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Structure-based design of new potent and highly selective PARP-1 inhibitor for treating colorectal cancer

12 Aug 2025

Abstract excerpt

Poly (ADP-ribose) polymerase 1 (PARP-1) exhibits high expression levels in colorectal cancer (CRC) patients and participates in multiple DNA damage repair pathways, thereby emerging as an attractive target. Herein, we identified a series of PARP-1 inhibitors (termed as compounds 1-6) by pharmacophore modelling, virtual screening and biological evaluation. Enzyme inhibition assays demonstrated that compound-5...

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PMID: 40793788
DOI: 10.1080/14756366.2025.2542358

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