MedChemWatch
Monthly Newsletter September 2018

Photo Competition - Reality of Medicinal Chemistry - Winners announced!

The Communication Team is delighted to announce the winner and two runners-up of the 2018 Photo Competition "Reality of Medicinal Chemistry":

We are thrilled by the success of this first edition of the competition, which attracted 78 applications, 1500 online votes during the first round and around 200 votes at the EFMC-ISMC 2018 for the final selection!

Congratulations to all the contestants for their participation! All the pictures will be published in the 2019 edition of the EFMC Yearbook, and will be displayed in the future editions of the MedChemWatch.  

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 on 8 November 2018.

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

Parkinson’s is a progressive neurodegenerative disorder having no known cause, typically with onset later in life. Prevalence in the 60-69-year-old population is estimated to be approximately 1.0%, rising to 2.7% in those over 80. There are more than one million people living with Parkinson’s today in Europe; with an ageing population this figure is forecast to double by 2030. The condition is characterised by difficulty in moving and tremor, as well as psychiatric issues. It leads to a progressive reduction in the quality of life and those affected require increasing care. This imposes a significant socioeconomic burden which currently amounts to €13.9 billion of healthcare expenditure annually.

There is no cure for Parkinson’s yet. The current ‘gold standard’ medication, levodopa, was introduced in 1967, with few new therapeutic agents being registered since then. As such, there is an urgent need to develop new and better treatments. However, despite clinical strategies remaining largely unchanged over the past 50 years, our understanding of the disease mechanisms in Parkinson’s has advanced dramatically, revealing novel druggable targets. Hence, the disorder is in need of extra investment to translate these exciting opportunities into life changing therapies for patients.

In addition to genetic mutations, a potential risk factor for Parkinson’s disease is exposure to some toxins or herbicides, including diquat. In 2015, the European Food Safety Agency (EFSA) declared the herbicide to be potentially harmful and indicated it should be banned. The European Commission did not submit the proposal to the ScoPAFF, and invited EFSA to revise its opinion.

The workshop aims to look at the causes of Parkinson’s disease as well as possible ways forward, both clinically, but also on a political level, notably through the upcoming Horizon Europe research framework programme.

I am a Medicinal Chemist/Chemical Biologist – Laura Heitman, LACDR, Leiden University, The Netherlands

This week we introduce you to the story of Laura Heitman (LACDR, Leiden University, The Netherlands), who is a runner up for the EFMC Young Medicinal Chemist in Academia prize.

How did you get interested in Medicinal Chemistry?
As a bachelor student I followed a course on “Design and Synthesis” (Ontwerp & Synthese in Dutch), and the idea that a small molecule can modulate a large protein intrigued me.

Where and when did you obtain your PhD diploma?
Department of Medicinal Chemistry, University of Leiden, The Netherlands in April 2009.

What was the topic of your PhD project?
“Allosteric modulation of ‘reproductive’ GPCRs”

Where did you have your postdoc position?
I didn’t – I was able to obtain a tenure track assistant professorship immediately after my PhD.

Where do you work at the moment and what is your current position?
Division of Drug Discovery and Safety, University of Leiden – Associate Professor (Tenured).

What are your current research interests?
Novel concepts to target GPCRs, such as allosteric modulation and target binding kinetics.

What do you like most in your job?
Teaching, supervising and mentoring the next generation, i.e. bachelor, master and PhD students.

What kind of tasks your job includes?
My job is quite diverse, which I like very much. It consists of research, teaching and management.

What kind of skills your job requires?
In my opinion: enthusiasm, curiosity and flexibility.

What do you consider your biggest achievement in your scientific career?
That so far nine of my PhD students have graduated in time, all resulting in PhD theses to be proud off.

Are you currently looking for a new PhD and postdoc students?
My group currently consists of six PhD students, one PostDoc and a technician.
I currently don’t have a vacancy, but that can change. Of course, I am interested to host excellent people when they can secure their own funding, e.g. Marie Curie Fellowship.

What are the features of a successful PhD student or postdoc?
Enthusiasm, perseverance, curiosity (good experimental and writing skills)
How would you describe yourself as a supervisor?
Enthusiastic, structured, empathic

What is the most embarrassing thing you did in the lab while doing experiments, e.g. explosions?
Ow, I once broke a tabletop centrifuge, because I did not distribute the epp cups evenly. It even caused the fire alarm to go off…

Which scientist do you admire the most and why?
Prof Ad IJzerman. He was my PhD supervisor, and still is my mentor. I admire how he build his group to contain all features of medicinal chemistry (i.e. organic chemistry, computational chemistry and molecular pharmacology). Moreover, he is able to keep the atmosphere in his group friendly and social (while science can be quite competitive and stressful at times).
In general, I admire scientist who are able to combine a family with a scientific career. I know from my own experience that this is quite a challenge.

Did you experience any unfair situations during your scientific career?
Luckily not.

Which paper of yours you are the proudest of and why?
I am currently most proud of my Nature paper in 2016 in collaboration with UCSD (Prof Handel lab). In general, I am most proud of the papers resulting from (interdisciplinary) collaborations.
Which field of medicinal chemistry do you consider the most promising in the future?
I think that any field taking the desired in vivo pharmacology in mind is promising. This sounds trivial, but is often lacking.

What would you like to ask from other medicinal chemists?
How they would describe the field of ‘Medicinal Chemistry’, or how they feel they contribute to the field of ‘medicinal chemistry’.

What would you guess to be the next major breakthrough in medicinal chemistry?
I am biased of course, but a major breakthrough would be when a small molecule designed to have optimal target binding kinetics reaches the market. So far, some marketed drugs have been shown in retrospect to be efficacious due to optimized target binding kinetics. Having a ‘prospective’ example would really be a breakthrough (further) supporting the importance of this concept.

EFMC is supporting the International Year of the Periodic Table of Chemical Elements 2019 (IYPT2019)

We are very proud to relay the new EuChemS Periodic Table depicting the issue of element scarcity on the occasion of the upcoming International Year of the Periodic Table of Chemical Elements 2019 (IYPT2019).

The EFMC shares their hope that this image will lead to reflection, and ultimately action, that it will raise awareness of the threat this poses and also hope to see it have an impact on policy, education and on individual actions. 

The Periodic Table has a lot of potential, and could be disseminated in an effective way by providing schools, universities and wider networks with it, whether in hard copies or electronically. Please feel free to also use it to print onto various merchandise items, such as T-shirts, bags, ….

The Periodic Table is now freely downloadable in high resolution on EuChemS’ website. The work is licensed under the Creative Commons Attribution NoDerivs CC BY-ND.

Support notes, which explain in more detail how the Periodic Table has been designed, and which also include some questions for students, will soon be available for download on our website. Versions in other languages are to be developed.

We strongly encourage you to share it as widely as possible (website, social media, …).

If you have any questions, please contact the EuChemS Secretariat at: secretariat@euchems.eu

EFMC Awards 2018 - Ceremony

The 2018 Award Ceremony took place during the XXV EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2018), held on September 2-6, 2018 in Ljubljana, Slovenia.

Nauta Pharmacochemistry Award for Medicinal Chemistry and Chemical Biology

    

Prof. Christa Müller – University of Bonn, Germany

For her extensive contribution to the field of adenosine and purinergic receptors, from the design of novel ligands to the study of their therapeutic potential, and for her support of the European Medicinal Chemistry community. Dr. Müller is a highly cited scientist who has developed a number of tool compounds now used by many labs around the world. She has set up numerous international collaborations, and is a co-founder of the Pharmacenter in Bonn. Her noted contributions to the Medicinal Chemistry community include continued editorial and advisory duties, educational initiatives, and the organization of international conferences.

After the ceremony on Sunday September 2, Prof. Christa Müller gave a lecture on: Tools and Drugs for Purine Targets - Important Players in Inflammation and Cancer


UCB-Ehrlich Award for Excellence in Medicinal Chemistry

   

Prof. Adam Nelson – University of Leeds, United Kingdom

For his ground breaking work to explore novel chemical space, especially natural product-like, diversity-oriented and activity-directed synthesis.  Prof. Nelson implemented his vision that chemical synthesis should align with drug discovery needs, and introduced methods that have been taken up by the medicinal chemistry community to profile synthetic targets for lead-likeness and chemical novelty. He plays an important role in the European Lead Factory, chairing its Library Selection Committee, and leads the “Next Generation Chemistry for Medicine” theme at the Rosalind Franklin Institute, in the UK.

On Monday September 3, Prof. Adam Nelson gave a lecture on: How Best to Discover Bioactive Small Molecules? 


Prous Institute-Overton and Meyer Award for New Technologies in Drug Discovery

   

Prof. Benjamin Cravatt – Scripps Research Institute, USA

For his major contribution to the development of chemical proteomics, and in particular the introduction and refinement of the activity-based protein profiling (ABPP) technology. This novel approach allows the study of enzyme function in complex systems: This, and the efforts of Prof. Cravatt to identify tools for chemical biology, led to the identification of novel therapeutic targets for the treatment of human diseases of the central nervous system.

On Tuesday September 4, Prof. Benjamin Cravatt gave a lecture on: Activity-Based Proteomics - Protein and Ligand Discovery on a Global Scale

Photographer - Fabien Venturi
Contact: venturifab@yahoo.fr

EFMC Prizes 2018 - Ceremony

The 2018 Prizes have been conferred during EFMC-ISMC 2018 in Ljubljana, Slovenia.

The « EFMC Prize for a Young Medicinal Chemist in Academia » and the « EFMC Prize for a Young medicinal chemist in Industry » have been established by the EFMC to acknowledge and recognize an outstanding young medicinal chemist working in academia or in industry within Europe.The prizes are given annually and consist of a diploma, 1.000€ and an invitation for a short presentation at an EFMC Symposium. Two runners-up are also identified and acknowledged.

Winner of the Industry Prize was Marton Csékei (Servier Research Institute of Medicinal Chemistry, Hungary), and he gave a talk on the “The Challenges of Restoring Programmed Cell Death Through MCL1 Inhibition”. The most meritorious runner-up was Giovanni Bottegoni (Heptares Therapeutics, United Kingdom).


Alexander Titz (HIPS Saarbrücken, Germany) won the 2018 EFMC Prize for a Young Medicinal Chemist in Academia. At the EFMC-ISMC Symposium, he gave a talk entitled “Carbohydrate-binding Proteins as Targets for Anti-Infectives and Diagnostics: ESKAPE pathogen Pseudomonas aeruginosa and its Lectins“. Markus Muttenthaler (University of Vienna, Austria) and Laura Heitman (LACDR, Leiden University, The Netherlands) have been identified and acknowledged as runners-up.

   

Photographer - Fabien Venturi
Contact: venturifab@yahoo.fr

The 10 EFMC Best Poster Prizes at EFMC-ISMC

The EFMC is pleased to announce the recipients of the 10 "EFMC Best Poster Prizes"

The EFMC is pleased to announce the recipients of the 10 "EFMC Best Poster Prizes"

 « Read more »

 

  • Lisa Barbaro, Monash University, AU
  • Emma Evertson, AstraZeneca, SE
  • Niels Hauwert, Vrije Universiteit Amsterdam, NL
  • Jan Hellmann, FAU Erlangen-Nuremberg, DE
  • Christina Lamers, University of Basel, CH
  • Grant McGonagle, GlaxoSmithKline,UK
  • Janez Mravljak, University of Ljubljana, SI
  • Vlad Pascanu, University of Zurich, CH
  • Elisabeth Rexen Ulven, University of Southern Denmark, DE
  • Céline Ronin, NovAliX, FR

Each poster prize consist of a diploma, a 200€ prize and a one year free subscription to MedChemComm, the official EFMC journal.

The prizes were awarded at EFMC-ISMC 2018 in Ljubljana.

Congratulations to all the 10 worthy candidates!

Photographer - Fabien Venturi
Contact: venturifab@yahoo.fr

EFMC Roche Studentships 2018

The sixth EFMC-Roche studentships have been announced by Yves P. Auberson (EFMC) and Hayley Binch (F. Hoffmann-La Roche) at the EFMC-ISMC 2018.

The recipients were Miroslav Kosar (University of Edinburgh, UK) and Michael Bogdos (University of Strathclyde, UK). We would like to congratulate both of them for their fantastic achievement.

One of the goals of the EFMC is to enhance interactions at the industry/academia interface and to promote improved cooperation between the pharmaceutical industry and academia. EFMC and F. Hoffman-La Roche therefore proposed an opportunity to broaden the awareness to European University based chemistry students of the EFMC activities by rewarding excellence accomplished during a medicinal chemistry internship in industry.

EFMC would also like to thank F. Hoffman-La Roche for their contribution and support.

To find more about the EFMC Prizes and studentships, we invite you to visit the EFMC website https://www.efmc.info/roche_studentship

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

Congratulations to Anthe Janssen who received the Public’s Choice Prize at EFMC-YMCS 2018.

At the EFMC Young Medicinal Chemist Symposium in Ljubljana the “Public’s Choice Prize” for the best presentation was awarded to Anthe Janssen of the group of Mario van der Stelt of Leiden University in The Netherlands.

The title of his talk was ‘Synthesis and biological evaluation of BIA 10-2474: an irreversible and aspecific FAAH inhibitor’. In his PhD study he investigated the FAAH inhibitor BIA 10-2474 that caused death of one volunteer in a phase 1 trial. By using activity-based proteomic methods he showed that the drug inhibits several lipases, which are not targeted by another clinically tested FAAH inhibitor.

Anthe Janssen was The Netherlands representative at EFMC-YMCS 2018 as winner of the national presentation prize in a session medicinal chemistry at the FIGON Dutch Medicines Days 2017, a two-day national symposium on drug development and medicines.

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.

 

ISSUE SPONSORED BY


MercachemSyncom is the leading European drug-discovery contract research organization for solving your chemistry challenges. From the design and synthesis of small-molecules to delivery of the first GMP batches. For over 25 years we blend vast scientific knowledge and inventiveness to make great leaps on your behalf. We go further to unlock new potential.

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EFMC SPONSORED EVENTS

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

EFMC SPONSORED SCHOOLS

September 19-21, 2018
Rimini, Italy
Summer School in Pharmaceutical Analysis (SSPA)

October 7-12, 2018
Leysin, Switzerland
13th Swiss Course on Medicinal Chemistry

JOB PORTAL

MsC student or PhD internship, KU Leuven: Cellular and Molecular Medicine, Leuven, Belgium

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