Design, Synthesis and Characterization of Covalent KDM5 Inhibitors Histone lysine demethylases (KDMs) are involved in the dynamic regulation of gene expression and play a critical role in several biological processes. Achieving selectivity over the different KDMs ha...

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

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

Investigating the bioorthogonality of isocyanides Isocyanides have been applied in bioorthogonal reactions as triggers for uncaging reactions. However, emerging evidence suggests that they may label proteins covalently. We synthesised a fluorophore-conjugated isocyanide and analysed its protein reactivity. Our results suggest that isocyanides cannot be considered

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

In this @chemcomm.rsc.org paper, the groups of @meganwright.bsky.social and Stuart Warriner investigate the metal-independent labeling of proteins using isocyanides.
pubs.rsc.org/en/content/artic...
#ChemBio #ChemSky #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.
pubs.acs.org/doi/10....
#ChemSky #ChemBio #DrugDiscovery #Kinases

Mapping cellular targets of covalent cancer drugs in the entire mammalian body vCATCH is a volumetric tissue labeling technique enabling cellular-resolution mapping of covalent drug targets throughout the entire mammalian body.

Amazing paper by the groups of Li Ye and Ben Cravatt of @scripps.edu in @cp-cell.bsky.social. They developed the vCATCH method to map in vivo, to which tissues and cell types #CovalentInhibitors bind with spatial resolution in whole intact mouse bodies. www.cell.com/cell/fulltex...
#ChemSky #ChemBio

#ChemBio #ChemSky #ChemPro #ProteoProbes #CovalentInhibitors

Precipitation-first synthesis and deep profiling of a 1200-member acrylamide library for covalent drug discovery Screening libraries of low molecular weight (LMW) compounds are foundational in early-stage drug discovery. However, the parallel synthesis of milligram-scale large libraries – especially for covalent inhibitors – remains constrained by resource-intensive purification protocols, high solvent consumption, and

Interesting paper by the group of Alexander Dömling in Green Chemistry. They used an Ugi four-component reaction followed by product precipitation for the efficient synthesis and purification of a >1200-member acrylamide library.

pubs.rsc.org/en/cont...
#CovalentInhibitors #ChemSky #ChemBio

"Rapid Antibiotic Discovery using a Direct-to-Biology Approach"

Storm van der Voort from the group of Hermen Overkleeft and our group at the @led3hub.bsky.social presented his research into efficiently finding new antibacterially active #CovalentInhibitors and their targets.

#ChemSky #ChemBio

Insightful talk by Dieuwertje Streefkerk at #NWOCHAINS. She talked about their synthetic work on stereochemically defined sulfur(VI) electrophiles and their use as #CovalentInhibitors on the example of chymotrypsin inhibition.

onlinelibrary.wiley.com/doi/full/10....
#ChemSky #ChemBio #Electrophiles

Exciting talk by Kevin Neumann (@neumannlab.bsky.social) at #NWOCHAINS. He talked about the tetrazine- and triazine-thiol exchange reactions for #bioconjugation and #peptide cyclization. He also discussed their potential application for #CovalentInhibitors.
onlinelibrary.wiley.com/doi/full/10....

Great talk by Marta Artola at #NWOCHAINS. She talked about the use of modified sugars as inhibitors and molecular #chaperones in #DrugDiscovery. Great insights into the use of cyclic sulfamates and sulfamidates as reactive groups for #CovalentInhibitors
pubs.acs.org/doi/10.1021/...
#ChemSky #ChemBio

#Chemistry #ChemBio #ChemicalProteomics #ChemPro #ProteoProbes #DrugDiscovery #Glycotime #Peptides #Materials #Synthesis #Undruggable #CovalentInhibitors
(3/3)

Now I am looking forward to two days of exciting science, including our focus session on #CovalentInhibitors as well as many exciting presentations by #PhD and #postdoc researchers. (8/8)

This great @science.org paper by Vividion and @crick.ac.uk headed by Matt Patricelli and @juliandownward.bsky.social on covalent inhibitors of the PI3Kα-RAS interaction. Exciting project on #CovalentInhibitors and #ChemicalProteomics.
www.science.org/doi/10.1126/...
#ChemSky #ChemBio #DrugDiscovery

Are you interested in novel covalent inhibitors and diverse strategies, through which you can find new chemistries for them?
Then check out our Focus Session on "Covalent Inhibitors and where to find them" at the CHAINS conference by NWO. (1/4)
#Chemistry #CovalentInhibitors #ChemBio #DrugDiscovery

The Jones Lab is hiring postdoctorate fellow positions in chemical biology - a great opportunity to be at the forefront of next-generation covalent chemical biology research: | Lyn Jones The Jones Lab is hiring postdoctorate fellow positions in chemical biology - a great opportunity to be at the forefront of next-generation covalent chemical biology research: https://lnkd.in/e3Y-UCDa ...

Great opportunity to do a #postdoc in the field of #CovalentInhibitors with a great mentor in the group of @lynjoneschembio.bsky.social at @danafarber.bsky.social!

www.linkedin.com/posts/lynhow...

#ChemBio #Chemistry #ChemSky #DrugDiscovery

🔬 Exciting news — I’ll be starting the Craven Lab at Yale this fall! | Gregory Craven 🔬 Exciting news — I’ll be starting the Craven Lab at Yale this fall! After a fantastic postdoc at UCSF, I’m thrilled to be launching my lab in Yale's Institute for Biomolecular Design and Discover...

Great opportunity to work as a #postdoc with Gregory Craven at @yale.edu in an exciting field!
#ChemBio #Chemistry #CovalentInhibitors

www.linkedin.com/posts/gregor...

The final #FlashTalk session gave another exciting overview of different early #DrugDiscovery topics including #CovalentInhibitors for glycosidases (Rob Lammers), host-directed therapies for bacterial infections (Bart van Lieshout) and covalently drugging transcription factors (Shaima Abdalla).

Schematic mechanism of tri-complex formation and Elironrasib (RMC-6291). Generated from PDB: 9BFX

In our latest Medicinal Chemistry in Review blog, we highlight the discovery of Elironrasib (RMC-6291), published by Revolution Medicines .
domainex.co.uk/news/medicin...
#Domainex #DrugDiscovery #CovalentInhibitors

Covalent fragment approaches targeting non-cysteine residues Covalent fragment approaches combine advantages of covalent binders and fragment-based drug discovery (FBDD) for target identification and validation.…

He started by giving a very clear overview of the concept of #CovalentInhibitors and the important advantages that they can have in #DrugDiscovery. He especially highlighted, how powerful covalent fragments can be in this context. (2/7) www.sciencedirect.com/science/arti...

Congrats to lab alum SW @sijiewang.bsky.social on his recent paper! Boilermakers blazing trails with their big jumps! #phagedisplay #covalentinhibitors #fluorosulfates
pubs.acs.org/doi/10.1021/...

Very excited to see the scientific community forming over here and to have reached 500 followers. I will try to ramp up my activities again posting on literature on #Science, #Chemistry, #Chemsky, #ChemicalBiology, #Antibiotics, #CovalentInhibitors, #ChemicalProteomics and #ABPP.

Great to see so many new people from the scientific community joining here. Welcome! I would be very happy to connect with everyone on topics such as #Science, #Chemistry, #Chemsky, #ChemicalBiology, #Antibiotics, #CovalentInhibitors, #ChemicalProteomics, #ABPP and general topics of #academia.