Proteomics

Dataset Information

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Comprehensive selectivity profile of PARP inhibitors using kinobeads


ABSTRACT: Explore kinase off-targets of several PARP inhibitors using kinobeads

INSTRUMENT(S): Orbitrap Fusion Lumos, Q Exactive HF-X, Orbitrap Exploris 480, Q Exactive HF

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Placenta, Hepg2 Cell, Hek-293 Cell, K-562 Cell, Cell Line Cell

SUBMITTER: Maria Faelth Savitski  

LAB HEAD: Marcus Bantscheff

PROVIDER: PXD045297 | Pride | 2025-05-06

REPOSITORIES: Pride

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Publications


An in-depth multiomic molecular characterization of PARP inhibitors revealed a distinct poly-pharmacology of niraparib (Zejula) mediated by its interaction with lanosterol synthase (LSS), which is not observed with other PARP inhibitors. Niraparib, in a similar way to the LSS inhibitor Ro-48-8071, induced activation of the 24,25-epoxysterol shunt pathway, which is a regulatory signaling branch of the cholesterol biosynthesis pathway. Interestingly, the combination of an LSS inhibitor with a PARP  ...[more]

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