Filippov ADPr lab
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leidenadpr.bsky.social
Filippov ADPr lab
@leidenadpr.bsky.social
190 followers 110 following 3 posts
Bio-organic synthetic lab with focus on the synthesis of ADP-ribose related biopolymers.
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leidenadpr.bsky.social
We have a new article out in collaboration with the group of Michiel Vermeulen at @nkinl.bsky.social
Photoaffinity probes based on olaparib for Proteomics profiling. Simple but powerful 💪
Read here: chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/...
Olaparib is a widely used PARP inhibitor for the treatment of BRCA-mutated cancers. To comprehensively understand the drug's clinical impact, measuring its interactions with intended on- and off-targets is crucial. In this study, olaparib's on- and off-targets were profiled using photoaffinity labeling, a powerful, proteome-wide method for studying the direct interactions between a drug and its protein targets. A novel photoaffinity probe was designed and used in a proteomic screening to discover novel targets of olaparib in the human proteome. The probe, incorporating a pre-installed biotin group, bypasses the limitations of using a copper(I)-catalyzed click reaction in cell lysates for reporter group conjugation and revealed a broad range of olaparib interactors, including previously unreported proteins, in a quantitative mass spectrometry-based proteomic screening using HeLa whole cell lysate. This study contributes to our current understanding of the pharmacology of olaparib and provides a valuable tool for elucidating drug interactors within cell lysates, potentially guiding the development of more targeted therapeutics with fewer off-targets.
February 11, 2025 at 9:46 AM
leidenadpr.bsky.social
Illuminating talk by Zach Armstrong at #ReedijkSymposium in Leiden. Cryo-EM on human fucosidase doi.org/10.1016/j.st... and more fascinating glycoscience
https://doi.org/10.1016/j.str.2022.07.001 Cryo-EM structure of human fucosidase
November 22, 2024 at 12:52 PM