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Updated: Feb 7, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
2-(2-nitrobenzylidene) indolin-3-one compound inhibits transmembrane prostate androgen-induced protein (TMEPAI)
Yuyin Li1, Jianjun Wang1, Ning Song1
1Key Lab of Industrial Fermentation Microbiology of the Ministry of Education, School of Biotechnology, Tianjin University of Science and Technology, Tianjin, China.
Objectives:
The transmembrane prostate androgen-induced protein (TMEPAI) is aberrantly expressed in many cancer and plays a crucial role in tumourigenesis, which makes it a potential cancer therapeutic target for drug discovery.
Materials And Methods:
Here, we employed a firefly luciferase reporter driven by the TMEPAI gene promoter to screen for compound capable of inhibiting the expression of TMEPAI, and the effects of TMEPAI inhibitor on cancer cell proliferation were evaluated using the colony formation assay, cell cycle analysis, Ki-67 immunofluorescence assay and EdU incorporation assay.
Results:
2-(2-nitrobenzylidene) indolin-3-one (JHY-A007-50) was identified and shown to effectively inhibit the TMEPAI promoter activity. Further studies revealed that JHY-A007-50 specifically inhibited the expression of TMEPAI at both the mRNA and protein levels. Moreover, we found that JHY-A007-50 could inhibit cell proliferation and induce cell cycle arrest at the G1 phase. Our results showed that overexpression of TMEPAI decreased the inhibitory effects of JHY-A007-50 on cancer cell proliferation, and JHY-A007-50 did not affect the cell viability of HeLa cells knocked down of TMEPAI.
Conclusions:
Taken together, these results suggest that compound JHY-A007-50 mediates the downregulation of TMEPAI expression and inhibits cell proliferation in cancer cells.
Insights
A novel compound, JHY-A007-50, effectively inhibits the transmembrane prostate androgen-induced protein (TMEPAI) and suppresses cancer cell proliferation. This discovery offers a potential new therapeutic strategy for cancer treatment targeting TMEPAI.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Aberrant expression of transmembrane prostate androgen-induced protein (TMEPAI) is implicated in tumorigenesis.
- TMEPAI represents a potential therapeutic target for cancer drug discovery.
Purpose of the Study:
- To screen for compounds that inhibit TMEPAI expression.
- To evaluate the effects of identified inhibitors on cancer cell proliferation.
Main Methods:
- A firefly luciferase reporter assay was used to screen for TMEPAI inhibitors.
- Cancer cell proliferation was assessed via colony formation, cell cycle analysis, Ki-67 immunofluorescence, and EdU incorporation assays.
Main Results:
- 2-(2-nitrobenzylidene) indolin-3-one (JHY-A007-50) was identified as a potent inhibitor of TMEPAI promoter activity.
- JHY-A007-50 suppressed TMEPAI expression at both mRNA and protein levels, inhibited cancer cell proliferation, and induced G1 phase cell cycle arrest.
- Overexpression of TMEPAI reduced the inhibitory effects of JHY-A007-50, confirming TMEPAI's role in mediating the compound's action.
Conclusions:
- Compound JHY-A007-50 effectively downregulates TMEPAI expression.
- JHY-A007-50 demonstrates significant potential in inhibiting cancer cell proliferation, highlighting its therapeutic promise.
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