Proteomics

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Total and phosphoproteome analysis of effects of topoisomerase 1 and ATR inhibitors in small cell lung cancer nuclei


ABSTRACT: Total and phosphoproteome analysis of effects of topoisomerase 1 (SN-38) and ATR (M1774) inhibitors in small cell lung cancer. Experiments performed in nuclear extract. See MetaData for more information.

INSTRUMENT(S): Orbitrap Exploris 480

ORGANISM(S): Homo Sapiens (ncbitaxon:9606)

SUBMITTER: Lisa Jenkins  

PROVIDER: MSV000091336 | MassIVE | Tue Feb 21 13:44:00 GMT 2023

SECONDARY ACCESSION(S): PXD040313

REPOSITORIES: MassIVE

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Publications

The Novel ATR Inhibitor M1774 Induces Replication Protein Overexpression and Broad Synergy with DNA-targeted Anticancer Drugs.

Jo Ukhyun U   Arakawa Yasuhiro Y   Zimmermann Astrid A   Taniyama Daiki D   Mizunuma Makito M   Jenkins Lisa M LM   Maity Tapan T   Kumar Suresh S   Zenke Frank T FT   Takebe Naoko N   Pommier Yves Y  

Molecular cancer therapeutics 20240701 7


Ataxia telangiectasia and Rad3-related (ATR) checkpoint kinase inhibitors are in clinical trials. Here we explored the molecular pharmacology and therapeutic combination strategies of the oral ATR inhibitor M1774 (Tuvusertib) with DNA-damaging agents (DDA). As single agent, M1774 suppressed cancer cell viability at nanomolar concentrations, showing greater activity than ceralasertib and berzosertib, but less potency than gartisertib and elimusertib in the small cell lung cancer H146, H82, and DM  ...[more]

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