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Discovery and characterization of a novel inhibitor of CDC25B, LGH00045

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Aim: Cell division cycle 25 (CDC25) phosphatases have recently been considered as potential targets for the development of new cancer therapeutic agents. We aimed to discover novel CDC25B inhibitors in the present study. Methods: A molecular level high-throughput screening (HTS) assay was set up to screen a set of 48000 pure compounds. Results: HTS, whose average Z′ factor is 0.55, was finished and LGH00045, a mixed-type CDC25B inhibitor with a novel structure and relative selectivity for protein tyrosine phosphatases, was identified. Furthermore, LGH00045 impaired the proliferation of tumor cells and increased cyclin-dependent kinase 1 inhibitory tyrosine phosphorylation. In synchronized HeLa cells, LGH00045 delayed cell cycle progression at the G2–M transition. Conclusion: LGH00045, a novel CDC25B inhibitor identified through HTS, showed good inhibition on the proliferation of tumor cells and affected the cell cycle progression, which makes it a good hit for further structure modification.

Keywords: LGH00045; cell circle; cell division cycle 25B; cyclin-dependent kinase 1; high-throughput screening; inhibitor

Document Type: Research Article


Affiliations: National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China

Publication date: October 1, 2008


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