Leiden Early Drug Discovery & Development (LED3)

#DrugDiscovery #Automation #VirtualScreening #MedicinalChemistry #HitDiscovery #ChemSky #ChemBio

New preprint from our LED3 hub on ChemRxiv!

The labs of @sebastianpomplun.bsky.social , @gjpvwesten.bsky.social and Laura Heitman with first author @seanmckenna.bsky.social present COMBINAUT: an automated parallel synthesis platform for rapid access to 22.9M-compounds.

chemrxiv.org/doi/full/10....

How do mycobacteria assemble a highly impermeable outer cell envelope?

The group of Sebastian Geibel has elucidated the structure of two long-chain acyl-CoA carboxylases that are key to mycolic acid and complex lipid biosynthesis.
www.biorxiv.org/content/10.6...
#DrugDiscovery #cryoEM #Tuberculosis

Very much looking forward to the @led3hub.bsky.social Lecture by Christina Woo (@thewoolab.bsky.social)! I am sure it will be a great one.

If you are interested in #ChemicalProteomics and/or targeted protein degradation #TPD, you will not want to miss it.

#ChemSky #ChemBio #DrugDiscovery #degrader

We are looking forward to the LED3 Lecture of Christina Woo (@thewoolab.bsky.social) on February 26th. She will talk about "Rewriting Protein Modifications".

If you are interested, make sure to come by!

www.universiteitleiden.nl/en/science/l...

#ChemBio #ChemSky #ChemicalProteomics #TPD

Great @led3hub.bsky.social Lecture by @anneosbourn.bsky.social. She talked about the amazing diversity of plant natural products, the gene clusters for their synthesis and their recombinant production for applications in #food and #health.

www.nature.com/articles/s41...
#Plants #NaturalProducts

We are very happy that @anneosbourn.bsky.social from the @johninnescentre.bsky.social visited us today for a LED3 Lecture. She talked about "Harnessing plant metabolic diversity for food and health applications".

#Plants #NaturalProducts #GeneClusters #DrugDiscovery #ChemBio #ChemSky #Food #Health

@anneosbourn.bsky.social (from @johninnescentre.bsky.social) is today’s @led3hub.bsky.social seminar speaker on Harnessing plant metabolic diversity for food and health applications
#NaturalProducts

Are you interested in cutting-edge research in Early Drug Discovery and Development?

We have a great program for our LED3 Lectures for the remaining academic year. Check out the program and mark your calendars!

www.universiteitleiden.nl/en/science/l...
#DrugDiscovery #ChemSky #ChemBio

We are looking forward to the LED3 Lecture of Anne Osbourn on January 29th She will talk about "Harnessing plant metabolic diversity for food and health applications".

If you are interested, make sure to come by!

www.universiteitleiden.nl/en/science/l...

#ChemBio #ChemSky #Plants #Metabolites

Our dean Jasper Knoester addresses our faculty @leidenscience.bsky.social in his New Year's speech. Interesting insights into the future strategic goals of our faculty and great to hear him highlight the priority themes including the @led3hub.bsky.social with new theme leader @mvdstelt.bsky.social.

CellEKT: A Robust Chemical Proteomics Workflow to Profile Cellular Target Engagement of Kinase Inhibitors The human genome encodes 518 protein kinases that are pivotal for drug discovery in various therapeutic areas, such as cancer and autoimmune disorders…

The group of @mvdstelt.bsky.social of our @led3hub.bsky.social published CellEKT for profiling of the cellular targets of kinase inhibitors, which is further developed in the company Omivera (omivera.com). (3/12)
www.sciencedirect.com/science/arti...

Barcode-free hit discovery from massive libraries enabled by automated small molecule structure annotation - Nature Communications Affinity-selection platforms are powerful tools in early drug discovery, but current technologies such as DNA-encoded libraries (DELs) are limited by synthesis complexity and incompatibility with nucl...

The group of @sebastianpomplun.bsky.social of our @led3hub.bsky.social developed self-encoded libraries (SELs) that allow affinity-selection MS-based screening of protein binders from large libraries in a single experiment without the need for a barcode. (6/12)
www.nature.com/articles/s41...

Experimental glycopeptide antibiotic EVG7 prevents recurrent Clostridioides difficile infection by sparing members of the Lachnospiraceae family - Nature Communications Treatment of Clostridioides difficile infections (CDI) with vancomycin is associated with high relapse rates. In this study, the experimental glycopeptide antibiotic EVG7 was found to effectively trea...

The groups of Nathaniel Martin of our @led3hub.bsky.social and the @smitslab.bsky.social published the powerful semisynthetic guanidino lipoglycopeptide EVG7 to treat Clostridioides difficile infections. (11/12)
www.nature.com/articles/s41...

News Details

Exciting news that @fda.gov has approved the first oral GLP-1 agonist for clinical use for @novonordisk.bsky.social.
www.novonordisk.com/content/nnco...

It was amazing to hear about the science behind these medications directly from Lotte Bjerre Knudsen in her @led3hub.bsky.social Lecture.

Excited to be part of the @led3hub.bsky.social of @leidenscience.bsky.social and of the organizing committee of the #LED3Lectures and #LED3Symposium. I am convinced that these are amazing initiatives that strengthen our collaborative spirit. New exciting activities are coming in 2026 and 2027.

We heard insightful LED3 Lectures by Paola Picotti, Andrea Rentmeister, Jeff Kelly, @jpoverington.bsky.social, Kim Lewis, Ed Tate, Jay Keasling, Willem Velema, Nicolas Winssinger and Lotte Bjerre Knudsen.(3/3)
#DrugDiscovery #Chemistry #Biology #PharmaceuticalSciences #ChemBio @unileiden.bsky.social

We are happy that we could continue our activities to bring our researchers closer together including the LED3 PhD/Postdoc Symposium #LED3Symposium and our flagship #LED3Lectures, in which we heard talks by a diverse selection of world-leading speakers in the field of #DrugDiscovery. (2/3)

Another exciting year for our LED3 hub comes to a close. We were able to celebrate many successes including grants, publications, awards and started companies. In 2025, the activities of LED3 were also formalized in the theme "Drug Discovery and Development" of @leidenscience.bsky.social. (1/3)

Interesting article by the American Peptide Society about the recent publication by the group of @sebastianpomplun.bsky.social of our @led3hub.bsky.social on using BindCraft to predict #peptide binders to high value protein targets.
americanpeptidesociety.org/aps-news/bin...

Eleven Open Competition Domain Science XS grants for Leiden researchers Eleven researchers from Leiden University have been awarded an Open Competition Domain Science ENW XS grant by the Dutch Research Council for their research projects. They are researching how to make ...

Congratulations to the LED3 members that received NWO XS grants:
@mads-chem.bsky.social - Inhibiting the growth of brain tumours
Margo Dona - Rapid personalised treatment for anaplastic thyroid cancer
Sandra Irmisch - Producing rare substances for medicines

www.universiteitleiden.nl/en/news/2025...

ReCHEMbinant stapling enhances intracellular delivery and bioactivity of engineered protein inhibitors Protein therapeutics have transformed drug discovery by enabling modulation of challenging targets inaccessible to small molecules. However, most prot…

New Publication from our LED3 hub!

The group of @sebastianpomplun.bsky.social published "ReCHEMbinant stapling enhances intracellular delivery and bioactivity of engineered protein inhibitors" in the journal Chem.

www.sciencedirect.com/science/arti...

#ChemSky #ChemBio #DrugDiscovery #MYC #Cancer

ReCHEMbinant stapling enhances intracellular delivery and bioactivity of engineered protein inhibitors Protein therapeutics have transformed drug discovery by enabling modulation of challenging targets inaccessible to small molecules. However, most prot…

Interesting paper by the group of @sebastianpomplun.bsky.social of our @led3hub.bsky.social. Chemical stapling of recombinant proteins on the example of the Myc inhibitor Omomyc leads to enhanced serum stability, cellular uptake and intracellular activity.
www.sciencedirect.com/science/arti...

Jessica Hoang (supervised by @kimmb1.bsky.social and @mverdoes.bsky.social of the Leiden University Medical Center)

Lars van Abswoude (supervised by @mvdstelt.bsky.social, Monique Mulder and @stephanhacker2.bsky.social)
(4/4)

Afterwards, the following LED3 researchers presented their exciting projects:

Nick Puijmbroeck (supervised by @mvdstelt.bsky.social and Sander van Kasteren)

Tijn Vleeshouwer (supervised by Sander van Kasteren)

... (3/4)

The projects of work package 4, which is led by Sander van Kasteren, were presented in a session chaired by @mvdstelt.bsky.social.

First, Marc Baggelaar from @utrechtuniversity.bsky.social gave an overview of the overall work package. (2/4)

It is great to see, how highly represented LED3 researchers are at the #iCNS meeting of the Institute for Chemical Neuroscience. Exciting that our researchers are making so many important contributions to this innovative research direction. (1/4)
#ChemSky #ChemBio #Neuroscience #DrugDiscovery

Cheap Computation of Small Peptide Binders

Interested in computationally predicting peptide binders to a protein-of interest?

Check out this @science.org blog post by @dereklowe.bsky.social on the work by @sebastianpomplun.bsky.social of our @led3hub.bsky.social on predicting peptide binders using BindCraft.

www.science.org/content/blog...

Cheap Computation of Small Peptide Binders

Exciting to see the study on the prediction of high-affinity #peptide binders to proteins-of-interests by the group of @sebastianpomplun.bsky.social of our LED3hub highlighted by @dereklowe.bsky.social in his @science.org blog.

www.science.org/content/blog...

#ChemSky #ChemBio #DrugDiscovery