#covalentinhibitors — Public Fediverse posts

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

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

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

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

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

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

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

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

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

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

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

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

Very excited to see this study by the group of David Konrad out in JACS Au.

Ortho-dichloroacrylophenone is a highly reactive, cysteine-directed electrophile for peptide and protein labeling as well as chemoproteomic profiling. Glad that our group could make a small contribution.

https://pubs.acs.org/doi/10.1021/jacsau.5c00692
#ChemBio #Chemistry #ChemPro #ProteoProbes #CovalentInhibitors

"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 presented his exciting research into efficiently finding new antibacterially active #CovalentInhibitors using a direct-to-biology approach and into finding their targets using residue-specific chemoproteomics with the isoDTB-ABPP technology at #NWOCHAINS.

#Bacteria #Antibiotics #Chemistry #ChemBio #ChemicalProteomics #D2B

"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 presented his exciting research into efficiently finding new antibacterially active #CovalentInhibitors using a direct-to-biology approach and into finding their targets using residue-specific chemoproteomics with the isoDTB-ABPP technology at #NWOCHAINS.

#Bacteria #Antibiotics #Chemistry #ChemBio #ChemicalProteomics #D2B

"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 presented his exciting research into efficiently finding new antibacterially active #CovalentInhibitors using a direct-to-biology approach and into finding their targets using residue-specific chemoproteomics with the isoDTB-ABPP technology at #NWOCHAINS.

#Bacteria #Antibiotics #Chemistry #ChemBio #ChemicalProteomics #D2B

"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 presented his exciting research into efficiently finding new antibacterially active #CovalentInhibitors using a direct-to-biology approach and into finding their targets using residue-specific chemoproteomics with the isoDTB-ABPP technology at #NWOCHAINS.

#Bacteria #Antibiotics #Chemistry #ChemBio #ChemicalProteomics #D2B

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.

https://onlinelibrary.wiley.com/doi/abs/10.1002/anie.202415873
https://onlinelibrary.wiley.com/doi/full/10.1002/anie.201915519
#Chemistry #ChemBio #Electrophiles

Exciting talk by Kevin Neumann 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.

https://onlinelibrary.wiley.com/doi/full/10.1002/psc.3548
https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/ceur.202500273
#Chemistry #ChemBio #DrugDiscovery

Great talk by Marta Artola at #NWOCHAINS. She talked about the use of modified sugars as inhibitors and molecular #chaperones in #DrugDiscovery. Exciting insights into the use of cyclic sulfamates and sulfamidates as reactive groups for #CovalentInhibitors.
https://pubs.acs.org/doi/10.1021/acscentsci.7b00214
#Chemistry #ChemBio

We explored the question, from which different areas of chemistry, including glycochemistry, peptide chemistry, materials chemistry and synthetic method development new electrophiles for covalent inhibitors can originate in order to keep expanding the druggable space. (2/2)

#Chemistry #ChemBio #ChemicalProteomics #ChemPro #ProteoProbes #DrugDiscovery #Glycotime #Peptides #Materials #Synthesis #Undruggable #CovalentInhibitors

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).