GTPases have long been considered key examples of undruggable proteins. While this has been overcome for K-Ras using #CovalentInhibitors, for many other family member #DrugDevelopment has not been shown.

Congratulations to Johannes Morstein on winning one of the @GDCh_BioChem Young Scientist Awards for his work addressing this challenge by identifying druggable, allosteric pockets in several GTPases.

https://www.cell.com/cell/fulltext/S0092-8674(24)00908-5
#Biochemistry #ChemBio #GTP #GTPases #Chemistry
CC: @gdch

Great talk by Akane Kawamura at #Biochemistry2026. She talked about her group's exciting work on the #Biochemistry of JmjC demethylases with important implications for #epigenetics. Exciting insights into arginine demethylation.

https://febs.onlinelibrary.wiley.com/doi/10.1002/1873-3468.14586

She also talked about the potential of these enzymes in #DrugDiscovery including the discovery of #CovalentInhibitors for KDM5.

https://onlinelibrary.wiley.com/doi/full/10.1002/anie.201810179
#Chemistry #ChemBio #Biochemistry
CC: @gdch, @GDCh_BioChem

She also talked about the potential of these enzymes in #DrugDiscovery including the discovery of #CovalentInhibitors for KDM5. (2/2) onlinelibrary.wiley.com/doi/full/10.... #ChemSky #ChemBio #Biochemistry

Design, Synthesis and Characte...

I was very happy to be able to talk about some of our work at #Biochemistry2026. I presented results of Patrick Zanon, Marnix Roseboom, Julia Pols and Storm van der Voort on new covalently reactive groups, chemical proteomics methods and screening technologies.

https://www.nature.com/articles/s41557-025-01902-z
#Chemistry #ChemBio #Biochemistry #Chemoproteomics #CovalentInhibitors

Overall, I hope that 2026 will yield at least the same degree of scientific progress as 2025. (12/12)

#Chemistry #ChemBio #Science #Antibiotics #Synthesis #TPD #Degrader #Proteomics #Kinases #RNA #Screening #CovalentInhibitors #DirectToBiology

A covalent KEAP1 activator in the clinics: A team at Vividion led by Matt Patricelli developed a covalent molecular glue for KEAP1, which leads to suppression of NRF2-dependent cancer growth. Excited to see, how the three clinical programs that Vividion built based on #CovalentInhibitors discovered by #ChemicalProteomics will progress. (7/12)
https://aacrjournals.org/cancerdiscovery/article/doi/10.1158/2159-8290.CD-25-1187/771133/A-covalent-allosteric-molecular-glue-suppresses?searchresult=1
Overall, I hope that 2026 will yield at least the same degree of scientific progress as 2025. (12/12) #Chemistry #ChemBio #Science #Antibiotics #Synthesis #TPD #Degrader #Proteomics #Kinases #RNA #Screening #CovalentInhibitors #DirectToBiology
Let's start the year off right with an exciting paper post! In this @[email protected] paper, the groups of @[email protected] and Stuart Warriner investigate the metal-independent labeling of proteins using isocyanides. pubs.rsc.org/en/content/artic... #ChemBio #ChemSky #CovalentInhibitors

Investigating the bioorthogona...

Let's start the year off right with an exciting paper post!

In this Chemical Communications paper, the groups of Megan Wright and Stuart Warriner investigate the metal-independent labeling of proteins using isocyanides.

https://pubs.rsc.org/en/content/articlelanding/2026/cc/d5cc04136h
#ChemBio #Chemistry #CovalentInhibitors

Interesting J. Med. Chem. paper by the group of Michael Waring. They developed alkynylpyridopyrimidinones that covalently target Cys775 of EGFR to allow development of #CovalentInhibitors even against the C797S resistance mutant.
https://pubs.acs.org/doi/10.1021/acs.jmedchem.5c02924
#Chemistry #ChemBio #DrugDiscovery #Kinases