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Cambridge MedChem Consulting

The Chemical Probes Portal now includes several PROTACs

The Chemical Probes Portal now includes several PROTACs in the list of recommended chemical probes and even more are under review by the Scientific Advisory Board.

PROTACs are bifunctional molecules that bind to the target protein and an E3 ligase, the simultaneous PROTAC binding of two proteins brings the target protein in close enough proximity for polyubiquitination by the E2 enzyme associated to the E3 ligase, which flags the target protein for degradation through the proteasome.

ProtacCycle

They have also put together a really useful list of criteria to help define the best choice of Protac probe.

David Rees BMCS Hall of Fame and Medal 2020

A lot has happened over the last couple of months but I wanted to highlight the latest inductee to the 2020 RSC BMCS Hall of Fame. https://www.rscbmcs.org/awards/halloffame/

The BMCS is delighted to announce that David Rees PhD, FRSC, FMedSci, Chief Scientific Officer at Astex Pharmaceuticals, will be the 2020 inductee to its Hall of Fame, and the recipient of the associated medal. David is recognised internationally for his innovative use of chemistry in drug discovery. His research has forged bridges between academia and industry and he has held prominent positions in learned societies such as the Royal Society of Chemistry. He has led collaborations resulting in the discovery of three launched drugs, the anaesthetic agent Sugammadex which has been used in over 30 million patients in 60 countries, and the anti-cancer agents Ribociclib and Erdafitinib, both predicted to achieve blockbuster status. Much of Astex’s industry-leading productivity has been dependant on David’s chemical expertise. David is well known for his calm authority, scientific rigor and enthusiasm, and has over 140 publications and patents.

The current pandemic means that the formal presentation has been delayed but I'm sure many will want to join me in congratulating David on this well-deserved prestigious award.

The single most important factor determining the likelihood of success of a project is the quality of the starting lead

Have you identified a disease mechanism that should be explored in a drug discovery project? Then you may have also considered developing a screening assay to find new chemical starting points that could serve as candidates for drug development.

In the next European Lead Factory webinar, taking place on Thursday 28 January, Dr Saman Honarnejad, Director of Drug Discovery at Pivot Park Screening Centre, will give a presentation on guidelines for HTS assay development, with an emphasis on methods to design, evaluate and improve conditions for biochemical and cellular assay formats.

The event will take place via Microsoft Teams on 28 January 2021 from 11:00-12:00 (CET). Discussions with the audience will form a key part of the webinar and time will be made available for questions and answers.

Registration is free using this link https://events.europeanleadfactory.eu/elf/elf-webinar/.

The European Lead Factory welcomes drug targets in all therapeutic areas. Interested? Submit your screening proposal now. The next deadline to apply will be in January 2021. Full details are on the ELF website.

I've been involved in a number of screening campaigns and I can confirm this is a high quality screening deck.

Annual Site Review

As 2021 starts I'd like to wish you all a Happy New Year and hope that 2021 marks the start of the recovery.

The Drug Discovery Resources website continues to increase in popularity with 147,000 page views, an increase of 5% over the figure for 2019. The pages were visited by over 76,000 viewers and around 20% of the visitors come back on multiple occasions suggesting they find it useful. The visitors come from 177 different countries with the top countries being

  • United States (28%)
  • United Kingdom (14%)
  • India (10%)
  • Germany (3%)
  • Canada (3%)
  • Japan (2.5%)

Perhaps not unexpectedly one of the popular pages was COVID-19 and the Identification of "Drug Candidates" a checklist for those using virtual screening to identify potential hits for COVID-19 targets.

The other most viewed pages were

Looking at the operating systems 54% are Windows users, 20% Mac users, 12% Android, 10% iOS and 2% Linux.

Seasons Greetings

This has been a tough year for everyone but we still need to think about those less fortunate, as usual any monies saved on cards will be donated to the MS Society. Have a safe break and let's hope for better things in 2021.

seasonsgreetings

Still time to submit proposal to European Lead Factory

The closure date for the latest round of proposals for screening at the European Lead Factory is January 2021

The European Lead Factory welcomes drug targets in all therapeutic areas. Interested? Submit your screening proposal now. The next deadline to apply will be in January 2021.

Full details are on the ELF website.

I've been involved in a number of screening campaigns and I can confirm this is a high quality screening deck.

Open Source Antibiotics

Open Source Antibiotics is a consortium of researchers interested in open ways to discover and develop new, inexpensive medicines for bacterial infections.

There are already a couple of projects Mur Ligase and a series of Diarylimidazoles with unknown mechanism. Well worth a read.

All the structures of the molecules on the project are openly available in a spreadsheet https://docs.google.com/spreadsheets/d/168-a1_l51Nfbms67eG8zU8p-EhEtEO26FUzRInbu7fY/edit#gid=2078630269 feel free to have a browse.

New REVIVE Antimicrobial Encyclopaedia

Often when moving into a new therapeutic area it takes a while to pick up all the terms and acronyms, and antimicrobial research has some of it's own, not sure what a MIC is then head over to the REVIVE Antimicrobial Encyclopaedia and search.

The REVIVE Antimicrobial Encyclopaedia includes definitions of terms from the field of antimicrobials including ‘Active Pharmaceutical Ingredient’, ‘Bacterial efflux’ and ‘Minimum Inhibitory Concentration’. Each term has links for users to find more information on the subject and wherever available there are also links to REVIVE content such as webinar recordings and Antimicrobial Viewpoints on the subject. Some terms also include bespoke explanatory videos with clear diagrams featuring REVIVE experts.

REVIVE is a space for everybody with an interest in antimicrobial R&D. The Global Antibiotic Research and Development Partnership (GARDP) is a not-for-profit organization developing new treatments for drug-resistant infections that pose the greatest threat to health. We were created to ensure that everyone who needs antibiotics receives effective and affordable treatment, no matter where they live. We aim to develop five new treatments by 2025 to fight drug-resistant infections, focusing on sexually transmitted infections, sepsis in newborns and infections in hospitalized adults and children.

RSC Interest group membership

My RSC membership renewal form has just dropped though the letterbox.

IMG_3225

It is the ideal time to think about joining one of the RSC Interest groups.

Interest groups are scientific networks run by members for their community. Each group is themed around a specific area or application of the chemical sciences. They organise an annual series of events to cater for both their members and the wider scientific community. These events vary from: multi-day conferences and workshops to training events.

If you are interested in the computational side of drug discovery why not join the Chemical Information and Computer Applications Group CICAG code 86.

IMG_3226

Proposals for European Lead Factory

The closure date for the latest round of proposals for screening at the European Lead Factory is January 2021

The European Lead Factory welcomes drug targets in all therapeutic areas. Interested? Submit your screening proposal now. The next deadline to apply will be in January 2021.

Also note

Following the UK’s exit from the European Union on 31 January, we are pleased to confirm that the European Lead Factory still welcomes screening proposals from UK researchers.

You can read more about the screening facility here https://www.europeanleadfactory.eu/node/353.

The details of how to submit are here https://www.europeanleadfactory.eu/how-submit/drug-target-assays/how-it-works.

I've written about the ELF here.

screening