The competition has been a great success, attracting 64 applications with 1300 online votes for the first round and around 200 votes at the EFMC-ASMC'19 for the final selection!

Congratulations to all the contestants for their participation! All the pictures will remain available on the EFMC website, and some will be displayed in the future editions of the MedChemWatch.

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 Radka Snajdrova (Novartis Pharma, Switzerland) and she gave a talk on the “Cipargamin-Biocatalysis in the Discovery and Development of an Antimalarial Drug”. The most meritorious runners-up were Jo Alen (Grünenthal, Germany) & Jacob Bush (GSK, United Kingdom).

Andreas Koeberle (Friedrich-Schiller-University Jena, Germany) won the 2019 EFMC Prize for a Young Medicinal Chemist in Academia. At the EFMC-ASMC’19 Symposium, he gave a talk entitled “From the Elucidation of the Mechanism of Vitamin E to the Design of Innovative Drugs that Limit Inflammation and Enhance Resolution“. Anna Katharina Hirsch (HIPS, Germany) & Kamil Musilek (University of Hradec Kralove, Czech Republic) have been identified and acknowledged as runners-up.

Photographer - Fabien Venturi
Contact: venturifab@yahoo.fr

How did you get interested in Medicinal Chemistry?

Medicinal chemistry is the start of an incredibly long and complex story about getting a drug to the patient. I find being involved at the ‘birth’ of the project and being able to influence and impact how this molecule is made from such an early stage, whilst always keeping an eye on maintaining flexibility and optionality for future production scale, to be fascinating role.

Where and when did you obtain your PhD diploma?
In 2007 – it was a joint program between Vienna University of Technology and University of Chemistry and Technology in Prague.

What was the topic of your PhD project?
Asymmetric Baeyer-Villiger Oxidations using 2nd Generation Biocatalysts.

Where did you have your postdoc position?
1st York Structural Biology Laboratory, University of York, UK as Erwin-Schrödinger Fellow
2nd Dept. of Biotechnology and Enzyme Catalysis, Greifswald University, Germany

Where do you work at the moment and what is your current position?
Novartis Institute for Biomedicinal Research, as a group leader focused on driving progress and adoption of biocatalysis across the entire portfolio and at all stages in a compounds evolution.

What are your current research interests?
Biocatalysis is a subject that I believe has huge value for the synthesis of complex molecules, complementing traditional organic chemistry and providing a way for the pharma (and broader chemical industry) to change their image to one of an industry focused on sustainability and positive environmental impact. My research interests revolve around finding game changing biocatalysis solutions for the production of API’s, which we achieve through application of existing technologies and a constant drive to expand and develop the science though techniques such as protein engineering and bio-conjugations.

What do you like most in your job?
I find the scientific creativity and constant innovation to be very satisfying. Looking at a route and working with synthetic teams to reimagine what’s possible creates an energy and motivation to succeed that is addictive! There is a strong angle on people development in my role that occurs when people engage with biocatalysis and want to learn more and participate in what is naturally a very multi-disiplinary science, operating across a very wide research area.

What kind of tasks your job includes?
Discovery and implementation of novel and established biocatalysis technologies into drug discovery/development, which of course results in the ultimate goal of offering access to late-stage functionalisation capabilities, and the ability to support the drug development process in many tangential ways, such as the synthesis of metabolites. As a group leader, I have line management and various leadership roles, which broaden my role into many other aspects of the Novartis business, into areas as diverse as leading the promotion team, evaluating ‘strategic joint ventures with academic/industrial counterparts and leading a team of people to develop transformational science.

What kind of skills your job requires?
You need to love what you do – as in any field of science the progress is rapid and so staying on top of that becomes a lifestyle rather than a ‘job’! Following the literature, building networks and relationships and constantly looking for opportunities to apply the science is key. Equally being realistic and knowing the limitations of what is possible is key to maintaining credibility :)
Additionally, my job involves dealing with people from many disciplines and backgrounds at various levels in their career, so empathy, an open mind and good listening and communication skills are all vital (maybe a good dose of patience as well)!

What do you consider your biggest achievement in your scientific career?
Outside of being selected for this prize, which I view as an amazing honour, last year our team created a proposal for, and won a “Genesis Labs” award. This is a global competition for independent scientific pursuit, sponsored by Novartis, with the goal of delivering transformational science. We are currently half way through the project, in a very exciting phase.

How many PhD and postdoc students do you have at the moment?
Within my group are many highly experienced researchers who have attained academic excellence at different levels from apprentice to multiple post-docs, and who continue to grow their knowledge and capabilities on a daily basis, solving problems which directly impact the value of the Novartis portfolio. Outside of Novartis I lead a number of academic collaborations, including cooperations with PhD and postdoc students, as well as undergraduate lab courses in the local university.

What are the features of a successful PhD student or postdoc?
What separates a good from a great student is someone who has developed the confidence in their abilities to conduct independent research but maintains a critical internal ‘review process’ so they know when to keep pushing through a challenge or realise a topic is no longer worth pursuing. Being enthusiastic, a good communicator, resilient and supportive of others are all features that make a researcher, at any level, successful in their field. People who understand the impact and purpose of their research always seem to find the ability to ‘keep pushing through’ much better than those who are less involved in the bigger picture of what they are contributing towards.

How would you describe yourself as a supervisor?
I would like to think my team finds me to be the person they can come to when they have a problem, a success or a question. I prioritise finding time to listen to my team, understand their objective/motivation and finding ways to support them as they develop personally and professionally. Seeing people achieve what they thought was impossible, deliver excellence and enjoying their job is what makes me the happiest.

What is the most embarrassing thing you did in the lab while doing experiments, e.g. explosions?
I think as a researcher, we all have a little bit of a ‘cowboy’ in us and sometimes the drive to get things done quickly overcomes our more rational selves.. leading most people to have had a least a little drama in the lab – I created a little excitement one morning when washing out unreacted sodium from a Birch reactions into the sink...
I also seem to be on a bit of a roll currently with embarrassing acts outside the lab involving pouring coffee over myself, or my boss, or his boss... I don’t think I’m clumsy, but sometimes I gesticulate a little too much with my hands...

Which scientist do you admire the most and why?
Prof. Uwe Bornscheuer! My postdoc boss, he is a wonderful and kind person, 1st class scientist and has a great sense of humor!

Did you experience any unfair situations during your scientific career?
On being awarded a postdoc fellowship, I was told by several of my peers that I had won it only because I am woman.
That had a huge impact on me, as until that point I only considered my competition to be better scientists, and progression or recognition being awarded solely on that basis. When I heard comments around my fellowship being awarded on the basis of political or optical reasons, I found it very unfair. Taking a step back from this, when listening to feedback from the grant agency about the exceptional quality of my scientific proposal and knowing the effort I put in during the two months time it took to write it, I was able to disconnect myself from comments which I attribute to ‘sour grapes’ and an outdated mentality. There will always be situations that can be interpreted as being unfair, I only hope it’s not me causing it or that I have the strength of character to get past it.

Which paper of yours you are the proudest of and why?
The one I’m currently writing – a tutorial review. Being able to bring together a whole subjects worth of science in a comprehensive and easily accessible manner, building interest in the topic and sharing my enthusiasm for it is a great reward for the pain of summarising and coherently bringing together 1’000’s of papers and decades of research!!

Which field of medicinal chemistry do you consider the most promising in the future?
Medicinal chemistry is the start of the drug development process – it is a wonderfully multidisciplinary field of science and needs to solve many problems. I am always keen and motivated to find ways to leverage the work and results generated by medicinal chemistry teams in later stage development and finding technologies that are as applicable to the development chemist, as they are the medicinal chemist, builds in a layer of efficiency and effectiveness that streamlines the drugs development and production. Anything that supports this broadly applicable and scalable technology creation and adoption is going to deliver meaningful results in any organisation.

What would you like to ask from other medicinal chemists?
As a medicinal chemist you have the pressure to deliver to sometimes near impossible timelines, but please take a chance sometime to try biocatalysis and see what it can do for you and your project! You won’t be disappointed :)

What would you guess to be the next major breakthrough in medicinal chemistry?
Utilising the advances we have made in understanding topics such as protein folding and SAR I see the future of rationale based drug design being very bright.

How did you get interested in Medicinal Chemistry?

After studying biochemistry, it was actually our current DPhG president, Prof. Dr. Laufer, and my later supervisor, Prof. Dr. Werz, who rose my interest in this fascinating field.

Where and when did you obtain your PhD diploma?
2009 in Tübingen under supervision of Prof. Dr. Oliver Werz

Where did you have your postdoc position?
In the lab of Takao Shimizu at the University of Tokyo.

Where do you work at the moment and what is your current position?
I am currently group leader and head of the lipidomics facility at the Chair of Pharm./Med. Chemistry in Jena but I will move on October to the Michael Popp Research Institute at the University of Innsbruck, where I was offered a position as professor.

What are your current research interests?
By studying lipid signaling pathways using chemical probes, we aim to identify new drug targets, phytopharmaceuticals and bioinspired lead structures at the interface of cancer, inflammation and homeostasis.

What do you like most in your job?
To confirm revolutionizing hypotheses in collaborative efforts.

What kind of skills your job requires?
First of all, enthusiasm combined with patience and endurance.

Are you currently looking for a new PhD and postdoc students?
My team of four PhD students will expand in the near future, and we are currently looking for highly motivated PhD and postdoctoral students.

Which field of medicinal chemistry do you consider the most promising in the future?
I do not think that a single field will stand out but believe that interdisciplinary interactions within medicinal chemistry, chemical biology and beyond will be the key.

What would you guess to be the next major breakthrough in medicinal chemistry?
The dawn of OMICS screening platforms.

• Fabian Hulpia (University of Ghent, Belgium)
DISCOVERY OF 7-ARYL-7-DEAZAPURINE 3’-DEOXYRIBOFURANOSYL NUCLEOSIDE ANALOGUES AS ANTI TRYPANOSOMA CRUZI AGENTS

• Femke Meijer (Eindhoven University of Technology, The Netherlands)
SMALL MOLECULE MODULATION OF THE NUCLEAR RECEPTOR RORγt VIA A NOVEL, ALLOSTERIC BINDING SITE

• Vasiliki Pardali (National and Kapodistrian University of Athens, Greece) 
TOWARDS THE DEVELOPMENT OF NOVEL ANTI-HBV AGENTS: BLOCKAGE OF VIRUS REPLICATION BY N-HYDROXYIMIDES, THROUGH INHIBITION OF RIBONUCLEASE H

• Naoya Shindo (Kyushu University, Japan) 
SELECTIVE AND REVERSIBLE MODIFICATION OF KINASE CYSTEINES WITH CHLOROFLUOROACETAMIDES

• Rhia Stone (University of Queensland, Australia) 
FLUORESCENT MACROLIDE PROBES FOR EXAMINATION OF ANTIBIOTIC RESISTANCE

Each poster prize consists of a diploma, a 200€ prize and a one-year free subscription to MedChemComm.

Congratulations to all the 5 worthy candidates!

Photographer - Fabien Venturi
Contact: venturifab@yahoo.fr

According to the cooperation framework agreement within the MoU signed by CPA and the European Federation for Medicinal Chemistry (EFMC) in Manchester 2016, the CPA-EFMC International Symposium on Medicinal Chemistry (CPA-EFMC ISMC) was held concurrently.

The theme of CMCS2019 was “New targets, new technologies and new molecules” boosting the discovery and translation of original new drugs”, and that of CPA-EFMC ISMC was “Exploring new pathways to tackle immune-oncology”. The conference had 12 topics in form of satellite meetings with keynote, invited and oral communications distributed in parallel sessions as well as poster sessions along with informal discussions, providing an excellent platform for communications between researchers in the relevant fields, promoting the exchange and collaborations, and boosting the development and application of medicinal chemistry. The symposium attracted more than 3000 participants from academia and industry.

The EFMC session devoted to immune-oncology was held in the main Ballroom of the Century City Convention Centre which was almost full with more than 2000 attendees. The main session was chaired by the EFMC Treasurer Antoni Torrens and started with the opening remarks of the CPA Symposium Chair Kaixian Chen, and the EFMC President Yves P. Auberson who introduced the EFMC and its activities aimed to promote medicinal chemistry and chemical biology.

The session continued with three outstanding keynotes lectures by Weiping Zhou from Michigan University, Luc Van Hifte from Mercachem-Syncom and Norbert Schmees from Bayer. The speakers showed three alternative pathways to tackle immune-oncology such as ferroptosis, tankyrase inhibitors and small molecules aryl hydrocarbon receptor (AhR) inhibitors.

During the Conference the main CPA and EFMC officials had a working lunch meeting where they discussed the future of the MoU and unanimously committed to continue the interactions and activities aimed to strength the collaboration between both Associations. After this successful event a CPA session is planned to be held in EFMC-ISMC 2020 Symposium in Basel.

The EFMC thanks the speakers for their inspiring talks and the symposium organization for the great job done and for the warm and excellent treatment they provided.

 Report by Dr Antoni Torrens (Esteve Pharmaceuticals, Spain)

The Prize has been established by a generous gift from the Chemical Works of Gedeon Richter, Plc. (Budapest, Hungary) to acknowledge the key role that medicinal chemistry plays toward improving human health.

Applicants should be received by NOMINATION only, with just one person needing to serve in that capacity, although a total of five (5) individuals should be listed as referees overall. The package must be submitted electronically and should contain a complete resume, a professional autobiography of not more than two pages, and a one-page summary of what the individual considers to be his/her activities, accomplishments and/or publications that have had the most significant impact upon the field of Medicinal Chemistry. The material will be forwarded confidentially to an independent selection committee appointed by the IUPAC Subcommittee on Medicinal Chemistry and Drug Development.

For further information please contact Prof. Janos Fischer, Chairman of the IUPAC Sub-committee on Drug Discovery and Development, by email at j.fischer@richter.hu

Nomination materials should be uploaded by 15 December 2019 to IUPAC Secretariat via the following form

https://www.cognitoforms.com/IUPAC1/IUPACRichterPrize2020NominationForm

This year, the symposium will delve into the developments in the therapeutic use of peptides.

Confirmed Speakers

• Linkers for Peptide Conjugation
   Prof. Fernando ALBERICIO
   UNIVERSITY OF KWAZULU-NATAL, Durban, South Africa

• Synthetic Immune System Engagers – a Peptide-based Approach to Immune-oncology
   Prof. Christian F.W. BECKER
   UNIVERSITY OF VIENNA, Wien, Austria

• Macrocyclization as an Enabling Tool Toward Novel Peptide Drug Candidates
   Prof. Eric MARSAULT
   UNIVERSITY OF SHERBROOKE, Sherbrooke, PQ, Canada

• Targeting Receptor Complexes: A New Dimension in Drug Discovery
   Prof. Kristian STROMGAARD
   UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark

• Gate2Brain, Opening the Gate to CNS Therapies
   Dr Meritxell TEIXIDO
   INSTITUTE FOR RESEARCH IN BIOMEDICINE, Barcelona, Spain

Deadlines:
Poster submission & early-bird fee: 10th October

For more information, please visit: www.medchem.be
Share the word on social media using the #MedChem2019

SEQT Congress 2019 was attended by 100 participants from different countries: 87% from Spain, 8% from five EU countries, and 5% from three non-EU countries. The four day meeting, with many scientific highlights (12 invited speakers, 17 oral communications, and 36 flash presentations), got 40% trainee registrations (20 supported by the SEQT as a part of the young scientist support program), and 13% participants were from industry. 

The aim of the symposium is to illustrate the great potential and applications of RNA-targeting modalities in contributing to therapeutic innovation. This meeting is dedicated to a large audience of organic and medicinal chemists, biochemists and biologists from academic and industry. During this day, we will focus on recent advances in the field of RNA targeting using small molecules as well as oligonucleotides: the synthetic challenges involved in the design of RNA-targeting agents and on the validation of relevant RNA targets, as well as on the current methodologies used to study RNA/ligands interactions. RNA has already been drugged. Ribosomal RNA was drugged serendipitously with natural product antibiotics and later linezolid. A design-driven approach to drugging RNA was achieved with antisense oligonucleotides (ASOs) and then by RNA interference (RNAi) mechanisms.

More recently, small molecules that bind to the FMN riboswitch and to SMN2 pre-mRNA were reported and are close to clinical application. All those recent developments in the field of RNA-targeting definitely hold promise for future therapeutic applications.

List of confirmed speakers:

Matthew DISNEY (Scripps, Florida, USA): “Translating RNA sequence into lead small molecule medicines.”
Maria DUCA (Université Côte d’Azur, France): “Synthetic small-molecule RNA ligands : Scope and applications”
Mélanie ETHEVE-QUELQUEJEU (Université de Paris, France): “Modified RNAs as Molecular Tools for Structural and Functional Studies of RNAs dependents Enzymes”
Eric ENNIFAR (Université de Strasbourg, France): "Structure-guided discovery of novel ligands targeting the HIV-1 genomic viral RNA"
Jonathan HALL (ETH Zurich, Switzerland): “A Bright Future for Oligonucleotide Drugs”
Gerhard MUELLER (Gotham Therapeutics, Germany): “Epitranscriptomic readers, writers, and erasers: a biophysics and medicinal chemistry perspective”
Alleyn PLOWRIGHT (Sanofi-Aventis Deutschland GmbH, Germany): “Modulating RNA - recent drug discovery approaches and opportunities for diverse modalities”
Helene TRAN (Servier Research Institute, France): “Antisense Oligonucleotides Therapeutics for CNS Disorders”

Link for registration: http://www.sct-asso.fr/fall_one_day_symposium.html

BMCS HALL OF FAME: LAST CHANCE TO NOMINATE YOUR MEDICINAL CHEMISTRY HEROES

The BMCS Hall of Fame aims to recognize prominent chemists for outstanding, sustained, contributions to any area of interest to the BMCS. This is an Individual award to recognize prominence and significant, sustained, scientific impact in the field of medicinal chemistry, agriscience or chemical biology, including teaching excellence, outstanding contributions to the BMCS, or any combination thereof.

Nominations should be submitted by 30^th September 2019
For more information go to https://www.rsc.org/Membership/Networking/InterestGroups/BMCS/Activities/HallofFame.asp

20 Years of the Rule-of-Five symposium
20^th November 2019, Sygnature Discovery, Nottingham, UK
The call for poster abstracts will close on 6^th October
Website:  http://www.rsc.org/events/detail/39112/twenty-years-of-the-rule-of-five

Synopsis: This symposium will bring together researchers from a number of different areas of drug discovery and will provide a historical overview of the use of Lipinski’s rules, as well as looking to the future and how we use these rules in the changing drug compound landscape.

6^th  RSC / SCI symposium on Ion Channels as Therapeutic Targets
24^th to 25^th February 2020, Wellcome Genome Campus Conference Centre, Cambridge, UK
The call for poster abstracts will close 15^th November 2019
Website:  http://www.rsc.org/events/detail/36598/6th-ion-channels-as-therapeutic-targets

Synopsis: The symposium will showcase the most recent advances in ion channel science and promote scientific interaction between scientists with a shared interest in the field of ion channel drug discovery. The conference will be organised around series of plenary lectures delivered by international leaders in ion channels science and drug discovery from academia and industry.

1^st RSC BMCS Synthesis in Drug Discovery and Development symposium
27^th March 2020, Eli Lilly, Windlesham, Surrey, UK
The call for poster abstracts will close on 30^th January
Website:  http://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

2^nd Nucleosides and Nucleotides: synthetic and biological chemistry
21^st April 2020, Royal Society of Chemistry at Burlington House, London, UK
Website: https://www.maggichurchouseevents.co.uk/bmcs

Synopsis: Nucleosides are key structures for current drug development and have established roles as antivirals and anticancer agents. Their (poly)phosphorylated nucleotide counterparts are critical tools for chemical biology and sequencing technologies. In recent years, nucleotides have also become fundamental building blocks for the preparation of altered genes and coding systems for synthetic biology. This meeting seeks to explore and celebrate the chemistry that drives the development of modern nucleoside and nucleotide chemistry. It will bring together scientists who work at the interfaces of synthetic and biological chemistry to deliver new tools and insights for biology, and new leads for drug development.