PRIZE WINNERS ANNOUNCED FOR THE 2019 EFMC PRIZES FOR A YOUNG MEDICINAL CHEMIST IN INDUSTRY & ACADEMIA
EFMC Prize for a Young Medicinal Chemist in Industry 2019
Congratulations to the winner and two runners-up:
- Winner: Dr Radka Snajdrova (Novartis Pharma, Switzerland)
- Runners-up: Dr Jo Alen (Grünenthal, Germany) & Dr Jacob Bush (GSK, United Kingdom), the runners-up.
EFMC Prize for a Young Medicinal Chemist in Academia 2019
Congratulations to the winner and two runners-up::
- Winner: Prof. Andreas Koeberle (Friedrich-Schiller-University Jena, Germany)
- Runners-up: Prof. Anna Katharina Hirsch (HIPS, Germany) & Prof. Kamil Musilek (University of Hradec Kralove, Czech Republic)
The 2019 Prizes will be awarded at the VIII EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC’19)in Athens, Greece – September 1-5, 2019.
I AM A MEDICINAL CHEMIST/CHEMICAL BIOLOGIST: MEET GIANNAMARIA ANNUNZIATO, (UNIVERSITÀ DEGLI STUDI DI PARMA, ITALY)
In this edition, we present Dr Giannamaria Annunziato from the Università degli Studi di Parma, Italy. She is also the representative of the young scientists of the Italian Chemical Society.
Where and when did you obtain your PhD diploma?
I obtained the Ph.D. diploma in March 2017 at the University of Parma, spending four months at ETH of Zurich as visiting Ph.D. student.
What was the topic of your PhD project?
“New strategies to eradicate Microbial Resistance”, I’ve been involved into a very challenging and exciting project, from the synthesis of small molecules as inhibitors of pathogens’ “non-essential” pathways to the total synthesis of natural products derivatives endowed with antimicrobial activity.
Where did you have your postdoc position?
I had a postdoc position as a Medicinal Chemist at the University of Parma.
Where do you work at the moment and what is your current position?
At the moment I am Assistant Professor of Medicinal Chemistry at the Department of Food and Drug of the University of Parma and also, I am the representative of Medicinal Chemistry under-35 years old scientists at the Italian Chemical Society (Società di Chimica Italiana, SCI Giovani).
What are your current research interests?
Now I have the opportunity to work on different topics; I am still working on my former PhD project, trying to find small molecules as adjuvants of already existing antibiotics for which pathogens have developed resistance. From my point of view this is a very promising approach in this field because these targets that are “non-essential” are less prone to mutate and their inhibition make bacteria more susceptible to the attack of the host immune system and antibiotics. Another project in which I am involved is focused on the development of pharmacological chaperones able to restore the physiological activities of a mutated proteins underlying human diseases and, finally, I am also working on natural extracts in order to identify natural compounds endowed with interesting nutraceutical activities.
How would you describe yourself as a supervisor?
I always try to make my students curious about their work, pushing them to be patient, motivated, hard-working and creative which I think are the most important skills in this work.
Which scientist do you admire the most and why?
Rita Levi Montalcini, the first and only (up to now) Italian woman which won the Nobel prize in Medicine and Physiology. In my opinion she has been one of the most important Italian scientists, and I appreciate her commitment in science but also in social problems at a time when women hardly have chances.
Did you experience any unfair situations during your scientific career?
Which paper of yours you are the proudest of and why?
I am proud of every single paper I have contributed to publish in a scientific journal; there are a lot of studies and work behind all of them. Anyway, up to now, the paper of which I am proudest is my first as corresponding author, on the discovery of a new class of antifungal agents that selectively inhibits microbial carbonic anhydrase. Journal of Enzyme Inhibition and Medicinal Chemistry; 2018, 1, 1537-1544.
Which field of medicinal chemistry do you consider the most promising in the future?
The concept of pharmacological chaperone therapy has been emerging in the last years and is very intriguing and interesting. Pharmacological chaperones are small molecules that bind into a target protein and stabilize its native structure helping mutated proteins to restore their biological function. The ability to restore the native physiological function of a protein trough a small molecule or bio-macromolecule is something really exciting and challenging to obtain. Such modulators can find large applications in misfolding human diseases, such as neurodegenerative diseases, so I think that they will play an increasingly important role in medicinal chemistry in the next decades.
EFMC PHOTO COMPETITION 2019: ELEMENTS OF LIFE, DEADLINE EXTENDED TO JUNE 25!
We received many submissions but we would like to get even more, so get your camera and and send in your entry. The winner will receive a prize of €200!
There will also be prizes of €100 for two runners-up.
In addition, the best pictures will appear in cover of several issues of the EFMC Newsletter “MedChemWatch” and will be showcased in the annual Yearbook.
We want scientists from any level (eg. students to expert professionals) and affiliation (eg. academia and industry) to take the best shot possible and enter the competition!
The pictures will be judged by a two-round public vote. First online and afterwards during the “EFMC-ASMC'19”, where the best shots will be printed out and displayed at the conference for participants to vote live!
Submit your picture!
REPORT OF THE EFMC SHORT COURSE 2019: SMALL BECOMES BIG IN MEDICINAL CHEMISTRY: FRAGMENT-BASED DRUG DISCOVERY
The 15th EFMC short Course “Small Becomes Big in Medicinal Chemistry: Fragment-Based Drug Discovery (April 28- May 1, 2019) was followed by 22 participants. The participants came from European countries mainly, but from some faraway places too: Japan, Korea, USA. One of the aims of the EFMC short courses, a very intensive with ample discussions between participants and teachers was reached again. The course leader, Prof. Iwan de Esch (VU University, Amsterdam), had composed an attractive programme with lecturers from the FRAGNET European training network that is focused on Fragment-Based Drug Discovery. The speakers, Rod Hubbard, Gyorgy Keseru, Paul England, Ben Davis, Mike Hann, Xavier Barril and Gregg Siegal are world-renowned experts and together they very thoroughly covered all aspects of FBDD.
Over 85 percent of the participants rated the course as very good; the remaining participants scored the course as good.
The participants also scored the different teachers, for the content of their presentation and the way of presentation of it both. Using a score from 0 to 5, five being the highest, the lowest figure was 4.6, many scores of 5 were reached however.
Part of the success of the course is due to the pleasant venue in the midst of a beautiful park in the outskirts of Leyden, a city known for its rich history in arts (e.g., Rembrandt) and sciences.
The EFMC plans the next course on “New vistas in GPCR related drug discovery“ for Spring 2020. The course will be organized by Profs Gyorgy Keseru, Budapest and Rob Leurs, Amsterdam. Details on this course may be fund on the site of the EFMC soon.
NEWS OF THE SPANISH SOCIETY OF MEDICINAL CHEMISTRY (SEQT)
The Spanish Society of Medicinal Chemistry (SEQT) is organizing the 19th National Meeting “New challenges in drug discovery”, to be held in the Faculty of Pharmacy of the University of the Basque Country, Vitoria-Gasteiz (Spain) on July 8-11, 2019.
The scientific program will include both plenary and invited lectures as well as short oral communications and flash presentations, covering the main stages of drug discovery and development (provisional programme is shown on the website www.congresoSEQT2019.es.
Confirmed speakers to date
• Ignacio Alfonso (IQAC-CSIC, Spain)
• José Ignacio Andrés (Janssen Research & Development, Spain)
• Gonçalo Bernardes (University of Cambridge, UK)
• Maria Laura Bolognesi (University of Bologna, Italy)
• Erick M. Carreira (ETH Zürich, Switzerland)
• Kristof van Emelen (ProDigest BVBA, Belgium)
• Benoit Gauthier (CABIMER, Spain)
• Yvette van Kooyk (University of Amsterdam, The Netherlands)
• Luis M. Liz-Marzán (CIC Biomagune, Spain)
• Modesto J. Remuiñan (GlaxoSmithKline, Spain)
• Gianluca Sbardella (University of Salerno, Italy)
For further information and regular updates, please visit the website www.congresoSEQT2019.es
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is pleased to announce the call for nominations for the BMCS Hall of Fame & the Capps Green Zomaya Memorial Awards 2020, and some upcoming events.
BMCS Hall of Fame: call for nominations
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.
Independent nominations should include a one page synopsis detailing the justification and the candidate’s CV & publication list. The nomination may be further bolstered by additional independent letters of support. Nominations should be submitted by the end of September 2019.
For more information go to https://www.rsc.org/Membership/Networking/InterestGroups/BMCS/Activities/HallofFame.asp
Capps Green Zomaya Memorial Award 2020: Call for Nominations
The Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is pleased to invite nominations for the ninth Capps Green Zomaya Memorial Award in medicinal or computational chemistry.
The Award will be given to the individual judged to have made an important contribution to the discovery or development of new medicines. Nominations are invited for candidates, up to the age of 40, working in UK or international laboratories (candidates over the age of 40, who have taken career breaks, will be considered).
A Royal Society of Chemistry commemorative medal and certificate will be awarded to accompany the prize of £2,000.
Nominations should be submitted no later than 31st October 2019 to: Maggi Churchouse, RSC-BMCS Secretariat: E-mail: email@example.com
For further details, please access the activities link on www.rsc.org/bmcs
2nd RSC BMCS/ RSC CICAG Artificial Intelligence in Chemistry Symposium
2nd to 3rd September 2019, Fitzwilliam College, Cambridge, UK
The call for poster abstracts will close on 5th July
Synopsis: AI is experiencing a renaissance in development of new methods and practical applications to ongoing challenges in chemistry. This two-day conference will present the current efforts in applying these new methods. We will combine aspects of artificial intelligence and deep machine learning methods to applications in chemistry, agriscience, bioorganic chemistry, and chemical biology.
20th RSC / SCI Cambridge MedChem Symposium
8th to 11th September, Churchill College, Cambridge, UK
Synopsis: The 20th symposium, Europe’s premier biennial Medicinal Chemistry event, focussing on first disclosures and new strategies in Medicinal Chemistry. This conference will be of interest to both academic and industrial scientists engaged in all aspects of the drug discovery and development process.
THIS MONTH’S HIGHLIGHTED MEDCHEMCOMM ARTICLE IS:
“Discovery of 2-phenoxyacetamides as Inhibitors of the Wnt-depalmitoleating Enzyme NOTUM from an X-ray Fragment Screen”
In a collaborative study between UCL, the University of Oxford and The Francis Crick institute, Paul Fish et al. describe the development of NOTUM inhibitors that restore Wnt signaling for use in in vitro disease models where NOTUM over activity is an underlying cause. This article is part of the themed collection celebrating last year’s EFMC International Symposium on Medicinal Chemistry.
NOTUM is a carboxylesterase that has been shown to act by mediating the O-depalmitoleoylation of Wnt proteins resulting in suppression of Wnt signaling. Here, we describe the development of NOTUM inhibitors that restore Wnt signaling for use in in vitro disease models where NOTUM over activity is an underlying cause. A crystallographic fragment screen with NOTUM identified 2-phenoxyacetamide 3 as binding in the palmitoleate pocket with modest inhibition activity (IC50 33 μM). Optimization of hit 3 by SAR studies guided by SBDD identified indazole 38 (IC50 0.032 μM) and isoquinoline 45 (IC50 0.085 μM) as potent inhibitors of NOTUM. The binding of 45 to NOTUM was rationalized through an X-ray co-crystal structure determination which showed a flipped binding orientation compared to 3. However, it was not possible to combine NOTUM inhibition activity with metabolic stability as the majority of the compounds tested were rapidly metabolized in an NADPH-independent manner.
Read the article !
This article is part of the themed collection: Celebrating the 25th EFMC-ISMC
THE LATEST EDITION OF MEDCHEMCOMM, THE OFFICIAL JOURNAL OF THE EFMC, IS AVAILABLE AT:
EFMC SPONSORED EVENTS
May 15-17, 2019
2nd Molecules Medicinal Chemistry Symposium – Facing Novel Challenges in Drug Discovery
June 21, 2019
6th SEQT Young Researchers Symposium
June 27-30, 2019
Prague, Czech Republic
11th Joint Meeting on Medicinal Chemistry
July 3-5, 2019
55th International Conference on Medicinal Chemistry (RICT 2019)
EFMC ORGANISED EVENTS
September 1-5, 2019
EFMC-ASMC'19: EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry
September 5-6, 2019
EFMC-YMCS 2019: 6th EFMC Young Medicinal Chemist Symposium
September 6-10, 2020
EFMC-ISMC 2020: XXVI EFMC International Symposium on Medicinal Chemistry
EFMC ACCREDITED SCHOOL
June 30 – July 4, 2019
39th Edition of the European School of Medicinal Chemistry (ESMEC)
EFMC SPONSORED SCHOOLS
September 11-13, 2019
Summer School in Pharmaceutical Analysis (SSPA)
September 15-20, 2019
EUROPIN Summer School on Drug Design
Post doctoral Researcher Cheminformatics, Optibirum, Cambridge, United Kingdom
PhD/Post Doc positions at Université de Montréal (NSERC-Servier Research Chair in Medicinal Chemistry and Chemical Biology), University of MontreaL, Chemistry, Montreal, Canada