MedChemWatch
Monthly Newsletter June 2020

IN MEMORIAM HUIB OVAA (1973 – 2020)

It was with great sadness that we learnt of the death of Professor Dr. Huib Ovaa, Professor in Chemical Biology at the Leiden University Medical Center (LUMC). Huib was a world-class chemist and an international leader in the field of chemical biology. 

Born in 1973, Huib received his training chemistry at Leiden University and obtained a PhD degree from the same institution in 2001, with ‘Cum Laude’. From 2001 to 2004, Huib was first a postdoctoral fellow and then a junior faculty member at Harvard Medical School, where he expanded his research interest in immune chemistry and biochemical processes. In 2004 Huib returned to his home country, joining the Netherlands Cancer Institute as a principal investigator in chemical biology. In 2016 he moved his laboratory to LUMC, where he became a Professor in 2017.

During his career, Huib made significant and decisive contributions to chemical biology and medicinal chemistry, being recognized worldwide for his breakthrough research in the ubiquitin proteasome system. Ubiquitin and ubiquitin-like proteins are important post-translational protein modifiers central to a range of cellular processes that are dysregulated in a variety of diseases, but the mechanistic details of their function remain poorly understood. Huib addressed this challenging topic by designing unique chemical probes that paved the way to the study of deubiquitinating enzymes as therapeutic targets in cancer and neurodegenerative diseases. His interests also extended to ubiquitin ligases, proteins that directly assists the transfer of ubiquitin from an ubiquitin-conjugating enzyme to a protein, targeting this substrate for destruction by the proteasome. Remarkably, Huib was also an entrepreneur, using his expertise to co-found UbiQ, a company dedicated to development of ubiquitin research tools.

EFMC would like to remember Huib’s outstanding lecture at the EFMC-ACSMEDI Medicinal Chemistry Frontiers 2019 meeting in Krakow, where he elegantly presented his contribution to the study of protein ubiquitination and deubiquitination and its impact in drug discovery efforts.

EFMC regrets the loss of this brilliant scientist and presents its condolences to his family, his team and to Leiden University.

 

EFMC VIRTUAL EVENTS 2020

Due to the extraordinary circumstances created by the coronavirus pandemic, the EFMC has decided to hold a series of virtual events throughout the following months. Our aim is to appeal to the broad medicinal chemistry and chemical biology community and we hope to see you soon.  

  • EFMC-YSN MedChemBioOnline

This series of regular free to attend webinars, mixing science, soft-skills trainings and round table discussions, has been created to meet the current needs of our scientific community to continue interacting and sharing ideas and innovation, as well as providing early career scientists with opportunities to listen to outstanding scientists and expand their knowledge.

The second edition of the event will take place on June 30 (17.00 – 19.15 CEST) with a lecture on "Critical Targets and Drug Design to Combat Covid-19" by Prof. Arun K. Ghosh (Purdue University, United States) and a soft-skill training & round table discussion on stress management.

Website & registrations: www.efmc.info/efmc-ysn-medchembioonline

Recordings of the 1st edition are available on the EFMC YouTube Channel

  • EFMC-ISMC Virtual Event 2020: First Time Disclosures & Late Breaking News

A 2-days Virtual Event will take place on September 7-8, 2020 and will focus on two of the most popular EFMC-ISMC sessions. Have a look at the already confirmed speakers to-date.

Website: https://www.efmc-ismc-virtual.org/ | Registrations to open soon!

  • Virtual 7th EFMC Young Medicinal Chemist Symposium 2020

The 7th edition of the EFMC-YMCS will take place as free virtual event this year on the original dates of 10th and 11th September 2020.

The programme will feature keynote lectures by Prof. Pablo Rivera Fuentes (EPFL, Switzerland) and Prof. Angela Russell (University of Oxford, United Kingdom), oral communications by invited prize winners from national young medicinal chemist meetings in Europe, and two soft-skills training sessions.

Website & registrations : https://www.efmc-ymcs-virtual.org/

  • EFMC-YSN Virtual Poster Session

For all those who were looking forward to giving posters in Basel at EFMC-ISMC and EFMC-YMCS, the EFMC will propose a 24h virtual poster event on Twitter.

An abstract book will be available and 10 best poster prizes will be offered by the EFMC.

The event will take place on September 9 and more information will follow soon!

LITERATURE SPOTLIGHT

The “literature spotlight” section of the newsletter will bring you a summary of the recently published research in a concise and readable way. Multiple thematics from different journals will be highlighted thanks to the valuable contribution of Dr Clemens Zwergel (University of Rome, IT) from the communication team.

This fourth contribution will focus on the recently published article on innovative nanoparticles to fight P. aeruginosa infections (by Ho et al. in Angewandte Chemie).

Even though in the last months viral infections seem to be the top priority in research, we should not forget bacterial infections and the growing resistance to existing antibiotics. The elimination of resistant Pseudomonas aeruginosa (PA) infections, one of the most virulent pathogens causing nosocomial infections worldwide, is very challenging. Recently quorum sensing inhibitors (QSIs) interfering with biofilm formation have been a promising approach in combination with other antibiotics. Recently Ho et al. published an inspiring approach for simultaneous and improved pulmonary delivery of the hydrophilic antibiotic tobramycin (Tob) and a novel lipophilic QSI, described earlier by the same institute, to the infection sites through self-assembling squalenyl hydrogen sulfate nanoparticles (SqNPs). 

The proposed SqNPs preparation is a straightforward and scalable process. Importantly, the SqNPs were found to be compatible with human cells and also showed no toxicity on zebrafish embryos. The drug-loaded SqNPs showed improved biofilm penetration and enhanced efficacy in relevant biological barriers (mucin/human tracheal mucus, biofilm), leading to complete eradication of PA biofilms using a 16-fold lower Tob concentration than with Tob alone. This is especially notable as the currently available inhalation therapeutics are limited by their inability to overcome the strong penetration-limiting biological barriers protecting bacteria from anti-infective agents in the lungs.
The innovative approach and the promising data will hopefully allow a rapid clinical translation of new therapeutic modalities based on optimized QSI candidates and their co-delivery with suitable antibiotics.

Ho, D.-K., Murgia, X., De Rossi, C., Christmann, R., Hüfner de Mello Martins, A.G., Koch, M., Andreas, A., Herrmann, J., Müller, R., Empting, M., Hartmann, R.W., Desmaele, D., Loretz, B., Couvreur, P. and Lehr, C.-M. (2020), Squalenyl Hydrogen Sulfate Nanoparticles for Simultaneous Delivery of Tobramycin and an Alkylquinolone Quorum Sensing Inhibitor Enable the Eradication of P. aeruginosa Biofilm Infections. Angew. Chem. Int. Ed.. doi:10.1002/anie.202001407
https://onlinelibrary.wiley.com/doi/10.1002/anie.202001407

BEST PRACTICES IN MEDICINAL CHEMISTRY: COPYRIGHT

Copyright broadly refers to the legal rights of an owner of intellectual property, but the principles are not always clear to non-experts. Copyright is, however, present at every stage of scientific research and we face their implications daily, sometimes without knowing it.

In two slide decks, Martine Roth (Principal Trademark Attorney & Copyright at Novartis Pharma AG) briefly present the basic of copyright and introduce "Creative Commons", a nonprofit organization enabling the sharing and use of creative works through free legal tools.

Files can be found under this link.

GET TO KNOW FERRAN SANZ, POMPEU FABRA UNIVERSITY, SPAIN

In this edition, our #Iamamedicinalchemist is Prof. Ferran Sanz from the Pompeu Fabra University, Spain.

He was President of the EFMC from 2002 to 2005 and received the title of EFMC Honorary Fellows in 2020.

 

How did you get interested in Medicinal Chemistry?

It was at the beginning of my scientific career, when I was just a PhD student. I became interested in the interface between chemistry and biology and more concretely and how the, at that time incipient, molecular modelling methods, might contribute to the understanding of the mechanism of action of drugs.

Where and when did you obtain your PhD diploma?

I obtained my PhD diploma in 1982 in the Autonomous University of Barcelona. The topic of my PhD was the study of differential molecular determinants of MAO-A and MAO-B inhibitors using computational approaches.

Where do you work at the moment and what is your current position?

I am currently director of a Research Program on Biomedical Informatics, which is a joint program of the Pompeu Fabra University and the Hospital del Mar Medical Research Institute, located in Barcelona. My current research is focused on the development of new computational strategies and tools serving the biomedical research.

What do you like most in your job?

The most interesting aspect of my job is its multidisciplinary nature. The projects that we develop and the research team that I lead synergically integrate knowledge and professionals from several disciplines, such as medicine, biology, computer sciences, chemistry and pharmacy.

What kind of tasks your job includes?

As director of a program (a kind of academic department), constituted by more than sixty professionals including ten principal investigators and their groups, I have tasks related with the coordination and strategic guidance of the program, including bureaucratic duties that, as you can imagine, are the less attractive. In addition, I have some direct collaborators within the program, and I develop my own research projects in collaboration with them.

What kind of skills your job requires?

My job requires scientific and human experience and I think that have a lot of this taking into account my age.

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

I am particularly proud of the DisGeNET knowledge resource on gene-disease associations that we have been developing along the last ten years. It has become a worldwide recognized resource with more than 5000 users per month and more than 1000 bibliographic citations.

What is the most embarrassing thing you did in the lab while doing experiments?

Since I use to work in silico (computational) labs, explosions are not particularly usual, but we remember incidents related with floods in the room were our computer servers are located, which were particularly damaging.

Which scientist do you admire the most and why?

I particularly appreciate the history of Paul Janssen and his ability for leading an international pharmaceutical company without abandoning his direct involvement in the successful discovery of new drugs.

Which paper of yours you are the proudest of and why?

The papers that we have published about the DisGeNET resource, for instance the last one recently published in Nucleic Acids Research. I am also proud of my paper in Nature Reviews in Drug Discovery in which we reported the results of the IMI eTOX project on data sharing in predictive toxicology.

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

I am probably biased in this respect, but I think that the computational methods and tools offer great opportunities to medicinal chemistry. In particular, the joint exploitation of the biological, chemical and medical big data is very promising for improving the drug discovery process.

What would you like to ask from other medicinal chemists?

I would ask my colleagues to keep them always open-minded, combining their deep experience in the field of their specialization with a global scientific perspective.

What would you guess to be the next major breakthrough in medicinal chemistry?

Given my current professional focus, I do not have a deep insight on all the facets of the medicinal chemistry. However, I think that the incorporation of the systems biology perspective in the design of new drugs offers interesting perspectives.

Want to share your story with us? https://www.efmc.info/interviews-efmc 

RESULTS OF THE 3RD AND FINAL EFMC QUIZ

Congratulations to Adam Smalley (United Kingdom) for winning the 3rd EFMC Quiz with all the correct answers!

Two runners-up follow closely with 19 correct answers out of 20: Hrvoje Rimac (Hungary) & Usman Shabbir (United Kingdom).

We thank all the participants of the three quizzes for their massive participation, and we look forward to starting again soon!

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

The BMCS Committee has taken the decision to cancel all meetings in which it is part of the organising team up to and including the ‘8th RSC / SCI symposium on GPCRs in Medicinal Chemistry’ in September.

The BMCS announces the call for its Malcolm Campbell Memorial Prize and RSC-BMCS Hall of Fame.

MALCOLM CAMPBELL MEMORIAL PRIZE 2021

To continue the commemoration of his outstanding contributions in a broad range of chemistry and their application to the understanding of bioactivity, the Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is proud to invite nominations for the ninth Malcolm Campbell Memorial Prize. The prize will be awarded to the individual or team based in UK academia or industry who, in the judgement of the BMCS committee, has made the most significant scientific contribution to biological chemistry. Nominations could be from either discovery and/or process development and include medicinal, agrochemical or aromachemical research. The work should be timely and contemporaneous. A medal and certificate will be awarded to accompany the prize of £2,000.
Nominations should be submitted no later than 31st October 2020 to:
Maggi Churchouse, RSC-BMCS Secretariat, e-mail: maggi@maggichurchouseevents.co.uk
For further details, please access the activities link on www.rsc.org/bmcs
#BMCS_MCMP

RSC-BMCS HALL OF FAME AND MEDAL 2020 CALL FOR NOMINATIONS

The BMCS is pleased to announce the 2020 call for nominations for its Hall of Fame and associated medal which recognises chemists for outstanding, sustained, significant contributions to any area of interest to the BMCS including medicinal chemistry, agriscience, bio-organic chemistry, and chemical biology.
Independent nominations may be submitted by e-mail outlining the justification and including the nominee’s CV and publication list. Additional independent letters of support to reinforce the nomination are strongly encouraged. Nominees should be resident in the UK or continental Europe, or have spent a considerable proportion of their career there. There is no requirement to be an RSC or BMCS member. There are no age restrictions, and nominees may have an academic or industrial background.
Nominations should be submitted by the end of September 2020 and the outcome will be communicated to nominators and nominees by mid-December 2020. Inductees will receive a medal and certificate, and will be invited to give a plenary lecture at an appropriate BMCS organized conference.
For further details, see the full list of requirements and terms and conditions on the RSC website below. Independent nominations should be sent by e-mail to maggi@maggichurchouseevents.co.uk by 30th September 2020
#BMCS_HoF

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

The quarterly Chemistry in Europe newsletter is available online here

THIS NEWSLETTER IS KINDLY SPONSORED BY MERCACHEMSYNCOM


 

ISSUE SPONSORED BY

MercachemSyncom is the leading major European drug-discovery CRO for solving your chemistry challenges, from small to medium-sized molecule hits, to the first GMP batches of identified clinical candidates. To capture a glimpse of our capabilities, please visit our webinar on 17 June. 

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EFMC ORGANISED EVENTS

June 30, 2020
Online
EFMC-YSN MedChemBioOnline

September 7-8, 2020
Online
EFMC-ISMC Virtual Event 2020: First Time Disclosures & Late Breaking News

September 10-11, 2020
Online
EFMC-YMCS Virtual Event 2020: Virtual 7th EFMC Young Medicinal Chemist Symposium

October 18-21, 2020
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry: New Opportunities in GPCR Drug Discovery

EFMC SPONSORED EVENTS

October 26-27, 2020 
Eindhoven, The Netherlands
A Joint Future for Medicinal Chemistry and Chemical Biology in the Netherlands

November 5-7, 2020
Athens, Greece
18th Hellenic Symposium on Medicinal Chemistry (HSMC-18)

EFMC SPONSORED SCHOOL

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

JOB PORTAL

Postdoctoral scholar: Biocatalysis, Novartis Institutes for BioMedical Research, Basel Switzerland

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