• Eka Putra Gusti Ngurah Putu (Institut Curie, France)
• Irene Herrera González (Universidad de Salamanca, Spain)
• Jennifer Müller (ETH Zürich, Switzerland)
• Hermann Neitz (Universität Würzburg, Germany)
• Jana Volaric (Imperial College London, United Kingdom)
• Martin Wilkovitsch (TU Wien, Austria)

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 2024 winner will also receive a free registration and a 500€ travel grant to attend both the XXVIII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2024) and the 11th EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS 2024) which will take place in Rome, Italy on September 1-5 & September 5-6, 2024.

How did you get interested in Medicinal Chemistry?

I started my career with an apprenticeship as a chemical lab technician at Ciba Specialty Chemicals. After a few years working in industry, I then obtained a Bachelors and Masters in Chemistry from the University of Applied Sciences Northwestern Switzerland and the University of Basel, respectively. While being interested and trained as an organic chemist, I have always been extremely passionate about the application of chemistry within the health sciences. Therefore, for my PhD I have specialised in Medicinal Chemistry as I want my research to contribute to improving health within our society.

Where and when did you obtain your PhD diploma?

I have obtained my PhD in Medicinal Chemistry from Monash University in 2014. My PhD focused on the development adenosine A_2A receptor antagonists, dopamine D₂ receptor agonists and dual acting ligands for the treatment of Parkinson’s disease.

Where did you have your postdoc position?

I stayed at Monash University for my postdoc and worked in the group of Professor Peter Scammells, where I worked on the development of allosteric and bitopic ligands targeting muscarinic and adenosine receptors.

What are your current research interests?

My research interests are in the development of novel chemical probes to improve our understanding of proteins on a molecular level, and to address important questions in molecular biology related to the structure, activation, degradation, oligomerisation, allostery and selectivity of selected drug targets. 

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

We currently lack crucial insights into the function of cells and how they perform the billions of chemical reactions that keep us functioning each day, allowing us to sleep, breathe, move about, and stay healthy. While atoms and molecules are known to play a central role in this functioning, further chemical biology studies are needed to improve our understanding of vital processes within cells. My work is aimed to provide a better understanding of these chemical reactions within the body and use this information to develop better drugs.

What kind of tasks does your work involve?

My duties include running a medicinal chemistry lab, overseeing research projects, supervising students, preparing lectures, teaching, attending meetings as well as writing papers and applying for grants.

What do you like best about your work?

The biggest privilege is working with students on research projects. It combines two aspects that I am most excited about in my job 1) realising research ideas, and 2) teaching, working with and learning from the next generation of great minds. 

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

My group currently consist of 5 PhD, 2 master’s and 1 Honours students. I am always interested in expanding my group with talented and motivated PhD students that are interested in Medicinal Chemistry and/or Chemical Biology.

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

I don’t think that there is one particular achievement I am most proud of, but more the combination of a series of achievements. Growing up I wasn’t a very good student and an academic career seemed out of reach. The completion of a Bachelor’s Degree, Master’s Degree and PhD after several years of work experience in industry was only possible due to a lot of hard work and dedication. Therefore, running my own research group, teaching and supervising postgraduate students is something I not only enjoy, but I am proud of. 

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

This is a difficult question as behind every paper there is a lot of work and unique experiences. However, my first publication in the Journal of Medicinal Chemistry (M. Jörg et al. J. Med. Chem. 2015, 58, 718-738.) is very special to me as it sums up three years of work during my PhD. The majority of the work was performed by myself and this publication one of the highlights of my PhD.

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

Passion for their field of study, good work ethic, ability to work individually and also be a team player, attention to detail, drive to excel, high motivation, resilience, good communication and interpersonal skills.

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

Unfortunately, unfair situations are not uncommon in scientific careers (and probably most careers). For example, my non-traditional academic career path has prohibited me from applying to several early- and mid-career grants and fellowships due to age limitations. Thankfully, this has become less common over the last few years. I recommend connecting with people that actively support your career. Be resilient. Stay true to your values. Try to make the change that is needed to make it better for future generations.

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

In my second week of a 1-year internship, I forgot to turn on the water flow to one of the rotavaps. While this doesn’t sound too bad, it resulted in breaking the condenser of the rotavap, which is not easy or cheap to repair. It was a very embarrassing mistake and not a good way to join a new lab.

Which scientist do you admire the most and why?

There isn’t just one scientist that I admire the most. Generally, I am most inspired by genuine people that have faced and overcome some major obstacles in their career and/or life.

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

Some of the areas that have huge potential are protein degradation, DNA-encoded libraries, biomarkers, and personalised medicine. Additionally, machine learning will transform the way we work in drug discovery and beyond.

The human microbiome, especially in the gut, significantly influences drug efficacy and toxicity. Despite this, gut microbial metabolism is frequently overlooked in drug development. Medicen, a Paris-based health innovation cluster, has convened over 30 global academic and industrial experts to propose integrating microbiome science into drug discovery and development. Seven expert teams address diverse areas, producing state-of-the-art reports highlighting microbiome-related tools at each stage. Critical limitations include limited data on drug-microbiome interactions and lack of agreed standards. This paper presents proposals for utilizing microbiome tools to support drug development, alerting to potential microbiome-induced drug properties, and integrating microbiome data into predictive pharmacokinetic models. Detailed discussions on drugs metabolized by the microbiome support the working group's recommendations.

https://dmd.aspetjournals.org/content/early/2024/02/02/dmd.123.001605

Chlorine is one of the most common atoms present in small-molecule drugs beyond carbon, hydrogen, nitrogen, and oxygen. There are currently more than 250 FDA-approved chlorine-containing drugs, and their structures and syntheses have been tabulated in a review by Fang et al. in 2019 [1]. However, the beneficial effects of the chlorine substituent have not yet been discussed to the same extent as other small groups like methyl [2] or fluorine [3]. The seemingly simple substitution of a hydrogen atom (R = H) with a chlorine atom (R = Cl) can result in remarkable improvements in potency of up to 100,000-fold. Following the literature terminology of the “magic methyl effect” in drugs, the term “magic chloro effect” has been coined [4]. Although reports of 500-fold or 1000-fold potency improvements are often serendipitous discoveries that can be considered “magical” rather than planned, attempts to explain an unexpectedly significant chloro effect can be an important exercise. In this presentation, the effect of chlorine substitution on dipole moments, acidity, and lipophilicity, as well as hydrogen and halogen bonding, will be discussed in the context of ligand–protein binding and potency improvements. Furthermore, chlorine substituents can lead to profound effects on pharmacokinetic parameters including clearance, half-life, and drug exposure in vivo. Although there are case-by-case variations, a chlorine atom is able to combine the beneficial effects of a methyl group (e.g., lipophilicity, van der Waals interactions, steric effect) and a fluorine atom (e.g., electronegativity / electron-withdrawing ability, metabolic stability, increased acidity). Suggestions will be made regarding when (and when not to) include chlorine substituents in a preclinical molecule. Although the chlorine effect might be more beneficial for early preclinical studies, it can be argued that the chlorine effect can be useful at all stages of preclinical work, and understanding this effect better could lead to lessons that accelerate the cycle of drug discovery.

[1] Smith, B. R.; Eastman, C. M.; Njardarson, J. T. Beyond C, H, O, and N! Analysis of the Elemental Composition of U.S. FDA Approved Drug Architectures. J. Med. Chem. 2014, 57, 9764–9773.

[2] Fang, W.-Y.; Ravindar, L.; Rakesh, K. P.; Manukumar, H. M.; Shantharam, C. S.; Alharbi, N. S.; Qin, H.-L. Synthetic Approaches and Pharmaceutical Applications of Chloro-containing Molecules for Drug Discovery: A Critical Review. Eur. J. Med. Chem. 2019, 173, 117–153.

[3] Schönherr, H.; Cernak, T. Profound Methyl Effects in Drug Discovery and a Call for New C–H Methylation Reactions. Angew. Chem. Int. Ed. 2013, 52, 12256–12267.

[4] Gillis, E. P.; Eastman, K. J.; Hill, M. D.; Donnelly, D. J.; Meanwell, N. A. Applications of Fluorine in Medicinal Chemistry. J. Med. Chem. 2015, 58, 8315–8359.

[5] Chiodi, D.; Ishihara, Y. “Magic Chloro”: Profound Effects of the Chlorine Atom in Drug Discovery. J. Med. Chem. 2023, 66, 5305–5331.

Register for free here.

#GDCh (MedChem Division), #NextGenMedChem.

With the increasing approval of RNA modulating therapies, the speakers will give anyone interested in this topic an excellent opportunity to learn more about this theme. Speakers will cover successful approaches, future opportunities, and novel approaches being explored in industry and academia to exploit ways to downregulate, upregulate or change splicing in protein synthesis for therapeutic purposes. Speakers will also discuss safety and pharmacokinetic aspects of the modalities being explored. The morning session will focus on the use of oligonucleotide approaches to modulating RNA transcription, while the afternoon session will focus on small molecule approaches.

More information and registration on SMR.

RSC-BMCS Hot Topics: Covalent Drug Discovery 2024
16^th May 2024, Virtual
Registration will close on 15^th May
Website: https://www.rscbmcs.org/events/hottopicscdd24/

Synopsis: Covalent binding has emerged as a key strategy in contemporary drug discovery. This online, half-day meeting will bring together experts from both academia and industry to discuss recent advances in using covalent small molecules to target challenging protein targets. The BMCS Hot Topics online meetings are intended to highlight breaking areas of research in fields of science relevant to drug discovery. They will run as stand-alone half-day virtual events, 2-3 times per year. The programme will be targeted towards researchers working who would like to enhance their understanding of these nascent or developing fields.

BMCS 4^th Synthesis in Drug Discovery and Development
4^th – 5^th June, Virtual
Website: https://www.rscbmcs.org/events/sddd24/ 

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 aims to celebrate the crucial role of synthesis in the success of drug discovery and development.

6^th RSC-BMCS/DMDG New Perspectives in DMPK
Monday 17^th June, 2024 Liverpool Medical Institute,
Registration closes on 7^th June!
Website: https://www.rscbmcs.org/events/dmpk24/

Synopsis: Novel small-molecule-based therapeutic approaches represent a key component of the discovery landscape. The emergence of molecular glues, PROTACs, bicyclic peptides, and other novel chemistries often bring with them new challenges for drug discovery scientists; synthetic difficulty, beyond rule-of-five physicochemical properties, and complexity in the link between exposure and response, may complicate ADME characterisation and accurate human dose prediction, particularly for drugs aimed at oral administration. This meeting will provide a forum for the exchange of ideas between principal members of the DMPK research community on how we can rise to these challenges. Keynote talks from thought leaders will provide wider perspectives on how DMPK can contribute to the delivery of medicines to patients more quickly and efficiently.  There will be a balanced mix of oral and poster presentations, and networking opportunities throughout.

3rd RSC / SCI New Therapeutics for Global Health

9^th – 11^th September 2024, Cranfield Management Development Centre, Cranfield University, Milton Keynes

Abstract submissions are now open! Registration is now open!

Website: https://www.rscbmcs.org/events/ntgh24/

Synopsis: Tuberculosis, malaria and diseases caused by a diverse range of pathogens, including flaviviruses (eg dengue, West Nile), kinetoplastids (causative agents of Chagas disease, leishmaniasis, etc) and gut pathogens (worms, bacteria, parasites),remain a cause of high mortality across the globe. Fortunately, an ever-improving understanding of the complex life-cycles of these disease-causing pathogens is presenting increasing opportunities for those seeking to tackle these global health problems. This meeting will focus on medicinal chemistry approaches to developing new medicines for diseases affecting global health. Keynote talks from international experts from industry and academia, alongside perspectives detailing case histories in drug discovery, will highlight the latest developments in the field whilst also showcasing the opportunity for creativity and innovation.

7^th RSC-CICAG/RSC-BMCS Artificial intelligence in Chemistry

16^th – 18^th September, Churchill College, Cambridge

Registration is now open!

Website: https://www.rscbmcs.org/events/aichem7/

Synopsis: Artificial Intelligence is experiencing a renaissance in the development of new methods and practical applications to ongoing challenges in Chemistry. Following the successes of five annual “Artificial Intelligence in Chemistry” meetings starting in 2018, we are pleased to announce that the Biological & Medicinal Chemistry Sector (BMCS) and Chemical Information & Computer Applications Group (CICAG) of the Royal Society of Chemistry are once again organising a conference to present the current advances in AI and machine learning in Chemistry. The meeting will be held over two days and combine aspects of artificial intelligence and deep machine learning methods to applications in chemistry.  The programme will include a mixture of keynote talks, panel discussion, oral presentations, flash presentations, posters and opportunities for open debate, networking and discussion.

This year meeting has changed format to two and half days and will include workshop on first day, please keep checking website for updates.

9^th RSC/SCI Symposium on GPCR’s in Medicinal Chemistry
2^nd – 4^th October 2024, Evotec Campus Levi-Montalchini, Verona, Italy

Registration and Abstract submissions are now open!
Website: https://www.rscbmcs.org/events/gpcrs24/  

Synopsis: The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We were pleased to hold this 9th meeting in the series on GPCR drug discovery, which combined cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.

RSC-BMCS/SCI Targeting Protein Degradation 4
15^th 16^th October, Cranfield Management Development Centre, Cranfield University, Milton Keynes
Registration and Abstracts submissions are now open!

Website: https://www.rscbmcs.org/events/protdeg24/

Synopsis: One of the most exciting new therapeutic modalities to emerge in the 21st century has been Targeted Protein Degradation (TPD). In 2021, the Targeted Protein Degradation Market size was valued at USD 400.5 million and is poised to grow from USD 507.0 million in 2022 to USD 3,300.0 million by 2030 and so has attracted interest from academia, non-profit organisations through to CROs and small and large pharma.This multidisciplinary meeting aims to present the latest developments in the design, biology, chemistry and ADME in TPD within the general themes of PROTACS (including non-oncology targets), Molecular Glues and non-PROTAC degraders. We aim to highlight the newest in enabling technologies such as computational techniques, Direct to Biology, HT synthesis (click, photochemistry etc) and structural biology methods.

BMCS Postgraduate Symposium XVIII
12^th December 2024, University of Oxford, Oxford, UK

Registration and abstract submissions are now open!

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

Synopsis: This face-to-face meeting will comprise an oral and poster presentations from PhD students and post-doctoral workers researching in biological or medicinal chemistry. In addition, the agenda will feature invited keynote speakers from industry and academia.

Meetings in 2025

8^th RSC-BMCS / SCI Symposium on Ion Channels as Therapeutic Targets
31^st March – 1^st April, 2025, Hinxton Hall Conference Centre, Cambridge

11th RSC/SCI Symposium on Kinase Inhibitor Design
Monday 12 – Tuesday 13 May, 2025, Royal College of Physicians of Edinburgh, Edinburgh

RSC-BMCS / SCI 23rd Medicinal Chemistry Symposium
Sunday – Wednesday, 14th-17th September, 2025, Churchill College, Cambridge