Jake Bush
@jtbush.bsky.social
📤 178
📥 385
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Biotech and chemical biology | Industry-academia interface | Folk guitar and kite surfing
reposted by
Jake Bush
Ben Schumann
about 2 months 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...
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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 ...
https://chemrxiv.org/engage/chemrxiv/article-details/68dbc4cef416303770f685aa
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reposted by
Jake Bush
Jeannine Hess
2 months 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...
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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...
https://chemrxiv.org/engage/chemrxiv/article-details/68c80e219008f1a467a71ef2
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reposted by
Jake Bush
Stephan Hacker
12 months 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
add a skeleton here at some point
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reposted by
Jake Bush
Stephan Hacker
11 months 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...
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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...
https://www.nature.com/articles/s42004-025-01410-8
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reposted by
Jake Bush
Stephan Hacker
9 months ago
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
11 months 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...
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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...
https://www.nature.com/articles/s41467-024-55057-5
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reposted by
Jake Bush
Harry Wilders
12 months 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....
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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...
https://onlinelibrary.wiley.com/doi/full/10.1002/anie.202418314
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