MedChemWatch
Monthly Newsletter March 2020

TAKE THE EFMC QUIZ AND WIN AN EFMC GOODIEBOX

To celebrate our 50th anniversary, the EFMC Communication Team is launching a quiz mixing scientific questions & questions about the EFMC. 

Three Winners will be selected from the correct answers and will receive an EFMC GoodieBox full of surprises! 

Be quick, entries close on March 31!

Take the Quizz!

REVIVED SECTION: LITERATURE SPOTLIGHT!

The “literature spotlight” section of the newsletter will monthly 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 first contribution will focus on the recently published article on novel vaccination strategies for B. pertussis (by Wang et al. in Angewandte Chemie)

Pertussis, also known as whooping cough, is a highly contagious respiratory disease caused primarily by the infection of a Gram-negative bacterium Bordetella pertussis. Even though there are already vaccines already available, 24.1 million infections and 160,700 deaths have been estimated worldwide in children younger than 5 years alone each year due to pertussis even in developed countries suggesting an urgent need for a new vaccination approach. Wang et al. recently published an interesting article on Angewandte Chemie on novel vaccination strategies for B. pertussis. This bacterium possesses multiple rare sugars and unusual glycosyl linkages being a highly challenging medicinal chemistry target.

Molecular dynamics simulations and modeling allowed for the first time the chemical synthesis of the pertussis LPS like pentasaccharide containing three unusual sugar units (2-acetamido-2,4,6-trideoxy-4-methylamino L-galactose, mannoheptose, and 2,3-diacetamido mannuronic acid). The synthetic procedures involved exacting steps in building block preparation as well as stereochemical control in glycosylations.

The synthetic pentasaccharide was conjugated with a powerful carrier, bacteriophage Qβ as a vaccine candidate for the analysis of its potential as an antigen for anti-pertussis vaccine development comparing it to a gold standard glycan carrier KLH.

Immunization of mice with the conjugate of the pentasaccharide with a protein carrier, bacteriophage Qβ, led to anti-glycan IgG titers of several million ELISA units eliciting a significantly higher IgG antibody titer than the control. The antibodies generated were long lasting and boostable, and could recognize multiple clinical strains of B. pertussis

To sum up, the novel pentasaccharide is a promising starting point towards the development of new anti-pertussis vaccines.

Wang, P., Huo, C.''.chr('8208').''x., Lang, S., Caution, K., Nick, S.T., Dubey, P., Deora, R. and Huang, X. (2020), Chemical Synthesis and Immunological Evaluation of a Pentasaccharide Bearing Multiple Rare Sugars as a Potential Anti''.chr('8208').''pertussis Vaccine. Angew. Chem. Int. Ed.. doi:10.1002/anie.201915913

https://onlinelibrary.wiley.com/doi/10.1002/anie.201915913

THE EFMC JOB PORTAL OPENS TO PHD AND POST-DOC POSITIONS

The EFMC Job Portal is now also open to PhD and Post-Doc positions!

We invite everyone who has an open opportunity to advertise it through the EFMC. This service is free, open to all and widely advertised on the EFMC media channels.

Submit your advert via this link. It will be reviewed internally before publishing.

Follow also the #medchemjob on our various EFMC social media to stay updated.

MEET FILIPA RAMILO GOMES, THE NEW EFMC COMMUNICATION TEAM MEMBER

The EFMC Communication Team & Young Scientists Network is happy to introduce its newest member: Mrs Filipa Ramilo Gomes from the Instituto Superior Técnico (Universirty of Lisbon), Portugal. 

Filipa has already been very active and helpful in promoting the EFMC and the YSN, so we are lucky to have her on board! 

Want to know more about her? Read her #Iamamedicinalchemist interview below

 

Where and when did you obtain your PhD diploma?

For the past 4 years I have been working on my PhD at Instituto Superior Técnico, University of Lisbon, Portugal, under the supervision of Prof. M. Matilde Marques, Prof. Rita Guedes and Dr. Luís Sobral. I expect to obtain the degree during this Summer 2020. As part of my PhD project, I also collaborated with Inteligand Company, the University of Vienna and the Fraunhofer Institute.

What is the topic of your PhD project?

My PhD project focuses on epigenetics in cancer. I designed new EZH2 inhibitors, using 3-D pharmacophore models. Following this computational campaign, I selected and synthetized some of the most promising molecules with the intent of testing them against the target. Both biochemical and cellular assays were developed and implemented in order to identify hit compounds. In addition, ADMET profiling of the hits was also performed.

What are your current research interests?

As a Pharmacist, I would like to further build a research career in the development of new medicines. Metabolism and toxicity studies are expertise areas in which I would strive for an opportunity to work on.

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

My scientific career is still young, but I felt particularly rewarded that my computational models actually yielded hit compounds with good activity against my selected target.

Which scientist do you admire the most and why?

It is impossible for me to consider just one scientist. I admire many scientists who I have met during my scientific journey. I had the privilege to have meaningful conversations and learn a lot with people who are passionate about their research. People who work beyond the lab and dedicate their work so others may benefit. People with honest behavior, integrity, resilience and a sense of responsibility. People who give a voice to the aspiring scientists.

I feel mostly inspired by the examples set by women in science. Unfortunately, I feel that nowadays, women researchers still do not get the same attention, as well as credibility, enjoyed by their male counterparts. This cultural issue has been evolving in a positive way, however it is a struggle that we, women, inspired by other scientists who set the tone and example, should keep in mind and use as an extra inspiration in our daily work.

Fortunately, I have had many examples of people who can inspire others and I am grateful to all of them, particularly my supervisors for influencing and shaping the way I look at science, the way I work every single day.

Did you experience any unfair situations during your scientific career?

Unfortunately, there is a lack of opportunities in science in Portugal. I have contacted and felt the frustration in many young talents, who get discouraged and abandon their scientific careers.

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

At this stage in my career, I would say my next one!

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

I consider that medicinal chemistry is trending from therapeutics to diagnosis. Future will focus beyond the therapeutic target discovery and design of new modulators. Diverging from the actual amount of effort in trying to cure certain diseases (which should be always a purpose in medicinal chemistry) or develop new drugs with improved safety or efficacy profiles, I believe that the future of medicinal chemistry will allow us more certain, clear, and well-timed diagnosis of certain diseases, allowing us to prevent them, or at least have a better prognosis for them.

Predictive toxicology of the drugs is one promising field in medicinal chemistry. In a near future we could describe a complete ADMET profile using computational tools and large-scale in vitro models.

Thanks to the disruptive emerging technologies, Medicinal Chemistry will change. Big data, machine learning, artificial intelligence will all be crucial in changing the traditional Medicinal chemistry. The trends in cutting-edge innovation will be transversal to all the Medicinal Chemistry.

GET TO KNOW JACOB BUSH (GSK, UNITED KINGDOM)

Meet Jacob Bush, the Most-Meritorious Runner-Up in the EFMC Prize for a Young Medicinal Chemist in Industry 2019.

 

How did you get interested in Medicinal Chemistry?
As an undergraduate I enjoyed the language and logic of organic chemistry and was motivated to use these skills in an applied setting. I began to explore biomedical sciences and saw Chemical Biology as an opportunity to use chemistry to study life at a molecular level, whilst helping to discover transformational medicines for patients.

Where and when did you obtain your PhD diploma?
At the University of Oxford under the supervision of Prof. Christopher Schofield.

What was the topic of your PhD project?
Chemical biology approaches to study the pathways that cells use to sense oxygen.

Where did you have your postdoc position?
At the end of my PhD, many opportunities appealed to me. I loved the environment of academia but had also become increasingly interested in the translation of research. An opportunity at GSK was advertised and at the interview I was impressed by the freedom to work creatively, and to use innovation to have an impact on the lives of millions of patients. GSK has proved a fantastic place to work, with many outstanding scientists and a culture that follows the science.

Where do you work at the moment and what is your current position?
I am a team leader in a newly formed Chemical Biology department at GSK. My focus is on the development and industrialisation of new technologies to accelerate the discovery of potential new medicines. A big part of my role is to develop collaborations with academia which helps us harness a broader range of ideas to solve difficult scientific problems. I recently joined the Crick-GSK LinkLabs which is a chance to work with world-leading experts in biomedical sciences.

What are your current research interests?
Currently, we are building platforms to rapidly develop inhibitors for targets emerging from genomic studies - an area we are investing in significantly to identify and validate targets. We are also combining chemoproteomic and chemogenomic approaches to discover new targets with therapeutic potential. One focus area is using covalent fragments. Advances in proteomic technologies have created an opportunity to perform covalent fragment screening directly in live cells, providing more comprehensive and biologically relevant information of ligand interactions, while also circumventing the requirement for protein production and assay development. Such approaches enable exploration of unchartered biological space, and generation of large databases of ligand interactions across the proteome.

What do you consider your biggest achievement in your scientific career?
Machine learning and artificial intelligence are two of the most exciting technologies impacting drug development. One of the highlights of my career has been exploring the application of machine learning algorithms to accelerate drug discovery. Right now, I am excited to be at the forefront of the data-rich technologies we are building in chemical biology and to see how these new technologies will impact this field in the next year or so.

How many PhD and postdoc students do you have at the moment?
Are you currently looking for a new PhD and postdoc students?
I work with a team of PhDs at GSK and a team of post docs in the LinkLabs at the Francis Crick Institute. We are always looking for outstanding scientists, look up the GSK-Strathclyde collaborative PhD programme and the GSK-Crick LinkLabs on the GSK website.
What are the features of a successful PhD student or postdoc?
Understanding the context of your work and how it fits in with the research environment around you is essential to help prioritise workflows and focus your efforts for maximum impact. Also, working collaboratively and sharing your science and ideas is hugely beneficial, as well as more enjoyable.

Which scientist do you admire the most and why?
Carolyn Bertozi is doing some fantastic work in chemical biology and glycobiology. If you get the chance to catch one of her lectures or podcasts, I’d recommend it, she presents her work in a remarkably accessible and inspiring way.

Which field of medicinal chemistry do you consider the most promising in the future?
Tough question. I anticipate a shift away from studying one compound at a time in biochemical assays. There are so many exciting technologies and approaches emerging: chemoproteomics, chemogenomics, DNA encoded libraries, machine learning, covalent fragments, PROTACs and other bifunctional molecules. With all of these though, it will be important not to assume the technology will offer all the solutions, but to ensure it amplifies traditional medicinal chemistry.

ESMEC ALUMNI AWARD – APPLICATION DEADLINE IS MARCH 31

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 nominationsis: March 31, 2020

Applicants are invited to fill in the application form and to send their 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
e-mail: lucia.bedini@uniurb.it

INTERESTED TO LEARN MORE ABOUT “NEW OPPORTUNITIES IN GPCR DRUG DISCOVERY”? REGISTER FOR THE EFMC SHORT COURSE

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.

Deadline for Early Bird fee is March 30! Number of seats is limited.

Discover the speakers!

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.

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

2nd RSC BMCS / RSC NAG NUCLEOSIDES AND NUCLEOTIDES
21st April 2020, RSC, London, UK
The call for poster abstracts will close on 11th March
Website: http://www.rsc.org/events/detail/40136/rsc-bmcs-and-rsc-nag-2nd-nucleosides-and-nucleotides-synthetic-and-biological-chemistry

Synopsis: This meeting seeks to explore and celebrate the chemistry that drives the development of modern nucleoside and nucleotide chemistry. It will bring together scientists who work at the interfaces of synthetic and biological chemistry to deliver new tools and insights for biology, and new leads for drug development.

3rd RSC / SCI / DMDG TRANSPORTERS IN DRUG DISCOVERY AND DEVELOPMENT
21st-22nd April 2020, SCI, London, UK
Website: http://www.rsc.org/events/detail/41920/the-3rd-sci-rsc-symposium-on-transporters-in-drug-discovery-and-development

Synopsis: Cell surface transporters play a key role in human health and disease, both through their impact on drug disposition and as therapeutic targets in their own right. This third meeting in the series will feature talks on transporter structural biology, the impact of transporters on ADME and biodistribution, transporters as therapeutic targets and other aspects of transporters relevant to drug discovery and development.

4th AGRI-SCIENCE CHEMICAL BIOLOGY POSTGRADUATE SYMPOSIUM
22nd April 2020, White City Campus, Imperial College, London, UK
Website: http://www.rsc.org/events/detail/42681/4th-agri-science-chemical-biology-postgraduate-symposium

Synopsis: For PhD and postdoctoral students undertaking chemical biology research in areas related to agriculture and the agrisciences. Chemical Biology in this context refers to physical sciences tools and technologies (in Chemistry, Physics, Mathematics, and Engineering) that are being applied to tackle biological problems in the agri-sciences, at a molecular level. This conference brings together PhD and postdoctoral students from different research communities to showcase the current state of fungal, insect and plant chemical biology achievements within the spirit of multidisciplinary interaction and engagement

NEWS FROM EUCHEMS: 3RD EMPLOYMENT SURVEY FOR EUROPEAN CHEMISTS IS OPEN

The 3rd Employment Survey for European Chemists (ESEC3) opened on March 1, 2020. Participation in this survey will be open for all chemists and chemical engineers in Europe.

The online survey is available here: https://www.euchems.eu/esec3/

ESEC3 has been jointly prepared by EuChemS, its Young Chemists’ Network, the European Chemistry Thematic Network Association and part of it in collaboration with the American Chemical Society. It is supported by FECCIA and Cefic.

Learn more about it here

THIS NEWSLETTER IS KINDLY SPONSORED BY CRESSET


 

ISSUE SPONSORED BY CRESSET

Cresset provides software solutions and discovery services for small molecule design to pharmaceutical, biotech, agrochemical, flavour and fragrance companies. In collaboration with Elixir Software, Cresset has developed Torx™ - the only collaborative platform that truly accelerates every part of the Design-Make-Test-Analyze workflow.

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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

EFMC SPONSORED EVENTS

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

May 5-6, 2020
Liverpool, United Kingdom
5th RSC / DMDG / DMG New Perspectives in DMPK

June 1-2, 2020
London, United Kingdom
9th RSC / SCI Symposium on Kinase Inhibitor Design

EFMC SPONSORED SCHOOLS

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

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

JOB PORTAL

Assistant/Associate/Full Professors in Chemistry, Leiden University, Leiden, The Netherlands

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MoSMed Studentships at Durham University, Durham University, Durham, United Kingdom

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MoSMed Studentships at Newcastle University, Newcastle University, Newcastle, United Kingdom

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