ArticleOncotarget2015
Preclinical model in HCC: the SGK1 kinase inhibitor SI113 blocks tumor progression in vitro and in vivo and synergizes with radiotherapy.
Article in Oncotarget, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 62 citations in OpenAlex.
- Brain Permeable SGK1 Inhibitors: A Promising Therapeutic Strategy for Neurodegenerative Diseases.Journal of medicinal chemistry · 2026Article
- Discovery of a brain penetrant SGK1 inhibitor using a ligand- and structure-based virtual screening methodology.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Unraveling the Potential of SGK1 in Osteoporosis: From Molecular Mechanisms to Therapeutic Targets.Biomolecules · 2025Review
- Role of Serum/Glucocorticoid-Regulated Kinase 1 (SGK1) in Immune and Inflammatory Diseases.Inflammation · 2023Review
- Inhibition of serum- and glucocorticoid-induced kinase 1 ameliorates hydrocephalus in preclinical models.Fluids and barriers of the CNS · 2023Article
- RANBP1 (RAN Binding Protein 1): The Missing Genetic Piece in Cancer Pathophysiology and Other Complex Diseases.Cancers · 2023Review
- Expression profiles of glucocorticoid-inducible proteins in human papilloma virus-related oropharyngeal squamous cell carcinoma.Frontiers in oral health · 2023Article
- Long non-coding RNA VPS9D1-AS1 enhances proliferation, invasion, and epithelial-mesenchymal transition in endometrial cancer via miR-377-3p/SGK1.The Kaohsiung journal of medical sciences · 2022Article
- SGK1 in Cancer: Biomarker and Drug Target.Cancers · 2022Article
- Multiomics Differences in Lung Squamous Cell Carcinoma Patients with High Radiosensitivity Index Compared with Those with Low Radiosensitivity Index.Disease markers · 2021Article
- Expression Profiles of GILZ and SGK-1 in Potentially Malignant and Malignant Human Oral Lesions.Frontiers in oral health · 2021Article
- Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-Molecules (Basel, Switzerland) · 2020Article
- Drug repurposing against COVID-19: focus on anticancer agents.Journal of experimental & clinical cancer research : CR · 2020Review
- SGK1 in Human Cancer: Emerging Roles and Mechanisms.Frontiers in oncology · 2020Review
- Lack of PPARBioMed research international · 2020Article
- The Emerging Role of SGK1 (Serum- and Glucocorticoid-Regulated Kinase 1) in Major Depressive Disorder: Hypothesis and Mechanisms.Frontiers in genetics · 2020Review
- The prospect of serum and glucocorticoid-inducible kinase 1 (SGK1) in cancer therapy: a rising star.Therapeutic advances in medical oncology · 2020Review
- Review
- In Preclinical Model of Ovarian Cancer, the SGK1 Inhibitor SI113 Counteracts the Development of Paclitaxel Resistance and Restores Drug Sensitivity.Translational oncology · 2019Article
- Ras-ling with new therapeutic targets for metastasis.Small GTPases · 2019Article
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Authors and funding
20 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The SGK1 kinase is pivotal in signal transduction pathways operating in cell transformation and tumor progression. Here, we characterize in depth a novel potent and selective pyrazolo[3,4-d]pyrimidine-based SGK1 inhibitor. This compound, named SI113, active in vitro in the sub-micromolar range, inhibits SGK1-dependent signaling in cell lines in a dose- and time-dependent manner. We recently showed that SI113 slows down tumor growth and induces cell death in colon carcinoma cells, when used in monotherapy or in combination with paclitaxel. We now demonstrate for the first time that SI113 inhibits tumour growth in hepatocarcinoma models in vitro and in vivo. SI113-dependent tumor inhibition is dose- and time-dependent. In vitro and in vivo SI113-dependent SGK1 inhibition determined a dramatic increase in apoptosis/necrosis, inhibited cell proliferation and altered the cell cycle profile of treated cells. Proteome-wide biochemical studies confirmed that SI113 down-regulates the abundance of proteins downstream of SGK1 with established roles in neoplastic transformation, e.g. MDM2, NDRG1 and RAN network members. Consistent with knock-down and over-expressing cellular models for SGK1, SI113 potentiated and synergized with radiotherapy in tumor killing. No short-term toxicity was observed in treated animals during in vivo SI113 administration. These data show that direct SGK1 inhibition can be effective in hepatic cancer therapy, either alone or in combination with radiotherapy.
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