Tessera
Folgen

Jake Bush

@jtbush.bsky.social

Biotech and chemical biology | Industry-academia interface | Folk guitar and kite surfing

0 Posts191 Follower385 Folgt
Ben Schumann@drglycoben.bsky.social · 10mo ago

Check out our new preprint "Convergent Lead Discovery Strategies Yield Covalent and Non-covalent Inhibitors of Human UDP-Galactose-4-Epimerase" on Chemrxiv led by Will Browne in close collab with GSK @jtbush.bsky.social chemrxiv.org/engage/chemr...

Convergent Lead Discovery Strategies Yield Covalent and Non-covalent Inhibitors of Human UDP-Galactose-4-Epimerase

O-GalNAc (N-acetylgalactosaminyl) glycosylation is an abundant posttranslational modification in mammalian cells. Dysregulation of O-GalNAc glycosylation is implicated in cancer metastasis and immune ...

chemrxiv.org

Jeannine Hess@jeanninehess.bsky.social · 11mo ago

🧪 Excited to share our new work on reactive metallo-scaffolds (r-mS)! We combine metal complexes with chemoproteomics to discover new liganding sites across the proteome! Shout out to a great collaboration with GSK! Fantastic team effort 🫶🏻 chemrxiv.org/engage/chemr...

Proteome-Wide Target Identification Using Reactive Metallo-Scaffolds (r-mS): A Platform for Metallodrug Discovery

Metal complexes offer unique opportunities as scaffolds in chemical biology and drug discovery, with tuneable geometry, modular coordination environments, and structural features not readily accessibl...

chemrxiv.org

Stephan Hacker@stephanhacker2.bsky.social · 2y ago

Great paper by the group of @jtbush.bsky.social with first author @harrywilders.bsky.social in @angewandtechemie.bsky.social. They established a direct-to-biology approach to quickly screen covalent protein ligands and advance the covalent hits into a non-covalent inhibitor series. #ChemSky #ChemBio

Harry Wilders@harrywilders.bsky.social · 2y ago

I am happy to share that our recent work has been published in Angewandte Chemie. We demonstrate how ‘direct-to-biology’ screening can accelerate optimisation campaigns, yielding potent covalent and non-covalent inhibitors from reactive fragment hits. onlinelibrary.wiley.com/doi/full/10....

Stephan Hacker@stephanhacker2.bsky.social · 2y ago

Interesting paper by the groups of @katrinrittinger.bsky.social and @jtbush.bsky.social in @commschem.bsky.social. DIA-based chemical proteomics in combination with direct-to-biology compound optimization identifies new, enantioselective inhibitors for the DUB OTUD7B. www.nature.com/articles/s42...

Enantioselective OTUD7B fragment discovery through chemoproteomics screening and high-throughput optimisation - Communications Chemistry

The ovarian tumour protease (OTU) family of deubiquitinating enzymes (DUBs) are biochemically well-characterised and of therapeutic interest, however, only a few tool compounds exist to study their ce...

nature.com

George Biggs@george-biggs.bsky.social · 2y ago

Excited to share a key part of my postdoctoral work from @crick.ac.uk and GSK, published in Nature Communications. A collaborative project to develop a high-throughput chemoproteomics platform for profiling cysteine-reactive fragments in native biological systems. www.nature.com/articles/s41...

Robust proteome profiling of cysteine-reactive fragments using label-free chemoproteomics - Nature Communications

This paper presents a label-free chemoproteomics platform using data-independent acquisition to profile covalent fragment binding across the human proteome. The platform offers high reproducibility an...

nature.com

Harry Wilders@harrywilders.bsky.social · 2y ago

I am happy to share that our recent work has been published in Angewandte Chemie. We demonstrate how ‘direct-to-biology’ screening can accelerate optimisation campaigns, yielding potent covalent and non-covalent inhibitors from reactive fragment hits. onlinelibrary.wiley.com/doi/full/10....

Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery through Modular ‘Direct‐to‐Biology’ Screening

Direct-to-biology workflows promise to accelerate hit optimisation for drug discovery. Here, we describe a direct-to-biology method for the efficient synthesis and screening of cysteine-reactive frag...

onlinelibrary.wiley.com