β-Galactosidase (β-gal) is an important biomarker for ovarian cancers. In this work, we designed and synthesized a novel iridium(III)-based probe 1 for discriminating ovarian carcinoma cell lines from normal cell lines. The probe could detect β-gal even in the presence of a highly autofluorescent background. The probe also showed a good linear response to β-gal between 0 and 30 U/mL, with a detection limit of 0.51 U/mL. Importantly, complex 1 could selectively "light up" ovarian carcinoma cells, while exhibiting negligible luminescence in normal cells. Overall, complex 1 could be potentially used as a useful probe for detecting β-gal expression in the context of ovarian cancer diagnostics.
We report herein a novel rhodium(III) complex 1 as a new LSD1 targeting agent and epigenetic modulator. Complex 1 disrupted the interaction of LSD1-H3K4me2 in human prostate carcinoma cells and enhanced the amplification of p21, FOXA2, and BMP2 gene promoters. Complex 1 was selective for LSD1 over other histone demethylases, such as KDM2b, KDM7, and MAO activities, and also showed antiproliferative activity toward human cancer cells. To date, complex 1 is the first metal-based inhibitor of LSD1 activity.
The rhodium(iii) complex 1 was identified as a potent Wee1 inhibitor in vitro and in cellulo. It decreased Wee1 activity and unscheduled mitotic entry, and induced cell damage and death in TP53-mutated triple-negative breast cancer cells. 1 represents a promising scaffold for further development of more potent metal-based Wee1 antagonists.
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