MedChemWatch
Monthly Newsletter February 2020

BEST PRACTICES IN MEDICINAL CHEMISTRY – NEW SERIES OF VIDEOS LAUNCHED

It’s with great pleasure that we release the first of our series of videos and presentations Best Practices in Medicinal Chemistry. We hope these will be a valuable resource for the Medicinal Chemistry and Chemical Biology communities, providing useful reference material and stirring debate.

This one is dedicated to Validating Chemical Probes. High quality chemical probes are essential to explore human biology and diseases and as chemists, we have a big role to play to ensure high quality of the published probes.

The video is on our YouTube channel and the files can be found here.

GET TO KNOW HENK TIMMERMAN (VU UNIVERSITY AMSTERDAM, THE NETHERLANDS)

As EFMC is celebrating its 50th anniversary - we had the chance to interview Prof. Henk Timmerman, one of the founding father of the European Federation for Medicinal Chemistry, who was recently awarded the title of EFMC Honorary Fellow.

How did you get interested in Medicinal Chemistry?

Long story...I started my “chemistry” study in 1956. The first 4 years, the programme was very broad, but at the end of what we would call the bachelor level now, I bought a book with the title “Chemistry at the Service of Mankind” and was impressed by the stories on penicillin, DDT, crop protection, herbicides; and by the perspectives of compounds with a biological activity in general.

For what is now called master’s degree, I studied under the supervision of Prof. Wijbe Nauta, who was not only a professor at the Vrije University Amsterdam but also research director of the local pharma company Brocades. My future in science was defined!

(I would like to add that the term Medicinal Chemistry was at that time hardly introduced in Europe, and the field was certainly not accepted as an independent discipline yet)

What was the topic of your PhD project?

The title of my PhD thesis was Synthesis 2-Alkyl-1-[ortho-alkyl phenyl]cyclohexanols (Synthesis, conformation and some pharmacological investigations).

It was interesting that I could make use of NMR with one of the first instruments in the country (60 megacycles at that time) and in vitro pharmacology techniques, both not very common at that time.

Can you tell us more about your Career?

In the sixties it was, in The Netherlands at least, not common to start your career with a postdoc position. One went after obtaining the degree straight to a position in research, teaching or similare. I joined the team of Prof. Nauta at Brocades, in the pharmacology department.

Later on, I became the scientific director of the Pharma division of the company Gist Brocades, which was a world leader in antibiotics research.

In 1979 I returned to academia to become the successor of Prof. Nauta. 

As a special effort, I initiated a programme to stimulate the development of pharmaceutical research in Indonesia. This programme became very rewarding when we were able to introduce modern research in the « Fakultas Farmasi in Yogyakarta ». About ten local PhD programmes were completed and by far the most of the PhD's became full professor in Indonesia.

Currently I still serve science (EFMC, Dutch med. chem  section. I am also editor of a scientific journal: DDT-T), serve society (active in the « Dutch Society Against Quackery ») and involve myself in some social aspects.

What were your research interests?

My research has been concentrated on the relationships between structure and activity of biologically active compounds, with the objective to obtain new substances with an attractive profile for using them as active ingredients in medicines, or to become tools in solving existing questions in pharmacological issues (mechanisms of actions, receptor identification, receptor structures, etc.)

As a field I had selected histaminergic ligands, both agonists and antagonists. We were able to contribute to the the knowledge about all four types of histamine receptors; in 1979 only the H1 and the H2 receptor had been identified.

What kind of skills are needed to be a good researcher?

For teaching, it is clear you should be able to transfer knowledge, but moreover - and maybe more importantly - to educate people in a broader sense,  to  stimulate  scientific  curiosity,  to make  sure the  become  'independently' thinking  scientists. For research, a med. chemist needs knowledge in a very broad field and be able to communicate with colleagues in other scientific fields.

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

When I was a PhD student, I carried out a hydrogenation experiment. At a given moment the autoclave I used started to leak hydrogen! It made a terrible noise but was also extremely dangerous. The stupid thing was that I did the experiment during evening hours, being the sole person in the lab, inacceptable.

Did you experience any unfair situations during your scientific career?

It was during my years in industry. It happened twice that there was a vacancy for which I was told by management that I was the right person for but went to somebody which was senior. Do you understand? A clear case of mismanagement.

Another one: We had found a series of new ligands, with a very high activity at a given receptor. A co-worker of me told during an unofficial meeting at a department abroad about the finding. To our big surprise, one person attending the meeting filed a patent application on "our" series of compounds, with the activity we had found earlier. My co- worker had been imprudent, the other person involved showed an uncollegial, and even an inacceptable behaviour.

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

Without any doubt the further increase of interdisciplinary - I even prefer the term « transdisciplinary ». Those approaches will determine the coming successes of med. chem. research

What would you like to ask from other medicinal chemists?

Please, accept that organic synthetic chemistry, having been for many years the driving force of med. Chem, plays no dominating role in med. Chem anymore. New perspectives come from biology.

And also, please, read the position paper on our discipline!

If you would like to know more about Prof. Timmerman, stay tuned to the YouTube Channel were we will publish the full interview!

LAUNCH OF THE ESMEC ALUMNI AWARD

In 2020, the European School of Medicinal Chemistry (ESMEC) celebrates its 40th anniversary. To mark the occasion ESMEC is launching the first ESMEC Alumni Award.

The ESMEC Alumni Award will be given to an outstanding European researcher in the field of Medicinal Chemistry who has participated in the school either as an oral or poster presenter.

The prize consists of a diploma, a medal and an invitation to give a presentation at ESMEC 2020.

Deadline for nomination submissions: March 31st, 2020

Applicants are invited to fill in the enclosed form and to send the CV and a Proof of Participation with an oral or poster communication (Esmec Certificate of Participation and/or Abstract presented) by e-mail, stating in the subject box “ESMEC Alumni Award”, to both:

Prof. Marco Macchia
e-mail: marco.macchia@unipi.it                                     

Lucia Bedini

PETITION FOR A MORE AMBITIOUS BUDGET ALLOCATION TO THE NEXT RESEARCH FRAMEWORK PROGRAMME, HORIZON EUROPE

The EFMC strongly supports the Initiative for Science in Europe (ISE) and invites all its readers to sign the petition to their representatives in local governments and to the European Council, asking for a more ambitious budget allocation to the next Research Framework Programme, Horizon Europe.

The next meeting of the EU Council is on February 20, so please sign the petition rapidly!

Help us also promote it on social media using the hashtag #HEBudget, and tag @ISE_news!

THE YSN WAS PRESENT AT THE 13TH NATIONAL ORGANIC CHEMISTRY MEETING (13ENQO) IN AVEIRO, PORTUGAL

A team from our Young Scientists Network had a poster and flyers in Aveiro, and met many of the young participants.

It was an excellent opportunity to introduce the network and to start collecting volunteers to participate in the creation of a Portuguese MedChem Network. 

Filipa Ramilo-Gomes
University of Lisbon

If you’re not already a YSN member you can sign up here

THE PROGRAMME OF THE SHORT COURSE ON “NEW OPPORTUNITIES IN GPCR DRUG DISCOVERY” IS AVAILABLE

The new year brings the latest installment of in our ever-popular Short Course Series. This year, the course will provide an introduction for medicinal chemists and chemical biologists to New Opportunities in GPCR Drug Discovery, including concepts and methods applied in the structural biology, modelling, systems biology, pharmacology and medicinal chemistry of GPCRs. 

In addition, there will be a series of case studies, including the discovery of molecular probes, tool compounds, clinical candidates and marketed drugs.

Have a look at the programme & register today – Seats are limited to 35.

JOHN MACOR AWARDEE OF THE 2020 IUPAC - RICHTER PRIZE

John Macor has been selected as awardee of the 2020 IUPAC-Richter Prize in recognition of his research work on new drugs for the treatment of migraine. The acceptance lecture will be held in Basel, Switzerland in September 2020 at the XXVI European Federation of Medicinal Chemistry International Symposium on Medicinal Chemistry (EFMC-ISMC) and a second lecture at the 37th ACS National Medicinal Chemistry Symposium to be held in New York (June 28-July 1, 2020).

This year marks the eighth occasion of the IUPAC-Richter Prize, which was established in 2005 by IUPAC (International Union of Pure and Applied Chemistry) and Richter PLC. Awarded biannually, the awardee is announced by IUPAC following nominations and the decision of an independent international Selection Committee. According to the rules of the prize the awardee is expected to give two lectures, one in Europe and one in the United States, at international symposiums on medicinal chemistry. The lecture in which the prize is awarded occurs alternatively in Europe and in the United States. The awardee receives $ 10 000, which is sponsored by Richter PLC, and a plaque, which is presented by IUPAC.

The previous awardees were: 2006 Malcolm FG Stevens (UK), 2008 Jan Heeres (Belgium), 2010 Arun Ghosh (USA), 2012 Stephen Hanessian (Canada), 2014 Helmut Buschmann (Germany), 2016 Michael Sofia (USA), and 2018 Peter Grootenhuis (USA).

‘FRONTIERS IN MEDICINAL CHEMISTRY’ WITH CHEMICAL EPIGENETICS SESSION ORGANISED BY THE GERMAN MEDICINAL CHEMISTRY DIVISIONS OF GDCh AND DPhG

The German Chemical Society (GDCh) and the German Pharmaceutical Society (DPhG) cordially invite you to participate in the annual meeting on ´Frontiers in Medicinal Chemistry´ March 22-25, 2020, Freiburg, followed by the 3rd Chemical Epigenetics Meeting, March 25-27, 2020.

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 Chemical Proteomics – Activity based Protein Profiling, Macrocyclic and Covalent Inhibitors, Young Investigators, Novel Computational Methods, Epigenetics, and Highlights in Medicinal Chemistry and Case Studies. The scientific program will include lectures and poster presentations. It is the goal of the organizers 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. The Frontiers of Medicinal Chemistry Conference is followed by the
3rd Chemical Epigenetics Meeting, March 25 – 27, 2020

More information :

https://veranstaltungen.gdch.de/tms/frontend/index.cfm?l=9286&sp_id="2"
www.chemepi.org

NEWS FROM THE FRENCH SOCIETY OF MEDICINAL CHEMISTRY (SCT): “DRUG DISCOVERY IN THE RNA WORLD”

The French Medicinal Chemistry Society (Société de Chimie Thérapeutique – SCT) is pleased to invite you to Paris, on March 10th, 2020 for its 4th one-day thematic symposium focusing on the contribution of Chemical Biology to Molecular Therapeutic Innovations. 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”
  • Helene TRAN (Servier Research Institute, France): “Antisense Oligonucleotides Therapeutics for CNS Disorders”

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

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

A call for new inductees to the BMCS “Hall of Fame” and news of upcoming events.

HALL OF FAME AND MEDAL
The BMCS is pleased to announce a new call for nominations for The Hall of Fame and associated medal, to recognise prominent chemists for outstanding, sustained, significant contributions to any area of interest to the BMCS, e.g. medicinal chemistry, agriscience, bioorganic chemistry, chemical biology. Independent nominations may be submitted from March to September each year.

2nd RSC/SCI APPLIED LATE STAGE FUNCTIONALISATION SYMPOSIUM
18th to 19th February 2020, University of Manchester, Manchester, UK
Website: http://www.rsc.org/events/detail/41281/applied-late-stage-functionalisation-where-chemistry-meets-biology

Synopsis: The meeting will highlight some of the hot and emerging developments in the inorganic catalysis and biocatalysis arenas and both the academic and application of late-stage functionalisation methodologies

6th RSC/SCI SYMPOSIUM ON ION CHANNELS AS THERAPEUTIC TARGETS
24th to 25th February 2020, Wellcome Genome Campus Conference Centre, Cambridge, UK
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

1st RSC BMCS SYNTHESIS IN DRUG DISCOVERY AND DEVELOPMENT SYMPOSIUM
27th March 2020, Eli Lilly, Windlesham, Surrey, UK
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

NEWS FROM EUCHEMS: RELEASE OF THE QUARTERLY “CHEMISTRY IN EUROPE” NEWSLETTER

The quarterly Chemistry in Europe newsletter is available online here

In this issue, the editorial has been written by EuChemS President-Elect Floris Rutjes and some of the topics addressed include our investment during the IYPT19, the new European Commission, and inputs from our Members, Professional Networks and the EYCN.

THIS NEWSLETTER IS KINDLY SPONSORED BY OXELTIS

 

ISSUE SPONSORED BY

Oxeltis seasoned medicinal chemist team provides hit and lead optimization services, and expertise in particular areas of multi-step organic synthesis: heterocycles, macrocycles, nucleosides/nucleotides, modified sugars and oligo/polysaccharides. The team focuses on speed, quality and confidentiality in the services and collaborative ventures that it develops.

More info...

EFMC SPONSORED EVENTS

February 18-19, 2020
Manchester, United Kingdom
Applied Late Stage Functionalisation: Where Chemistry Meets Biology

February 24-25, 2020
Cambridge, United Kingdom
6th RSC / SCI Ion Channels as Therapeutic Targets Symposium

March 23-24, 2020
Eindhoven, The Netherlands
A Joint Future for Medicinal Chemistry and Chemical Biology in the Netherlands

March 27, 2020
Surrey, United Kingdom
Synthesis in Drug Discovery and Development

April 14-15, 2020
San Francisco, United States
Medicinal Chemistry Strategies to Mitigate Preclinical Safety Risks in Drug Discovery

April 21, 2020
London, United Kingdom
2nd Nucleosides and Nucleotides: Synthetic and Biological Chemistry

April 21-22, 2020
London, United Kingdom
The 3rd SCI-RSC Symposium on Transporters in Drug Discovery and Development

April 30, 2020
Hatfield, United Kingdom
31st Medicinal Chemistry in Eastern England

EFMC ORGANISED EVENTS

May 17-20, 2020
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry: New Opportunities in GPCR Drug Discovery

September 6-10, 2020
Basel, Switzerland
EFMC-ISMC 2020: XXVI EFMC International Symposium on Medicinal Chemistry

September 10-11, 2020
Basel, Switzerland
EFMC-YMCS 2020: 7th EFMC Young Medicinal Chemist Symposium

JOB PORTAL

Full Professor in Medicinal Chemistry, University of Gothenburg, Derpartment of Chemistry and Molecular Biology, Gothenburg, Sweden

Read more

EFMC ACCREDITED SCHOOL

June 28 - July 2, 2020
Urbino, Italy
European School of Medicinal Chemistry ESMECDiscovery

EFMC SPONSORED SCHOOL

October 4-9, 2020
Leysin, Switzerland
14th Swiss Course on Medicinal Chemistry

Find us on social media

EFMC Facebook EFMC Twitter EFMC LinkedIn EFMC Instagram

EFMC