ArticleGynecologic oncology2020
Dual targeting of GSK3B and HDACs reduces tumor growth and improves survival in an ovarian cancer mouse model.
Article in Gynecologic oncology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- Design, synthesis and antiproliferative activity of oxadiazole derivatives as potent glycogen synthase kinase-3/histone deacetylase 6 dual inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2026Article
- Targeting epigenetic networks to overcome cisplatin resistance in ovarian cancer: from mechanisms to clinical translation.Journal of ovarian research · 2026Review
- Immunocompetent C57BL/6 syngeneic mouse ovarian cancer models with defined genetic alterations.Scientific reports · 2025Article
- HDAC4/MybL1/YAP novel signaling axis is required for pancreatic cancer metastasis to the liver.International journal of biological sciences · 2025Article
- CSTF3 contributes to platinum resistance in ovarian cancer through alternative polyadenylation of lncRNA NEAT1 and generating the short isoform NEAT1_1.Cell death & disease · 2024Article
- INHBA(+) cancer-associated fibroblasts generate an immunosuppressive tumor microenvironment in ovarian cancer.NPJ precision oncology · 2024Article
- A deep learning model predicts the presence of diverse cancer types using circulating tumor cells.Scientific reports · 2023Article
- Inhibition of GSK3β activity alleviates acute liver failure via suppressing multiple programmed cell death.Journal of inflammation (London, England) · 2023Article
- MicroRNA-214-3p facilitates M2 macrophage polarization by targeting GSK3B.The Kaohsiung journal of medical sciences · 2022Article
- Characterization of neuroendocrine regulation- and metabolism-associated molecular features and prognostic indicators with aid to clinical chemotherapy and immunotherapy of patients with pancreatic cancer.Frontiers in endocrinology · 2022Article
- Efficacy evaluation of multi-immunotherapy in ovarian cancer: From bench to bed.Frontiers in immunology · 2022Review
- CIRCNV: Detection of CNVs Based on a Circular Profile of Read Depth from Sequencing Data.Biology · 2021Article
- Integrin α2β1 Represents a Prognostic and Predictive Biomarker in Primary Ovarian Cancer.Biomedicines · 2021Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
objectiveTo investigate the anti-tumor effect of a newly-developed dual inhibitor (APCS-540) of glycogen synthase kinase 3 beta (GSK3B) and histone deacetylases (HDACs) in ovarian cancer cells.
methodsThe effects of APCS-540 on cancer cell proliferation, migration, invasion and cancer stemness were investigated in vitro in human (KURAMOCHI, OVCA420, OVSAHO) and mouse (BR-Luc, ID8, MOSE-HRas-Myc) ovarian cancer cells. Cisplatin-sensitive (A2780) and cisplatin-resistant (A2780cis) cell lines were used to evaluate APCS-540's effect on chemoresistance. The immunocompetent syngeneic mouse model BR-Luc was used to test the effect of APCS-540 on ovarian cancer progression and survival.
resultsAPCS-540 showed significant anti-tumor effects in vitro in both human and mouse ovarian cancer cells. Importantly, APCS-540 demonstrated marked cytotoxicity against cisplatin-resistant cancer cells and reversed cisplatin-resistance when used in combination with platinum. APCS-540 significantly decreased cancer cell invasion. A significant 66% increase in survival was observed in mice treated with APCS-540 compared to control mice.
conclusionDual inhibition of GSK3B and HDACs via APCS-540 showed potent anti-tumor activity in vitro and in vivo, suggesting that APCS-540 may provide a novel treatment option for ovarian cancer, including the platinum-resistant disease.
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