MedChemWatch
Monthly Newsletter January 2022

WELCOME BY EFMC PRESIDENT RUI MOREIRA

Welcome to our first MedChemBioWatch for 2022!

After a challenging but successful 2021, we start this year with enthusiasm and by welcoming the new national adhering organisations that will be instrumental for EFMC to have a wider and global outreach. EFMC activities will continue to expand, with the new computational chemistry initiative, the Certified Schools programme, novel EFMC-YSN MedChemBioOnline webinars, and the XXVII EFMC International Symposium on Medicinal Chemistry and EFMC Young Medicinal Chemists’ Symposium to take place in Nice, France next September.

This is only possible due to the involvement and perseverance of many members and collaborators, including the EFMC Young Scientists Network. I am certain that we are all looking forward to the many opportunities EFMC offers for networking, connecting, and advancing medicinal chemistry and chemical biology...so, make sure you keep tuned!

Finally, on behalf of the EFMC, let me wish you a successful and healthy year.

Rui Moreira
EFMC President

EFMC YEARBOOK 2022 IS AVAILABLE

The official EFMC Yearbook 2022, "Medicinal Chemistry and Chemical Biology in Europe" is a valuable resource for those interested in quickly finding information on all things related to EFMC, such as the activities and composition of Member Societies, Corporate Members and the activities and events of EFMC and its working groups.

In a continuous effort to reduce its ecological footprint, EFMC has decided to produce the Yearbook as an electronic version only. For an optimal reading experience of the Yearbook, we recommend using Chrome, Microsoft Edge or Firefox.

READ THE PDF VERSION

EFMC AWARDS & PRIZES – DEADLINE IS APPROACHING (JANUARY 31, 2022)

The deadline to apply for one of the 2022 EFMC Awards or Prizes is quickly approaching!

The Awards and Prizes will be presented at the XXVII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022) to be held in Nice, France on September 4-8, 2022.

Nomination deadline is January 31, 2022!

Awards

The Award will be given for outstanding achievements in scientific research including contributions to the development of international organisational structures in Medicinal Chemistry and Chemical Biology.

To acknowledge and recognise outstanding research in the field of Medicinal Chemistry in its broadest sense by a young scientist. This Award has been established with the support of UCB Pharma.

To encourage innovation and investigation in technological development related to drug discovery, this Award, established with the support of the Prous Institute, will be given for the discovery, evaluation, or use of new technologies.

Prizes

To acknowledge and recognise outstanding young medicinal chemists and chemical biologists (≤ 12 years after PhD) working in European industry and academia.

To recognise excellence and merits at the early stage.

EFMC HONORARY FELLOWS – DEADLINE IS APPROACHING (JANUARY 31, 2022)

This life-long title and associated medal aim to recognise individuals who have provided outstanding support to the EFMC and contributed to strengthening the position of medicinal chemistry, chemical biology, or related fields in Europe.

Nominations can be submitted until January 31, 2022, and should include:

  • Brief curriculum of the nominee
  • Statement of the documented facts supporting the nomination, summarizing scientific achievements and support of EFMC activities (maximum two pages)
  • Two seconding nomination letters

Self-nominations are not accepted. There are no age restrictions, and nominees may have an academic or industrial background. Nominees should be European residents or have spent a considerable proportion of their career in Europe.

The award ceremony will take place during the opening of the XXVII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022) to be held in Nice, France on September 4-8, 2022. Appointed Honorary Fellows will be invited to attend the meeting and receive their award on stage.

More information and nominations on www.efmc.info/honorary-fellows

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 latest contribution will focus on the recently published article on “An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19” (by Dafydd R. Owen et al. in Science and highlighted as front cover in the same journal).

Here, in this article, Dafydd R. Owen et al. describe the efforts to identify oral SARS-CoV-2 inhibitors capable of targeting the main cysteine protease Mpro — also known as 3CL protease —, which would offer potential selectivity over the human proteome. In-depth structure-based lead optimization culminated in the selection of compound PF-07321332as a clinical candidate.

PF-07321332 is a potent SARS-CoV-2 MPro inhibitor (Ki = 3.11 nM) with excellent Vero E6 antiviral activity (EC50 = 74.5 nM), where the introduction of a nitrile group in the core scaffold plays a crucial role due to its ability to form a reversible covalent thioimidate adduct with the catalytic cysteine of Mpro. In addition, PF-07321332 displayed excellent off-target selectivity and in vivo safety profiles. Besides, PF-07321332 can be easily scaled up, and it has enhanced solubility and reduced epimer formation compared to other candidates.

As shown in recent PF-07321332 clinical assays, this small molecule has the potential to reduce the impact of this potentially fatal illness by diminishing both the severity of COVID-19 infections and the transmission. This discovery brings us optimism: hopefully, 2022 will be the year where the world ends the acute stage of the COVID-19 pandemic. The UK Medicines and Healthcare products Regulatory Agency (MHRA) very recently granted approval to Pfizer’s oral antiviral PAXLOVIDTM, a combination of PF-07321332 (nirmatrelvin) with ritonavir, for the treatment of COVID-19.

Dafydd R. Owen et al. « An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19 », Science, DOI: 10.1126/science.abl4784

Read the article: https://www.science.org/doi/10.1126/science.abl4784

GET TO KNOW ZAID (M. JABER) AL-OBAIDI, ALKAFEEL UNIVERSITY, IRAQ

In this edition, our #Iamamedicinalchemist is Zaid Al-Obaidi from the Alkafeel University, Iraq.

Get to know him better by reading our interview below.


How did you get interested in Medicinal Chemistry?
I got interested in Medicinal Chemistry while studying for my Bachelor in Pharmacy in 2007. This led me to my Master’s degree in Pharmaceutical Analysis with distinction at Sheffield Hallam University in the United Kingdom in 2013. Thereafter, I got my PhD in Iraq with distinction in 2019.

What was the topic of your PhD project?
The topic of my PhD project was entitled “In silico design, synthesis, characterization, and biological evaluation of spebrutinib analogues as antitumor agents against breast and colon cell lines”

Where are you currently working and what is your current position?
Currently, I am working as head of a department at the University of Alkafeel, College of Pharmacy.

What are your current research interests?
My current research interests are: computer-aided drug design, anticancer drugs, synthesis of new small molecules, green chemistry, microwave-assisted synthesis, and others.

How would you explain what your research area is to non-scientists?
My research area can be simply revealed as the design, synthesis, characterization, and biological evaluation of new molecules in an attempt to enhance the properties and overcome obstacles encountered with the existing drug molecules.

What do you like best about your work?
What I like the most about my work is the novelty in the synthesis of new molecules.

What kind of tasks does your work involve?
My work involves many tasks encompassing teaching, researching, and mentoring.

What kind of skills does your work require?
My work requires skills like being precise, creative, and patient.

What do you consider your greatest achievement in your scientific career?
My greatest achievement throughout my scientific career is the application of a WO-PCT patent.

Which of your papers are you most proud of and why?
I am most proud of the paper entitled “Advances in Applying Computer-Aided Drug Design for Neurodegenerative Diseases”. This is because I’ve worked with very talented scientists from Oxford, Cambridge, Aston Universities for almost a year.

What are the features of a successful PhD student or postdoc?
The features of a successful PhD student or postdoc can be illustrated in being undefeatable and never giving up.

How would you describe yourself as a supervisor?
My team would describe me as an excellent motivator who is full of positive energy

What is the most embarrassing thing you have done in the lab while doing experiments, e.g. explosions?
When I was doing a reaction during my PhD, I was evaporating the solvent under vacuum. Then one of the supervisors just entered the lab. Distracted, I just turn off the vacuum pump without closing the valve of the desiccator. This caused the pump oil to return back and spray on the samples worth approximately 1000 USD! It was an unforgettable moment!

What are your recommendations for a book, podcast, website, blog, YouTube channel or film?
As a book : An Introduction to Medicinal Chemistry - Graham Patrick. While the websites I do prefer are those of ACS and EFMC as they are very supportive.

Which scientist do you admire the most and why?
Professor Simona Francese, as she kindly supervised me during my MSc in SHU in the UK and she was a real scientist that taught me a lot of what I am today.

Which field of medicinal chemistry do you consider the most promising for the future?
Computer-aided drug design (CADD)

What advice would you give to someone who wants to know more about your field?
Medicinal Chemistry is a fascinating discipline that deserves every effort you would offer.

What would you like to ask from other medicinal chemists?
Please write down all the reaction conditions so they would be reproducible.

What would you expect to be the next major breakthrough in medicinal chemistry?
It might be the discovery of new druggable targets for neurodegenerative diseases.

MEET FABRIZIO MICHELI, EVOTEC, ITALY

Let us offer you the chance to meet another #Iamamedicinalchemist: Fabrizio Micheli from Evotec, Italy.

 

 

How did you get interested in Medicinal Chemistry?

I still was in high school when a medical doctor, friend of my family, suggested me to learn medicinal chemistry when discussing together of my desire to understand how drugs work in patients. Accordingly, despite choosing synthetic organic chemistry, I made my thesis on the synthesis of a non-natural amino acid and I learned all the associated biology and effects of the statins on the body. That was the reason for which I joined a pharma company as my first job despite having had offers from other branches of chemistry much closer to home.
In such a way I learned biology and pharmacology on the job and, a few years later, I also completed my pathway with a degree in medicinal chemistry.

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

I currently work for Evotec in the Levi-Montalcini campus in Verona. I am VP of the Medicinal Chemistry I department and I manage a group of about 45 people in the larger Evotec chemistry community, whose mission is to discover and develop highly effective therapeutics and make them globally available to the patients who need them. 

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

The discovery of a new drug is a long process, made by many small steps with a lot of potential hurdles and roadblocks to overcome. You may want to see it as cross-country race in a rainy day, but I do prefer to see it like a chess game in which you plan in advance the move to overcome the resistance of your opponent until the final goal is met.

What do you like best about your work?

Challenges and diversity. Every day you discover a novel potential routes to achieve your final target but also new obstacles along the path and you need to fix these potential issues. Every day you have new things to do as the disaster is always behind the corner and only a few molecules can survive the entire path till the end.

What kind of skills does your work require?

Being a drug hunter requires definitely vision, flexibility and resilience.

I remember a dialog in an old movie where the two characters speak about crossing a river “I need a man with very special qualities to lead. He's got to be tough enough to do it and he's got to be experienced enough to do it. Plus, one more thing. He's got to be dumb enough to do it... Start getting ready”.

To achieve a potential drug, you need to plan your strategy and your tactics very well, and you need to be flexible to overcome all the roadblocks that you might find on the road. Plus, you need to be resilient enough as many of your molecules will definitely fail. Only a tiny number will get to the finish line and you know that in advance.

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

Considering the fact that I only worked in the industrial environment, I am really proud of my more than 130 peer-reviewed articles and patents. Among them there is a J. Med. Chem. article that I love the most. It belongs to the discovery of a DA D3 antagonist. That was done in a highly competitive field with a very crowded IP area. It came after a previous closure of the research project and it contains the molecule which reached the proof of concept within humans following PET studies. 

Which scientist do you admire the most and why?

The first name which comes to my mind is the one of Dr. Tadataka "Tachi" Yamada. And this is not only as he recently passed away, but as he was an inspiring figure for me. He was a Japanese-born American physician and gastroenterologist and I met him when he was Chairman of Research and Development at GlaxoSmithKline. Being a scientist, Tachi fully understood the inherent difficulties of the research programmes. He was also an inspiring manager, whose focus was always on the patients pushing to make things with a great sense of urgency. I had the pleasure to meet him multiple times in my role of project leader. Despite his high position within the company, he had always time to look after the research programs, to give great suggestions and to also understand the tiny details of the projects. And one of the things that makes me proud is the co-authorship of a patent with him. 

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

Medicinal chemistry is a continuously evolving science. It is made by great expertise, learnings from the past and always with an eye well aimed at the future. It has the capability to retain all the goods from the different things that have been popping up during these years. In my humble opinion, the most promising and challenging thing that medicinal chemistry is facing is the impact of Artificial Intelligence/Machine Learning. This will surely help the scientists to achieve their targets and objectives with shorter timelines, in a more efficient way and in an always “greener” environment. But this future is not far. This future is now and we are ready for this new adventure.

MEDCHEM 2021 – REPORT OF THE ANNUAL ONE-DAY MEETING ON MEDICINAL CHEMISTRY OF SRC & KVCV

The 2021 edition of the annual One-day Meeting on Medicinal Chemistry of SRC (Société Royale de Chimie) & KVCV (Koninklijke Vlaamse Chemische Vereniging) took place in-person on November 19, 2021 at the impressive academic hall in Liège (Belgium). More than 100 scientists from all over Belgium and Europe gathered themselves under Covid Safe measures to follow and discuss the cutting-edge science presented by 12 invited speakers from Academia and Industry as well as posters presentations and exhibitors during this single day conference.

Because of the 50th birthdays of the medicinal chemistry divisions of SRC and KVCV, the common theme of the symposium was to give an overview of medicinal chemistry in Belgium. Therefore, one speaker of each university was invited together with speakers from Belgian pharma and biotech companies: UCB, Janssen Pharmaceutica, Galapagos and Confo Therapeutics.

 

 

The day started with an opening ceremony by Dr Laurent PROVINS (UCB, Braine-l'Alleud, Belgium) providing key numbers about research in Medicinal Chemistry in Belgium. Then, the first morning session chaired by Prof. Bernard PIROTTE (ULIÈGE, Liège, Belgium) allowed participants to get a first insight on the diversity of medchem activities in Belgium with the talks of Prof. Gilles BERGER (ULB, Brussels), Dr. Fabian HULPIA (JANSSEN, Beerse), Prof. Steven BALLET (VRIJE UNIVERSITEIT BRUSSEL, Brussels), Dr. Hans KELGTERMANS (GALAPAGOS NV, Mechelen), Dr. Dan BROOKINGS (UCB, Slough, United Kingdom) and Dr. Christel MENET (CONFO THERAPEUTICS, Brussels). A wide variety of topics and new technologies were presented.

During the lunch break posters were presented, discussed, and evaluated. The afternoon session was chaired by Prof. Serge VAN CALENBERGH (UGENT, Ghent). The second speaker panel was composed of Prof. Pieter VAN DER VEKEN (UANTWERP, Antwerp), Prof. Eveline LESCRINIER (REGA INSTITUTE - KU LEUVEN, Leuven), Dr. Lionel POCHET (UNAMUR, Namur), Dr. Frederik ROMBOUTS (JANSSEN, Beerse, Belgium), Prof. Raphaël FREDERICK (UCLOUVAIN, Brussels-Woluwe) and Dr. Pierre FRANCOTTE (ULIÈGE, Liège).

After a fruitful day, the closing ceremony was hosted by Prof. Koen AUGUSTYNS (UANTWERP), former EFMC president. Three poster prizes were attributed with the support of ChemMedChem to Siham BENRAMDANE (UANTWERP), Chiara BRUSTENGA (UCLOUVAIN) and Lorenzo CIANNI (UANTWERP).

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

The German Chemical Society (GDCh) and the German Pharmaceutical Society (DPhG) cordially invite you to attend the annual meeting on "Frontiers in Medicinal Chemistry", which will be held online on March 13 -16, 2022.

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: Non-Mainstream Chemotypes, Chemical Epigenetics, First Disclosures & Case Studies, Next Generation Drugs, Macrocycles, AI – Retrosynthesis and Automation, Medicinal Chemistry and Target Highlights, Young Investigators.

The scientific program will include lectures, and poster presentations. It is the goal of the organisers to make this meeting 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 available here.

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

The BMCS is happy to provide a report of its recent 15th BMCS Postgraduate Symposium and announces several upcoming events.

  • 5th RSC/DMDG/DMG New Perspectives in DMPK
  • 8th RSC-BMCS Fragment-Based Drug Discovery Meeting
  • 33rd Medicinal Chemistry in Eastern England (Hatfield Symposium)
  • 8th RSC/SCI symposium on GPCRs in Medicinal Chemistry

The 15th BMCS biological and medicinal chemistry symposium was held virtually on Friday 10th December 2021 and attracted 47 abstracts and 227 registered attendees who heard two plenary lectures and 8 young researcher lectures. There were also 22 poster presentations and the quality of the science presented was yet again extremely high.

I am pleased to announce that the prize awardees are as follows:

Oral presentations

  • Michael Rowlinson from the University of Manchester for his talk on ‘Discovery, Characterisation and Engineering of Ligases for Amide Synthesis’ (Winner)
  • Katherine MacFarlane from the University of Strathclyde for her talk on ‘Discovering Novel Antibody Recruiting Molecules Against LOX-1 Using DNA-Encoded Library Technology’ (Runner-up) 

Poster presentation

  • Karina Chan from the University of Strathclyde for her poster titled ‘PROTAC-kling permeability and cell-selectivity issues with an antibody-mediated approach’ (Winner)
  • Craig Steven from the University of Edinburgh for his poster titled ‘Design, Synthesis and Cellular Imaging of Fsp3-Inspired Bio-orthogonal Probes for Stimulated Raman Spectroscopy’ (Runner-up)

Participant’s prize                                

  • Jessica Graham from the CRUK Drug Discovery Unit at Newcastle University for her poster titled ‘Highly Efficient Buchwald-Hartwig Coupling of Arylamines for DNA- Encoded Library Synthesis’

The organising committee are grateful to all those companies and individuals who provided sponsorship for this meeting, without which it would be difficult to run as a free-of-charge event

5th RSC / DMDG / DMG New Perspectives in DMPK   

22nd and 23rd February 2022, Liverpool, UK

Last chance to register

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

Synopsis:    Members from across the DMPK research community are encouraged to join colleagues from across academic, industrial, and third-sector institutions and contribute to the ongoing discussion, evolution and application of DMPK in various scenarios

Fragments VIII:  8th RSC-BMCS Fragment-based Drug Discovery meeting

27th and 28th March 2022, Churchill College, Cambridge

Delegate Registration and Exhibitor/Sponsor registration is now open

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

Synopsis:  The aim of the meeting is to continue the focus on case studies in Fragment-based Drug Discovery that have delivered compounds to late stage medicinal chemistry, preclinical or clinical programmes. Over three-quarters of the presentations will be focused on case studies.

33rd Medicinal Chemistry in Eastern England (Hatfield symposium)

28th April 2022, The Fielder Centre, Hatfield, UK

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

Synopsis:  Known colloquially as the "Hatfield MedChem" meeting, this a highly successful, long-standing, one-day meeting which runs annually. The scientific program will comprise presentations showcasing medicinal chemistry case studies from tools to candidates, across a range of modalities, therapeutic areas and target classes, as well as covering more general topics from the forefront of drug discovery of relevance to medicinal chemists.

8th RSC/SCI symposium on GPCRs in Medicinal Chemistry

5th-7th October 2022, Verona, Italy

The call for oral abstracts will close on Monday 31st January 2022

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

Synopsis: The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We are pleased to be holding this 8th meeting in the series on GPCR drug discovery, which will combine cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.

THIS NEWSLETTER IS KINDLY SPONSORED BY


 

ISSUE SPONSORED BY

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EFMC ORGANISED EVENTS

May 8-11, 2022
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry New Opportunities in GPCR Drug Discovery

September 4-8, 2022
Nice, France
XXVll EFMC International Symposium on Medicinal Chemistry 

September 8-9, 2022
Nice, France
9th EFMC Young Medicinal Chemists' Symposium 

EFMC SPONSORED EVENTS

January 23-26, 2022
Santiago de Compostela, Spain
XX National Meeting of the Spanish Society of Medicinal Chemistry

January 24-28, 2022
Online
3rd Alpine Winter Conference on Medicinal and Synthetic Chemistry

February 16-18, 2022
Rome, Italy
3rd Molecules Medicinal Chemistry Symposium (MMCS): Shaping Medicinal Chemistry for the New Decade

May 16-19, 2022
Volgograd, Russia
5th Russian Conference on Medicinal Chemistry

JOB PORTAL

Junior Research professor in chemical biology – medicinal chemistry, University of Antwerp, medicinal chemistry – pharmaceutical sciences, Antwerp, BELGIUM
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PhD position for an organic chemist with an interest for drug discovery and proteomics, Technical University of Munich, TUM School of Life Sciences, Freising, GERMANY
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Medicinal Chemist, SpiroChem AG, Chemistry, Basel, SWITZERLAND
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