MedChemWatch
Monthly Newsletter October 2018

Zoom on some pictures of the « EFMC Photo Competition »!

To celebrate the amazing entries for the 2018 Photo Competition, we will highlight some of the pictures and their creators in coming editions of the MCW.

Can’t wait for more!? Discover them all on https://www.efmc.info/photocompetition

A tablet a day, keeps the doctor away - Ching Xiong Tan

A fun tablet making day!

The “coolest” molecule – Macías Álvaro Lorente

As a PhD student in medicinal chemistry I work modifying the structure of active compounds in an attempt to improve their activity. During the last synthetic step of my kinase inhibitor I changed the nucleophile in order to introduce a variation in the structure and just in this case, the mixture surprisingly froze. As a consequence, I got this beautiful white solid. Medicinal Chemistry never cease to amaze us.

Tiny Frozen Planet to Fight Cancer – Antonio Pereira

When leaving steroid-based hexacyclic compounds to dry overnight, one would always expect a white powder upon returning. Luckily, this reaction flask had different plans, and when I returned to the lab I was able to capture this photo before isolating the final product.

Applications are open for the “EFMC Prize for a Young Medicinal Chemist in Academia/Industry”

The “EFMC Prize for a Young Medicinal Chemist in Academia/Industry” were initiated to acknowledge and recognize an outstanding young medicinal chemist (≤ 12 years after PhD) working in academia or industry within Europe.

The Prizes are given annually and consists of a diploma, € 1.000 and an invitation for a short presentation at an EFMC symposium. Two nominees will also be identified and acknowledged in each category.

The winners of the prizes will be invited to give an oral communication at the 8th edition of the EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC’19), which will be held in Athens, Greece on September 1-5, 2019.

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

Deadline: January 31, 2019

I am a Medicinal Chemist/Chemical Biologist – Vlad Pascanu, University of Zurich, Switzerland

Vlad Pascanu from at the University of Zurich, Switzerland is so enthusiastic about medicinal chemistry that he even dreams about it!
Share with us your medicinal chemistry dreams at communication@efmc.info


Where and when did you obtain your PhD diploma?
I received my PhD in 2016 from Stockholm University, in Sweden.

What was the topic of your PhD project?
We were developing heterogeneous catalysts based on a class of porous materials called MOFs, which were making waves at the time. Interestingly, this topic was almost as new for my supervisor at it was for me. There were many mistakes I’ve made along the way and many lessons to learn, but it was an exciting experience.

How did you get interested in Medicinal Chemistry?
Some of these catalysts I mentioned above were active enough to raise interest from a big pharma company in Sweden. At one point, I got the chance to spend a couple of months in their labs and test my catalyst on their molecules. It was a fascinating experience to see such a vast amount of resources dedicated to science and to curing disease. It was then when I started to think it would be nice to be part of this effort and that this is a topic that would keep me curious for a long time to come.

Where do you work at the moment and what is your current position?
I am currently a postdoctoral researcher at the University of Zurich, in Switzerland. I have been here for about one year and a half now.

What are your current research interests?
We are interested to develop chemical probes that interrogate the function of major transcriptional co-regulators CBP/EP300. These are chromatin-remodeling factors involved in epigenetic regulation with essential roles in healthy embryonic development. However, their precise mechanisms of action and roles in oncologic malignancies are not yet elucidated. We focus on small-molecule inhibitors but also new modalities such as PROTACs and all sorts of other conjugated entities.

What do you like most in your job?
I like to think that our job is to create things (molecules) that have not existed before and use them to answer biological questions that could not be answered before, which is cool. Also, the freedom to test in the lab whatever idea I may have dreamt the night before is a priceless feeling. Another one of the rewards is being constantly surrounded by extremely intelligent people.

What kind of tasks your job includes?
I am spending the better part of my time doing organic synthesis and whatever is left, I spend it on reading, planning and trying to think of new solutions and strategies. I wish I could dedicate more time to that ever increasing pile of “to read asap” literature. However, we are a small group of people with not enough hands in the lab and way too many ideas. I also spend a considerable amount of time trying to prevent my younger colleagues from getting discouraged too quickly. I think that should be part of every postdoc’s responsibilities. Over the next couple of months, I hope I’ll get the chance to spend more time playing with zebrafish. But this all depends on how the synthesis goes.

What kind of skills your job requires?
There are some technical skills required, but I found that I could teach all the practicalities to a student in less than one semester. And these are probably the first skills that will be mastered by automated robo-chemists. Therefore, I cannot rely on that alone for the future. More important is the ability to connect different pieces of information and ask the right questions.

What do you consider your biggest achievement in your scientific career?
For the time being, my future goals are still considerably bigger than my achievements. There were perhaps a few moments when I felt that I must be doing something right. But I would rather answer this question in a few years’ time.

What are the features of a successful PhD student or postdoc?
Resilience is by far the most important. And that rare ability to not lose sight of the bigger picture and of your bigger goals, in the face of daily minor setbacks and obstacles. Then comes curiosity and being open to learn from others. Not least, ethics, in all its forms.

How would you describe yourself as a supervisor?
My experience in this direction is rather limited. There have been a couple of BSc and MSc students for whom I was responsible. If anything, I have learned that I need to work on my patience. Still working on that.

What is the most embarrassing thing you did in the lab while doing experiments?
I don’t think I have ever done something stupid enough to be memorable. Not more than the regular throwing your organic phase to waste or breaking the Dewar and giving everyone a mini-heart attack. Nevertheless, it was quite embarrassing when the cleaning staff found me at 6 a.m. on an inflatable mattress in the middle of our computer room, after I had missed the last metro home.

Which scientist do you admire the most and why?
I would choose Edward O. Wilson for the life-long dedication to his passion, for relentlessly advocating for science, for being a brilliant storyteller and for the energy that he still invests into seeding the same kind of passion in the hearts of young generations of scientists. Books such as “Letters to a young scientist” should be read by everyone, in the darkest moments of their PhD studies.

Did you experience any unfair situations during your scientific career?
Nothing serious. Even though I have spent the previous seven years as an immigrant, I was privileged enough to work in Stockholm and Zurich, which both have a highly developed culture of equality and tolerance, in the society as well as in the lab.

Which paper of yours you are the proudest of and why?
I have not published much during my medchem postdoc and the most interesting work has yet to come out. However, I am proud of a paper recently published from my PhD work (DOI: 10.1021/jacs.8b03505). This was an enormous collaborative effort to portray the entire lifecycle of a catalyst, which we had previously developed. We could take clear snapshots from the bench-stable precatalyst, to activated form in solution, aging into different species that operate through different mechanisms, and finally succumbing to deactivation pathways. It is a whole story from birth to death and it is an empowering feeling to get that kind of detailed insight into a process that you have been struggling to understand for years.

Which field of medicinal chemistry do you consider the most promising in the future?
I’m optimistic about the potential to use deep learning tools to predict pharmacokinetics and toxicity and hopefully reduce to some extent the demand for animal models.

What would you like to ask from other medicinal chemists?
I would be happy to see more medicinal chemists embracing more modern and less wasteful synthetic tools, along with the risks that it implies. Read Jonas Bostrom’s analysis on this topic (DOI: 10.1021/acs.jmedchem.5b01409).

What would you guess to be the next major breakthrough in medicinal chemistry?
I would bet my money on drugs based on new modalities, and in particular targeted protein degraders (PROTACs). They represent a fundamentally different mode of action that could, in theory, target proteins that lack a high affinity ligand or a well-defined enzymatic site. This technology could enable researchers to go after oncoproteins that were previously out of reach with small molecule inhibitors.

Want more stories!? Read them all on https://www.efmc.info/iamamedicinalchemist

Have you heard of the EFMC Young Scientists Network!? If you are under the age of 35, discover how it can help you!

Building a strong network at the very early stage in your career is crucial. Therefore, EFMC decided to create a new network for young scientists: the EFMC-Young Scientists Network

The aim of the EFMC-YSN is to inspire, connect and provide opportunities to medicinal chemists and chemical biologists under the age of 35 by:

  • holding dedicated events & competitions
  • offering awards to best PhDs & Post-docs
  • grants and scholarships to attend EFMC organised and sponsored events
  • providing a forum to exchange, seek advice and mentoring

Shaping itself it into a usefull tool, custom-made to your needs and managed by young scientists, for young scientists.

Join the EFMC-YSN now and get access to the content as it becomes available in the following weeks/months.

Questions? Reach out to us at ysn@efmc.info

Joint EFMC|EuChemS Workshop – Parkinson’s Disease: Causes & Cures – Registration Open

A workshop co-organised by the European Chemical Society (EuChemS) and EFMC, and chaired by Member of the European Parliament Pavel Poc will look at Parkinson’s Disease: Causes and Cures at the European Parliament (Brussels) on November 8, 2018.

Registration is now open! Click here to regsiter and for further information (outline, programme, speakers, abstracts).

The Section of Synthetic Drugs of the Czech Pharmaceutical Society joins the EFMC

The EFMC is thrilled to announce that The Section of Synthetic Drugs of the Czech Pharmaceutical Society has joined the Federation, becoming the 26th National Adhering Organisation of the EFMC.

It represents one more step in the aim of the EFMC to represent medicinal chemistry and chemical bioology societies in every European country, and we look forward to develop strong links with the local Czech scientific community.

We invite you to have a look at their website.

News from the Biological and Medicinal Chemistry Sector (BMCS) of the Royal Society of Chemistry (RSC)

GET THE BUG: 2nd RSC / SCI Symposium on Antimicrobial Drug Discovery

12th to 13th November 2018, SCI, London, UK

Website:  http://www.rsc.org/events/detail/29652/2nd-sci-rsc-symposium-on-antimicrobial-drug-discovery  

Following the first successful event in 2016, this meeting will examine the current state of the art from a medicinal chemist’s perspective.

Coinciding with World Antibiotics Awareness week, a two-day programme of speakers from industry and academia will highlight the challenges associated with discovering and developing new antimicrobials, whilst also showcasing emerging alternative strategies that are being developed to tackle infection.

News from the Division Medicinal Chemistry, Royal Netherlands Chemical Society (KNCV)

Prizes FIGON Dutch Medicines Days – delegate EFMC-YMCS 2019

During the FIGON Dutch Medicines Days, a two-day national symposium on drug development and medicines, the division Medicinal Chemistry of the Royal Netherlands Chemical Society awarded a presentation prize (€ 500) and poster prize (€ 200) to young researchers in medicinal chemistry.

The presentation prize was awarded to Jorick Bruins from the group of Floris van Delft of Wageningen University for the talk entitled ‘Functionalization of tumour-targeting antibodies via enzymatic oxidation of tyrosine to 1,2-quinones’.

In his PhD study he has developed a new method of rapid, site-selective and high-yielding conjugation by enzymatic oxidation of the phenol moiety in tyrosine residues expressed at the termini of antibodies to a quinone. Cycloaddition results in stable conjugation of a selected probe to an antibody with yields of over 95%.

Jorick Bruins will be the Dutch delegate for the EFMC-YMCS 2019 in Athens, where he will present his results obtained in his PhD study.

The poster prize was awarded to Tasia Amelia from the group of Ad IJzerman of Leiden University for the poster entitled ‘Revealing the activation mechanism of human adenosine A2A receptor by non-ribose ligands’. In her PhD study she synthesized several derivatives of LUF5833 and tested their affinity in order to understand the importance of structural determinants in the activation of the human adenosine A2A receptor.

News from EuChemS’ Young Chemists’ Network

The 2nd edition of the video contest Chemistry Rediscovered is now open/  It is organized by EYCN and celebrates the International Year of the Periodic Table in 2019.


The theme of this year is In your element”. For this competition, young chemists (12-35 years old) are challenged to make a creative 90 seconds video related to one or more elements of the periodic table. The competition is open, and videos can be submitted until the 31st of January 2019.

All participants of the competition will receive a copy of the EuChemS Periodic Table, specially designed for the International Year of the Periodic Table. In addition to that, they have a chance to win other Periodic Table-related goodies and the overall winner(s) will be invited to Paris in July 2019, for the 47th IUPAC congress.

All the detailed information can be found in the Rules and Regulations document.

For any further questions, don’t hesitate to contact the project leader, Yacintha Vermeer (yacintha@yacintha.nl).

Highlighted MedChemComm's article - What are the drugs of the future?

Are small molecules or biologics the drugs of the future? Small-molecule drugs have historically been the pillars of traditional medicine. However, recently, we seem to be amidst a scientific revolution with the rise of many FDA-approved biologic drugs.

This opinion article looks at the current state of small molecules and biologics and assesses what the future holds for these two broad classes of drugs.

Read the article!

The latest edition of MedChemComm, the official journal of the EFMC, is available at:

MedChemComm

 

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EFMC SPONSORED EVENTS

November 12-13, 2018
London, United Kingdom
2nd SCI/RSC Symposium on Antimicrobial Drug Discovery

JOB PORTAL

Associate Principal Scientist – Medicinal Chemist, Astrazeneca: Medicinal Chemistry Respiratory, Inflammation & Autoimmunity iMed, Gothenburg, Sweden

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Senior Research Scientist – Synthetic/Medicinal Chemistry, Astrazeneca: Medicinal Chemistry Respiratory, Inflammation & Autoimmunity iMed, Gothenburg, Sweden

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