@stephanhacker2.bsky.socialIs arginine a viable target for #CovalentInhibitor development?
Lately, this topic has seen a lot of movement with the development of new warheads. The groups of Balyn Zaro and Ian Seiple now add ninhydrin as a promising warhead to the toolbox to address this question.
@stephanhacker2.bsky.socialWhat to do, if cancer cells become resistant to a #CovalentInhibitor by mutating the reactive cysteine?
At #ICBS2026, Celine Wang from the group of Ziyang Zhang talked about her research into addressing BTK C481S with a β-lactone that targets the catalytic lysine.
@stephanhacker2.bsky.socialInteresting talk by Jinsu Bae from the group of Michelle Arkin at #ICBS2026.
He talked about the potential of oncogenic Gαq as a tatget in treating uveal melanoma and their work towards addressing it with a #CovalentInhibitor.
@stephanhacker2.bsky.socialNew paper by the group of Lyn Jones. They study the amino acid reactivity and plasma stability of sulfonyl imidazole (SuDEx) and triazole (SuTEx) electrophiles showing enhanced stability and tyrosine reactivity for SuDEx.
@stephanhacker2.bsky.socialNew paper by the group of Lyn Jones. They study the amino acid reactivity and plasma stability of sulfonyl imidazole (SuDEx) and triazole (SuTEx) electrophiles showing enhanced stability and tyrosine reactivity for SuDEx.
@stephanhacker2.bsky.socialI had a great time and hope to be back for the next event in 2028.
#CovalentInhibitor #DrugDiscovery #ChemicalProteomics #ChemBio #Chemistry #Science
(7/7)
@stephanhacker2.bsky.socialA true firework of covalent drug discovery to close out the Covalent Modulation in Drug Discovery Conference #CovModDrugDiscov!
Ed Tate presented a variety of exciting projects of his group.
#CovalentInhibitor #DrugDiscovery #ChemSky #ChemBio #Science
@stephanhacker2.bsky.socialInteresting talk by Michael Bodnarchuk from @astra-zeneca.bsky.social at #CovModDrugDiscov.
He talked about the use of computational tools to discover covalent, brain-penetrant KRAS G12C inhibitors.
#CovalentInhibitor #DrugDiscovery #ChemSky #ChemBio #Science
@stephanhacker2.bsky.socialInteresting talk by Federica Raguseo at #CovModDrugDiscov.
She talked about a phenotype-first approach to covalent drug discovery on the example of TYMS.
www.biorxiv.org/content/10.6...
#CovalentInhibitor #DrugDiscovery #ChemSky #ChemBio #Science
@britpharmsoc.bsky.social
@stephanhacker2.bsky.socialInteresting talk by Darrin McKenzie at #CovModDrugDiscov.
He talked about, how they set up an automated platform to study protein expression levels and cysteine engagement in living cells.
#CovalentInhibitor #DrugDiscovery #ChemBio #ChemSky #ChemicalProteomics #Science
@stephanhacker2.bsky.socialAlways great to see the amazing work by Patrick Zanon in our group highlighted in the talk of others.
www.nature.com/articles/s41...
#CovalentInhibitor #DrugDiscovery #ChemSky #ChemBio #Science #ChemPro #ProteoProbes
@britpharmsoc.bsky.social
@stephanhacker2.bsky.socialThe 2nd day of #CovModDrugDiscov gets on the way with an inspiring talk by Steven Gygi.
He talked about the power of TMT technologies for multiplexing to arrive at high-throughput residue-specific chemoproteomics.
#CovalentInhibitor #DrugDiscovery #ChemSky #ChemBio #ChemicalProteomics #Science
@stephanhacker2.bsky.socialInsightful talk by Matthias Gehringer at #CovModDrugDiscov.
He gave great insights into his group's work on making new kinases amenable to covalent drug discovery at cysteine and beyond.
onlinelibrary.wiley.com/doi/10.1002/...
#CovalentInhibitor #DrugDiscovery #ChemSky #ChemBio #Science #Kinase
@stephanhacker2.bsky.social#CovModDrugDiscov continues with an interesting talk by Mandy Ferdinand from Cancer Research Horizons.
She talked about methods to characterize covalent hits with a special focus on binding kinetics.
#CovalentInhibitor #DrugDiscovery #ChemSky #ChemBio #Science
@stephanhacker2.bsky.socialThe Covalent Modulation in Drug Discovery Conference #CovModDrugDiscov is off to a great start with an insightful talk by Matt Bilyard from Roche.
He talked about how they select targets for covalent drug discovery and then find and develop covalent binders.
@stephanhacker2.bsky.socialAnd we are on the way with the Covalent Modulation in Drug Disvovery Conference by @britpharmsoc.bsky.social.
Looking forward to two days filled with cutting-edge covalent drug discovery.
@stephanhacker2.bsky.socialI am looking forward to an exciting meeting.
#CovalentInhibitor #DrugDiscovery #ChemSky #Chemistry #ChemBio #ChemicalProteomics #ChemPro #ProteoProbes
(3/3)
@stephanhacker2.bsky.socialInteresting paper by the groups of Bradley Pentelute and Aaron Nile in Chemical Science.
They developed an on-resin, intermolecular Heck reaction to diversify acrylamides for covalent hit discovery using coPELs.
