ArticleScientific reports2016
Discovery of a small-molecule binder of the oncoprotein gankyrin that modulates gankyrin activity in the cell.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 35 citations in OpenAlex.
- Gankyrin-Protein Interactions in GI Cancers: A Novel Target of New Therapeutics.Chronic diseases and translational medicine · 2025Review
- Structural modification of the propyl linker of cjoc42 in combination with sulfonate ester and triazole replacements for enhanced gankyrin binding and anti-proliferative activity.Bioorganic & medicinal chemistry · 2024Article
- Synthesis and evaluation of 2,5-substituted pyrimidines as small-molecule gankyrin binders.Future medicinal chemistry · 2024Article
- Small-Molecule Gankyrin Inhibition as a Therapeutic Strategy for Breast and Lung Cancer.Journal of medicinal chemistry · 2022Article
- Second Generation Small Molecule Inhibitors of Gankyrin for the Treatment of Pediatric Liver Cancer.Cancers · 2022Article
- Visible-light-induced one-pot synthesis of sulfonic estersRSC advances · 2022Article
- Identification of a covalent binder to the oncoprotein gankyrin using a NIR-Based OBOC screening method.RSC advances · 2021Article
- Small Molecule Cjoc42 Improves Chemo-Sensitivity and Increases Levels of Tumor Suppressor Proteins in Hepatoblastoma Cells and in Mice by Inhibiting Oncogene Gankyrin.Frontiers in pharmacology · 2021Article
- Case Report: Contiguous Xq22.3 Deletion Associated with ATS-ID Syndrome: From Genotype to Further Delineation of the Phenotype.Frontiers in genetics · 2021Article
- Quantitative expression of Ikaros, IRF4, and PSMD10 proteins predicts survival in VRD-treated patients with multiple myeloma.Blood advances · 2020Article
- Small-Molecule Inhibitors of the Proteasome's Regulatory Particle.Chembiochem : a European journal of chemical biology · 2019Review
- Gankyrin is a novel biomarker for disease progression and prognosis of patients with renal cell carcinoma.EBioMedicine · 2019Article
- Arctigenin Inhibits Liver Cancer Tumorigenesis by Inhibiting Gankyrin Expression via C/EBPα and PPARα.Frontiers in pharmacology · 2018Article
- Gankyrin Promotes Tumor-Suppressor Protein Degradation to Drive Hepatocyte Proliferation.Cellular and molecular gastroenterology and hepatology · 2018Article
- Tumor Suppressor Down-Regulation Promotes Hepatocyte Proliferation: A New GANKster on the Block.Cellular and molecular gastroenterology and hepatology · 2018Article
- RNA Binding Protein CUGBP1 Inhibits Liver Cancer in a Phosphorylation-Dependent Manner.Molecular and cellular biology · 2017Article
- FXR-Gankyrin axis is involved in development of pediatric liver cancer.Carcinogenesis · 2017Article
- Article
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
Gankyrin is an ankyrin-repeat oncoprotein whose overexpression has been implicated in the development of many cancer types. Elevated gankyrin levels are linked to aberrant cellular events including enhanced degradation of tumour suppressor protein p53, and inhibition of gankyrin activity has therefore been identified as an attractive anticancer strategy. Gankyrin interacts with several partner proteins, and a number of these protein-protein interactions (PPIs) are of relevance to cancer. Thus, molecules that bind the PPI interface of gankyrin and interrupt these interactions are of considerable interest. Herein, we report the discovery of a small molecule termed cjoc42 that is capable of binding to gankyrin. Cell-based experiments demonstrate that cjoc42 can inhibit gankyrin activity in a dose-dependent manner: cjoc42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin, and it restores p53-dependent transcription and sensitivity to DNA damage. The results represent the first evidence that gankyrin is a "druggable" target with small molecules.
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