Poster Presentation 37th Lorne Cancer Conference 2025

Out with the new, in with the old: utilising drug repurposing strategies to target cancer cell invasion and treatment resistance via TGFβ-mediated EMT signalling in high-grade serous ovarian carcinoma (HGSOC) (#245)

Amy Sarker 1 , Michelle Wong-Brown 2 3 , Amani Alghalayini 1 , Kristie A Dickson 1 , Dongli Liu 4 , Caroline E Ford 4 , Nikola A Bowden 2 3 , Deborah J Marsh 1
  1. Translational Oncology Group, School of Life Sciences, Faculty of Science, University of Technology Sydney, Ultimo, NSW, Australia
  2. Drug Repurposing and Medicines Research Program, Hunter Medical Research Institute, New Lambton Heights, NSW, Australia
  3. School of Medicine and Public Health, University of Newcastle, Newcastle, NSW, Australia
  4. Gynaecological Cancer Research Group, School of Clinical Medicine, Faculty of Medicine and Health, University of New South Wales, Sydney, NSW, Australia

Ovarian cancer is the 8th most common cancer in women, accounting for 4.7% of cancer-related deaths worldwide​1​, and claiming ~1050 Australian lives in 2023​2​. The most common and aggressive subtype, high-grade serous ovarian carcinoma (HGSOC) is characterised by treatment resistance and metastatic disease. Epithelial-to-Mesenchymal-Transition (EMT) is a cellular plasticity program that increases cell motility and is associated with drug resistance​3​. Unimpeded by anatomical barriers, aggregates of HGSOC cells spread throughout the peritoneal cavity in fluid known as ascites, re-attaching at distal locations, including the omentum.  Transforming Growth Factor-β (TGFβ) is a pleiotropic cytokine involved with EMT​4​. Despite increasing interest in both EMT and TGFβ, there are no clinically-approved therapies targeting these factors in solid tumours. Outcomes of in silico analyses using the virtual ligand-based screening-tool BLAZE™ (Cresset Discovery Services, UK) revealed Topoisomerase II-inhibitor and DNA-damaging agent Teniposide as a potential modulator of TGFβ activity, uncovering a novel role for this drug. Teniposide is FDA-approved for the treatment of refractory childhood Acute Lymphoblastic Leukaemia under the tradename Vumon®. Our preliminary investigations in a physiologically-relevant model of HGSOC cells established using the RASTRUM™ 3D bioprinter (Inventia Life Science), demonstrated that low-doses of Teniposide dismantled cellular aggregates indicative of EMT. This finding provided evidence that Teniposide could be repurposed as an EMT-targeting, anti-invasive agent for HGSOC at low doses, where adjuvant administration with standard-of-care platinum drugs has the potential to increase treatment success. Drug repurposing utilises in silico methods to screen clinically approved drugs with known safety profiles on targets beyond their intended use, bypassing the high costs, extensive timelines, and low success rates of traditional drug discovery pipelines. The repurposing of Teniposide into a low-dose anti-invasive therapy may provide additional treatment options, lengthen progression-free survival, and improve quality of life for patients with HGSOC; a highly-favourable and paradigm-shifting approach.  

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  4. Yeh HW, Lee SS, Chang CY, Lang YD, Jou YS. A new switch for TGFβ in cancer. Cancer Res. 2019;79(15):3797-3805. doi:10.1158/0008-5472.CAN-18-2019