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Jake Bush

@jtbush.bsky.social
191 followers 385 following 0 posts

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

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Reposted by Jake Bush
Ben Schumann @drglycoben.bsky.social · 07/10/2025
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...
chemrxiv.org
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 ...
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Reposted by Jake Bush
Jeannine Hess @jeanninehess.bsky.social · 23/09/2025
🧪 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...
chemrxiv.org
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...
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Reposted by Jake Bush
Stephan Hacker @stephanhacker2.bsky.social · 11/12/2024
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
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Reposted by Jake Bush
Stephan Hacker @stephanhacker2.bsky.social · 17/01/2025
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...
nature.com
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...
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Reposted by Jake Bush
Stephan Hacker @stephanhacker2.bsky.social · 17/03/2025
Great @chemrxiv.bsky.social preprint by a team of GSK around @jtbush.bsky.social. They showcase the power of single- and multi-step direct-to-biology approaches by developing a potent, cell-active actylamide inhibitor for WRN helicase. chemrxiv.org/engage/...
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Reposted by Jake Bush
George Biggs @george-biggs.bsky.social · 10/01/2025
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...
nature.com
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...
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Reposted by Jake Bush
Harry Wilders @harrywilders.bsky.social · 11/12/2024
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....
onlinelibrary.wiley.com
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...
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