THE EFMC YEARBOOK 2021 IS AVAILABLE
The official EFMC Yearbook 2021, "Medicinal Chemistry and Chemical Biology in Europe" is a valuable resource for those interested in quickly finding information on all things 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 imprint, EFMC have decided to produce the Yearbook as an electronic version only. For an optimal read through of the Yearbook, we recommend using Microsoft Edge or Firefox.
READ THE PDF VERSION
The “literature spotlight” section of the newsletter will bring you a summary of the recently published research in a concise and readable way. Papers covering a range of medicinal chemistry and chemical biology from a variety of journals will be explored by the Communication Team; today’s excerpt is brought to you by Dr Nadia M. Ahmad (Charles River Laboratories).
This tenth contribution will focus on the recently published article on the “Nonpungent N''.chr('8209').''AVAM Capsaicin Analogues and Cancer Therapy” (by Dasgupta et al. in J. Med. Chem.).
The need for anticancer therapies is never-abating, and therefore novel therapies, modes of action, and new starting points are constantly being sought. Dasgupta et al. have recently described the optimisation of non-pungent capsaicin-like analogues for the treatment of several cancers. Capsaicin analogues tend to be more closely associated with the treatment of pain, particularly when binding at the transient receptor potential vanilloid (TRPV) receptor family, and of these particularly so as potent agonists of TRPV1. That said, while capsaicin and its analogues have now been found to have anticancer properties, this does not arise from their activity at the TRPV1 receptor. In fact, capsaicin and its analogues act by a signalling pathway which eventually downregulates a ‘Substance P’, a neuropeptide that in turn helps trigger the release of inflammatory cytokines.
Capsaicin analogues as clinical compounds have the disadvantage of poor pharmacokinetic properties including, amongst others, minimal aqueous solubility and poor bioavailability. As such, efforts have been made in extensive SAR studies to identify and subsequently optimise non-pungent capsaicin analogues. Of all these, the N-acyl vanillylamide (N-AVAM) family have received the most attention – not only are they improved analgesics compared to capsaicin, but they also side-step the cancer-inducing profile of capsaicin itself. The authors describe their second-generation approach to N-AVAM capsaicin analogues with improved PK properties and therapeutic index via the use of molecular modelling and high-through virtual screening experiments. This included the design of analogues using a pharmacophore model, isolation of N-AVAM capsaicin analogues from natural sources, as well as generation of analogues using plant oils as starting materials, and more traditional synthetic chemistry. The authors were able to design and synthesise analogues which suppressed the growth and invasion of, for example, human small cell lung cancer cells, at 20-fold lower concentration compared to capsaicin. While the PK profiles of the compounds do still require further optimisation, the authors describe the use of nanoparticles as a method to produce sustained-release formulations and, in doing so, particularly improve the bioavailability. With these, and subsequent, improvements, the hope for potential novel N-AVAM capsaicin analogue-based therapies in appropriate combinations remains high.
Stephen D. Richbart, Jamie R. Friedman, Kathleen C. Brown, Rama S. Gadepalli, Sarah L. Miles, John M. Rimoldi, Gary O. Rankin, Monica A. Valentovic, Maria T. Tirona, Paul T. Finch, Joshua A. Hess, Piyali Dasgupta*
Nonpungent N''.chr('8209').''AVAM Capsaicin Analogues and Cancer Therapy
J Med Chem. 2021 Jan 12, ASAP
DOI: doi/10.1021/acs.jmedchem.0c01679 PMID: 33433953
XXVI EFMC INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY (EFMC-ISMC 2021) – CALL FOR ABSTRACTS
The EFMC, together with the International Organising Committee, have decided that the XXVI EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2021) will be run as a fully Virtual Event, from August 29 to September 2, 2021. We are convinced that this is the right decision to allow as many scientists as possible to safely take part in this important scientific gathering.
Calendar of Abstract Submissions
- Deadline for Oral Communication submission and free Poster submission: March 25, 2021
- Announcement of the accepted oral communications: mid-May, 2021
- After March 25, 2021 and until June 24, 2021, abstracts for Posters can still be submitted, but with a handling fee of 50,00€
EFMC-ISMC 2021 will cover advances in drug discovery in major therapeutic areas, including bacterial and viral infections, diseases of the brain, heart, and respiratory system, fibrotic diseases, and cancer. EFMC-ISMC 2021 will also feature most recent advances in new technologies such as artificial intelligence in drug discovery and chemical synthesis, the role carbohydrates in disease pathology and carbohydrate-based drug discovery, the exploitation of RNA as drug target, small molecule-induced stem cell differentiation, or the impact of cryo-EM on drug discovery and design.
In a series of dedicated sessions, the interface between chemical biology and drug discovery will be highlighted, including topics such the use of chemical probes for target discovery, molecular imaging, and photochemical approaches. In response to frequent requests by attendees of previous conferences, two sessions will be dedicated to advances in synthetic methodology for drug discovery. Finally, particular emphasis will again be put on first time disclosures and recent highlights in medicinal chemistry.
Discover the list of confirmed speakers.
More information and registration on www.efmc-ismc.org.
Share the news on social media with the #EFMC_ISMC.
EFMC GRANTS 2021 – APPLICATIONS ARE OPEN
EFMC is funding grants for EFMC organised events with the aim to support the participation of young academic scientists. Upon application, EFMC will cover full registration fees of up to 20 applicants.
To apply for an EFMC grant, please fill in the application form and upload your CV, publication list, abstract, motivation letter, and support letter from the supervisor.
Deadline for EFMC-ISMC Symposium: March 25, 2021.
Participation of both "EFMC-ISMC" & "EFMC-YMCS" is mandatory in order to receive the grant.
More information and application on www.efmc.info/ysn-grants.
GET TO KNOW JESSICA REYNOLDS (UNIVERSITY OF OXFORD, UNITED KINGDOM)
In this edition, our #Iamamedicinalchemist is the winner of the 2020 EFMC-YMCS Presentation Prize, Dr Jessica Reynolds (University of Oxford, United Kingdom). She is currently writing her DPhil thesis and has been awarded the EPSRC Doctoral Prize, allowing her a further six months after hand in to complete her work with Professor Stuart Conway, and explore new ideas.
What is the topic of your PhD project?
My project focuses on exploring different chemical tools to probe the function of TRIM proteins. We have developed small molecule probes targeting the bromodomain of TRIM33, and have incorporated these ligands into the design of proteolysis-targeting chimeras.
What do you like most in your job?
I enjoy the collaborative and interdisciplinary nature of medicinal chemistry which provides so many opportunities for learning new skills. Sharing knowledge and expertise is certainly the best way to advance science!
Which scientist do you admire the most and why?
I really admire Frances Arnold for her work on directed evolution of enzymes, the applications of the work are astounding and will definitely change our world for the better.
Which field of medicinal chemistry/chemical biology do you consider the most promising in the future?
I think PROTACs are fascinating tools for probing protein function. I am very interested to see the results of the cancer-targeting PROTACs currently in clinical trials. If they are successful, it will open up a whole new path for cancer treatment.
You want to share your story with us!? Answer our questionnaire and contact the Communication Team (email@example.com)
NEWS FROM THE SECTION FOR MEDICINAL AND PHARMACEUTICAL CHEMISTRY OF THE CROATIAN CHEMICAL SOCIETY
For the last four years, the Section for Medicinal and Pharmaceutical Chemistry of the Croatian Chemical Society has organised mini symposia on Medicinal and Pharmaceutical Chemistry. The main goal of the mini symposia was to enable young scientists, mainly PhD students and postdocs, to present their scientific work. Other than learning about other people's scientific work, presenters work on their presentational skills and get valuable feedback in a friendly environment. In all, this is a good opportunity for young scientist to grow, learn new things, meet new people and potentially start scientific collaborations. During the first three mini symposia, a total of twenty four young scientists presented their research.
The last i.e. the 4th mini symposium of Medicinal and Pharmaceutical Chemistry was held in December 2020 with ten young researchers presenting their work. Because of the COVID-19 pandemic, the symposium was held virtually. This enabled our small scientific community to continue to share ideas and network, albeit in a slightly different way. Other than being able to give scientific talks from their own home, this mini symposium was open to the public and more than 60 people attended, which is the highest number of attendees so far.
To motivate young researchers to continue their scientific work in the field of pharmaceutical and medicinal chemistry, the Section for Medicinal and Pharmaceutical Chemistry of the Croatian Chemical Society and Fidelta Ltd. established the Award for Young Medicinal and Pharmaceutical Chemists in 2019. The Award will be given each year to young scientists under the age of 35 in recognition of excellent scientific achievements in the field of medicinal and pharmaceutical chemistry.
The Award committee consists of representatives of the Section for Medicinal and Pharmaceutical Chemistry of the Croatian Chemical Society and Fidelta d.o.o., who have so far presented two Awards to young scientists. In 2019, the Award was given to Dani Škalamera PhD, for his presentation on the 3rd Mini-symposium of Medicinal and Pharmaceutical Chemistry titled “Synthesis and Evaluation of QS-17/18-Based Vaccine Adjuvants”. In 2020, the Award was given to Maja Beus PhD, for her presentation on the 4th Mini-symposium of Medicinal and Pharmaceutical Chemistry, titled “Combating Bacterial Communication with Chloroquine-Based Fumardiamides”.
The Section for Medicinal and Pharmaceutical Chemistry is looking forward to organizing future Mini symposia and supporting young medicinal chemists in their scientific journey.
NEWS FROM THE DIVISION OF MEDICINAL CHEMISTRY OF THE GERMAN CHEMICAL SOCIETY (GDCH)
The German Chemical Society (GDCh), the German Pharmaceutical Society (DPhG) and the Swiss Chemical Society (SCS) cordially invite you to attend the annual meeting on ´Frontiers in Medicinal Chemistry´ March 8 -10, 2021.
The online event will focus on current developments, novel approaches, and cutting-edge technologies in the field of medicinal chemistry and drug research with the following sessions: Degraders and Molecular Glues, Antiviral Agents, Young Investigators, Highlights in Medicinal Chemistry, First Disclosures & Case Studies, Covalent Binders and Fragments, Cryptic Binding Pockets and Novel Methods in Medicinal Chemistry and Case Studies.
The scientific program will include lectures and poster presentations. It is the goal of the organizers to make FIMC 2021 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 HELLENIC SOCIETY OF MEDICINAL CHEMISTRY (HSMC)
Due to the current condition related to COVID-19 pandemic and the measures announced by the Greek government, the Organizing Committee of the 18th Hellenic Symposium on Medicinal Chemistry (HSMC-18), in agreement with the Hellenic Society of Medicinal Chemistry (HSMC), have decided that the Symposium will be held online on February 25-27, 2021.
It will continue the tradition of biannual meetings, established for 35 years, in Greece as a forum for the discussion of recent advances in medicinal chemistry. The topics include drug design and lead identification and optimization, protein-protein interactions and protein degradation, ADME/Tox properties, advances in Synthetic Medicinal Chemistry, Natural Products, Pharmacology, as well as the impact of Artificial Intelligence in the integration of data-intensive practices to Drug Discovery.
Under this multidisciplinary research umbrella the major therapeutic areas, such as treatment of inflammatory diseases, infectious diseases, metabolic disorders, cardiovascular diseases, neurodegenerative diseases and oncology, will be discussed. Sections on Pharmaceutical Analysis will be integrated in the symposium program.
Discover the list of Confirmed Speakers.
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 announce several upcoming events.
Virtual - 7th RSC/SCI symposium on GPCRs in Medicinal Chemistry
24th and 25th February 2021 (two afternoon sessions)
Registration is open!
Synopsis: The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. This series of events on GPCR drug discovery combines dissemination of cutting-edge medicinal chemistry with innovative structural biology and novel drug design approaches
Virtual - Synthesis in Drug Discovery and Development
22nd and 23rd March 2021 (two afternoon sessions)
Registration is open!
Synopsis: This symposium aims to highlight and celebrate the crucial role that 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.
Virtual - Kinase 2021: 9th RSC / SCI Symposium on Kinase Inhibitor Design
14th and 15th April 2021 (two afternoon sessions)
Synopsis: With more than 25 FDA-approved small molecules, the field of kinase inhibition continues to attract significant investment from the drug discovery and development community. The event will encompass case studies of ongoing programmes as well as successful past programmes.
Virtual – 2nd Nucleosides and Nucleotides: Synthetic and Biological Chemistry
20th April 2021
The call for poster abstracts will close on 10th March
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.
21st RSC / SCI Medicinal Chemistry Symposium
12th to 15th September 2021, Churchill College, Cambridge, UK
The call for poster abstracts (first round) will close on 30th April
Synopsis: Europe’s premier biennial Medicinal Chemistry event, focusing on first disclosures and new strategies in medicinal chemistry
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EFMC ORGANISED EVENTS
March 30, 2021
7th EFMC-YSN MedChemBioOnline
August 29-September 2, 2021
EFMC-ISMC 2021 - XXVI EFMC International Symposium on Medicinal Chemistry
September 9-10, 2021
EFMC-YMCS 2021 - 8th EFMC Young Medicinal Chemists’ Symposium
EFMC SPONSORED EVENTS
February 24-25, 2021
7˝th RSC / SCI symposium on GPCRs in Medicinal Chemistry
February 25-27, 2021
18th Hellenic Symposium on Medicinal Chemistry (HSMC-18)
March 22-23, 2021
Synthesis in Drug Discovery and Development
April 14-15, 2021
Kinase 2021: 9th RSC / SCI Symposium on Kinase Inhibitor Design
April 20, 2021
2nd Nucleosides and Nucleotides: Synthetic and Biological Chemistry
April 29, 2021
The 3rd SCI-RSC Symposium on Transporters in Drug Discovery and Development
April 29, 2021
32nd Symposium on Medicinal Chemistry in Eastern England
June 29-30, 2021
The BMCS Mastering MedChem VI: 6th RSC-BMCS Symposium on Mastering Medicinal Chemistry
Scientist, Medicinal Chemistry / Organic Chemistry, University of Dundee, School of Life Sciences, Dundee, United Kingdom
Structural Biology & Biophysics Scientist, University of Dundee, School of Life Sciences, Dundee,
Senior Synthetic Chemists in Medicinal Chemistry, AstraZeneca, Gothenburg, Sweden
DISCNGINE, Ile de France, Paris, France
Drug Hunter @Aqemia, France (Paris) - deeptech startup leveraging AI and quantum-inspired physics for drug discovery, AQEMIA, Paris, France