predictions of human intestinal absorption, plasma protein binding and hERG inhibition were all favourable. Both top-scoring compounds were also found to be absent of pan-assay interference structures (PAINS). Finally, SwissTarget predicted these compounds were liable to interact with kinases and proteases, highlighting the importance of undertaking future studies to evaluate the off-target activity of these novel PDE4 inhibitors.

Read the article

EFMC GRANTS – APPLICATIONS DEADLINE IS APPROACHING

EFMC is funding grants for EFMC organised events with the aim to support the participation of young academic scientists. Upon application, a limited number of grants will be covered by EFMC, corresponding to:

To apply for an EFMC grant, please fill in the application form and upload your CV, publication list, abstract, motivation letter, and support letter from the supervisor.

More information, deadlines, and application on www.efmc.info/ysn-grants.

THE LATEST EFMC REVIEW ON THE TRENDS THAT DRIVE INNOVATION IN DRUG DISCOVERY

Just published! The latest EFMC review on the trends that drive innovation in drug discovery is available to readers: 

A wealth of opportunities: Novel tools for chemical biology including chemical inducers of proximity, designer probes or RNA-targeting agents enable innovative tactics for therapeutic approaches. This article explores recent developments combining the power of medicinal chemistry and chemical biology, highlighting their extraordinary potential to address sophisticated biological questions and manipulate complex biological pathways to develop novel therapies.

GET TO KNOW KRISTIINA HUTTUNEN (UNIVERSITY OF EASTERN FINLAND, FINLAND)

In this edition, our #Iamamedicinalchemist is Dr Kristina Huttunen from the University of Eastern Finland.

Get to know her better by reading the interview below:

 

How did you get interested in Medicinal Chemistry?

It happened relatively late, during my first year of bachelor’s studies. I did not plan to continue with chemistry at the university, I never enjoyed that much of organic chemistry in high school, even though it was easy subject to me. I only applied to study chemistry at the University of Jyväskylä, since it was an easy way for me to start my university studies. Then something strange happened during the first year, and I decided to put all my effort into medicinal chemistry (only 10 students per year were selected to have Med.Chem. as the main subject). At that time, I already find it really fascinating, I just didn’t knew it exists before my bachelor’s. I guess I’m a classical example, that you may not know at the age of 18 what you really want to do in your life, and it may still turn out to be ok in the end.

What was the topic of your PhD project?

Design, synthesis, and evaluation of prodrugs for improved and targeted drug delivery. My main project was to improve the oral bioavailability of anti-diabetic agent, metformin via increased permeation, but in my secondary project, I also developed cytochrome P450-bioactivated liver-targeted prodrugs.

Where did you have your postdoc position?

Auckland Cancer Society Research Centre, University of Auckland, New Zealand in Distinguished Professor, Sir William (Bill) A. Denny’s research group, during 2009-2011. I developed novel inhibitors of perforin, a pore-forming cytolytic protein that is associated with several autoimmune diseases.

Where are you currently working and what is your current position?

At the School of Pharmacy at the University of Eastern Finland. Currently, I’m an Associate Professor and I lead the research group called ”Transporter-mediated Targeted Drug Delivery” team (Huttunen lab).

What are your current research interests?

Brain-drug delivery across the blood-brain barrier but also intrabrain distribution of drugs via membrane transporters. But I’m always interested in any kind of targeted drug delivery application to any part of the body.

How would you explain what your research area is to non-scientists?

Drugs are only effective if they are delivered to the right place. They also can be very toxic if they are delivered to the wrong place. To improve the effectiveness and safety of your medicines, I’m developing compounds that can utilize specific membrane transporters (proteins that also deliver sugar to your brain cells) to improve the distribution and exposure of drugs at the target site within the body.

What kind of tasks does your work involve?

These days, mainly writing and reading. Writing grant applications, manuscripts, reports, etc. and reading scientific papers, theses, and other student writings. However, despite all the digitalization, the most valuable tools for me still are the pen and paper, I’ll prefer to design my compounds and write original ideas in my notebook. Of course, supervising and leading a research group involves a lot of different everyday tasks, like being present/available for the group members.

What kind of skills does your work require?

Of course pharmaceutical or medicinal chemistry background is a requirement to understand the basics, however, I’m one of those persons who believes that the right attitude, motivation to learn and readiness to step out of your comfort zone (not fearing the failures) are the keys in your personal success. The needed skills can be learned and improved along with your career. In addition, soft skills, like good communication skills are highly appreciated in any multidisciplinary and multinational research group these days.

How many PhD students and postdocs do you currently supervise?

I have 4 soon finalizing Ph.D. students, 3 recently started Ph.D. students and I also co-supervise 3 Ph.D. students with other group leaders. I also supervise 1 postdoc/senior scientist and 2 technicians and have a handful of ERASMUS and M.Sc. students every year.

Are you currently looking for a new PhD student or a postdoc?

I just recruited a couple of new Ph.D. students, so currently not, but I’m always open to work with Ph.D. students and postdocs who are willing to apply their own funding, e.g., Marie Sklodowska-Curie position.

How would you describe yourself as a supervisor?

Hmmm… easy-going, open-minded, fair but strict, supportive. As I was planning to become a figure skating coach as a teenager, I think I still got it in my veins and my supervision style is quite coaching. I’ll throw the student into the deep end of the pool and then teach them to swim. I always said to my students that I’m learning together with them! 

What do you consider your greatest achievement in your scientific career?

I’m really proud of my current team and the creative atmosphere that we have that supports novel innovations and the growth of young scientists. I think I have come a long and curly way to get to this point and learn a lot about how to lead a research team successfully.

Which of your papers are you most proud of and why?

I probably would say my third J.Med.Chem. paper of L-type amino acid transporter 1 (LAT1) inhibitor as an anti-cancer agent, which was one of my first papers, for which I received funding after my Ph.D., supervised the students who gave their input, and finally I put the results together and wrote the paper. My postdoc Professor Bill Denny said that I should be the first and last author in that one! I almost burst into tears, since it was so true.

https://pubmed.ncbi.nlm.nih.gov/27253989/

What are the features of a successful PhD student or postdoc?

As mentioned above, I highly value the curiousness and motivated attitude over the specific skills. In addition, the soft skills that enable you to work successfully in the research group and scientific community are very valuable.

What advice would you give to someone who wants to know more about your field?

Well, that depends on the background, how much you understand in the first place and what are your possibilities to dig deeper. Attending conferences or having a mentor could be steps for young scientists, but for non-scientists, it is a bit more challenging question…

What would you like to ask from other medicinal chemists?

These days, everyone seems to be overwhelmed with deadlines and unfinished tasks, how do you manage your time and make sure that your brain can also rest and recover?

Have you experienced any unfair situations during your scientific career? How would you advise scientists facing similar situations?

Yes, many times. The academic world can be cruel and people can be greedy. My advice would be that pick up your fights wisely. There is no point to waste time and energy on something that cannot be changed anyway. But make sure that it won’t happen again. Therefore, I try to avoid psychologically toxic environments and people. 

What is the most embarrassing thing you have done in the lab while doing experiments, e.g. explosions?

As a summer intern during my bachelor’s, my supervisor asked me to make anhydrous DMF by using molecular sieves (overnight). I asked her shall I also stir the mixture, and she said yes. In the next morning, I had a nice porridge in my erlenmeyer, since the sieves were completely destroyed due to the stirring. I was just amazed that my supervisor didn’t know this beforehand either.

What are your recommendations for a book, podcast, website, blog, YouTube channel or film?

I’m a bit boring person here, but I would recommend everybody to get distant from their work during their free time. Therefore, I prefer to listen to music, go to nature, play with the kids, etc. and give my brains something refreshing!

Which scientist do you admire the most and why?

Each and every powerful woman in history, like Rosalind Franklin, Marie Sklodowska-Curie, and a Finnish geneticist Leena Palotie-Peltonen. But of course, I respect all the scientists, regardless of gender, who have the passion to increase our knowledge resulting in better healthcare, respect of natural resousources and piece in the world.

Which field of medicinal chemistry do you consider the most promising for the future?

Well, many diseases, and particularly brain diseases, are very complex, with several different mechanisms contributing at the same time. Therefore, I believe that drugs that can affect multiple targets at the same time are highly needed. However, no drug is effective, unless it is delivered to the target site, so in that respect, I believe that achievements in drug delivery applications can be results in real breakthroughs.

What would you expect to be the next major breakthrough in medicinal chemistry?

I would like to believe that we can still go greener in our chemistry and digitalization is a key step in saving our resources. However, to be successful, we still need even more multidisciplinary understanding over different research fields and the ability to communicate at such a level, in which all the actors from different fields can give their greatest contribution to the next real breakthrough for humankind.

BECOME ONE OF OUR INTERVIEWEES

 

Are you a Medicinal Chemist/Chemical Biologist/Computational Chemist?
Are you passionate about science?
Want to be our next interviewee?

Share your story with us by taking our questionnaire:
https://www.efmc.info/interviews-efmc

NEWS FROM THE DIVISION OF MEDICINAL CHEMISTRY OF THE GERMAN CHEMICAL SOCIETY (GDCH)

The German Chemical Society (GDCh) and the German Pharmaceutical Society (DPhG) together with the Austrian Chemical Sociedty (GOeCH) and the Austrian Pharmaceutical Society (OePhG) cordially invite you to attend the annual meeting on ´Frontiers in Medicinal Chemistry´ April 3 - 5, 2023, in Vienna, Austria.

The international symposium will focus on current developments, novel approaches and cutting-edge technologies in the field of medicinal chemistry and drug research with sessions on 

First Disclosures & Medicinal Chemistry Highlights

Molecular Glues & Degraders

RNA-Modifying Enzymes

Translational Science Case Studies

New Chemical Technologies

Young Investigators.

The scientific program will include lectures, and poster presentations. It is the goal of the organizers to have this meeting become an event of scientific excellence, attractive to both industrial and academic scientists in Medicinal Chemistry, Chemical Biology, and related fields of research.

More information and registration will be available here.

NEWS FROM THE FRENCH SOCIÉTÉ DE CHIMIE THÉRAPEUTIQUE (SCT)

The French Société de Chimie Thérapeutique is inviting you to join their thematic meeting: New antiviral strategies: From Bench to Bedside, scheduled on April 19, 2023 in Paris, France.

Registration deadline is March 31, and deadline for poster submission is March 20!

The COVID-19 epidemic of recent years has taught us that a multidisciplinary approach to scientific research is essential for the development of new therapies. The « New antiviral strategies : from bench to bedside» Thematic meeting is at the frontiers of developing new health technologies for the benefit of patients. It will be an opportunity for international experts from two different disciplines, chemistry and biology, to exchange. Also young researchers (PhD students, post-docs..) will be able to present their research work and expand their networks.

More information on https://bit.ly/3IYTA0V.

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

The BMCS is pleased to announce some upcoming events:

  • 7th RSC-BMCS Mastering Medicinal Chemistry
  • 7th RSC-BMCS / SCI Symposium on Ion Channels as Therapeutic Targets
  • 10th SCI/RSC Kinase Symposium on Inhibitor Design
  • 3rd Synthesis in Drug Discovery and Development
  • 3rd RSC Anglo-Nordic Medicinal Chemistry Symposium

7th RSC-BMCS Mastering Medicinal Chemistry

22nd March 2023, Burlington House

Website: https://www.rscbmcs.org/events/mastermedchem23/

Synopsis: Mastering Medicinal Chemistry VII 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.


7th RSC-BMCS / SCI Symposium on Ion Channels as Therapeutic Targets
27th and 28th March 2023, Wellcome Genome Campus, Cambridge

Website: https://www.rscbmcs.org/ionchannels23

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

Website:  https://www.rscbmcs.org/events/kinase/

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

 

3rd Synthesis in Drug Discovery and Development

23rd – 24th May 2023, Virtual

Website:  https://www.rscbmcs.org/events/sddd23/

Synopsis:  Synthesis is at the heart of drug discovery and development. The industry has increasingly demanded higher quality clinical candidates and has sought to exploit less druggable biological targets. Densely functionalised small molecules with a high degree of synthetic complexity are often the result of these demands. Successful programmes therefore require the application of innovative synthesis in all stages of discovery and development. The medicinal chemist’s toolbox is also enhanced by the introduction of novel bioisosteres, often made available only through the application of new synthetic methods. This symposium aimed to celebrate the crucial role of synthesis in the success of drug discovery and development

 

3rd RSC Anglo-Nordic Medicinal Chemistry Symposium

13th-16th June 2023, Hotel Comwell Borupgaard, Snekkersten, Denmark

Deadline for poster abstracts is 4th May 2023

Website:  https://www.rscbmcs.org/events/anmc/  

Synopsis:  Organised with Nordic affiliations, the scientific programme will feature themed lectures, focusing on medicinal chemistry and related technologies and disciplines across a range of drug targets and modalities. A distinguishing feature of this symposium is the collegiate style which encourages an atmosphere of information sharing and learning.

ACSMEDI-EFMC Medicinal Chemistry Frontiers 2023


 

ACSMEDI-EFMC Medicinal Chemistry Frontiers 2023

Early bird fee and OC deadline is approaching!

Register quickly to benefit from reduced rates and submit your abstract before March 16 to be considered for one of the 18 selected Oral Communications.

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
Zagreb, Croatia
IX International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC)

September 7-8, 2023
Zagreb, Croatia
10th EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS)

November 16-18, 2023
Basel, Switzerland
EFMC International Symposium on Chemical Biology (EFMC-ISCB)

EFMC SPONSORED EVENTS

March 22, 2023
London, United Kingdom
The BMCS Mastering MedChem VII: 7th RSC-BMCS symposium on mastering medicinal chemistry

March 27-28, 2023
Cambridge, United Kingdom
7th RSC-BMCS/SCI Symposium on Ion Channels as Therapeutic Targets

April 3-5, 2023
Vienna, Austria
Frontiers in Medicinal Chemistry

April 27, 2023
Hatfield, United Kingdom
34th Medicinal Chemistry in Eastern England (Hatfield symposium)

May 15-16, 2023
Braunschweig, Germany
International Helmholtz Drug Discovery Conference – HDDC2023

May 21-24, 2023
Siena, Italy
IX European Workshop in Drug Synthesis (EWDSy)

May 23-24, 2023
Virtual Event
3rd Synthesis in Drug Discovery and Development

CERTIFIED SCHOOLS

June 19-21, 2023
Santiago de Compostela, Spain
VIII SEQT Summer School

July 2-6, 2023
Urbino, Italy
European School of Medicinal Chemistry (ESMEC)

September 10-15, 2023
Vienna, Austria
Vienna Summer School Drug Design

JOB PORTAL

Postdoc 'Decoding the binding principles of small molecules to RNA', Palacky University, CZECH REPUBLIC
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Postdoctoral position in medicinal chemistry, University of Angers, FRANCE
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Postdoctoral Position in Radiopharmaceutical Development and Preclinical Imaging, University Hospital Basel, SWITZERLAND
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Applications Scientist, Schrödinger, FRANCE
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