ArticleOncotarget2017
Structure based discovery of clomifene as a potent inhibitor of cancer-associated mutant IDH1.
Article in Oncotarget, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed, 30 citations in OpenAlex.
- Machine learning-based QSAR and structure-based virtual screening guided discovery of novel mIDH1 inhibitors from natural products.Journal of computer-aided molecular design · 2025Article
- Clomiphene Citrate Medication for Infertility and Risk of Stillbirth or Neonatal Death: A Population-based Cohort Study.The Journal of clinical endocrinology and metabolism · 2025Article
- Emerging therapeutic strategies in glioblastsoma: drug repurposing, mechanisms of resistance, precision medicine, and technological innovations.Clinical and experimental medicine · 2025Review
- The regulatory mechanisms and inhibitors of isocitrate dehydrogenase 1 in cancer.Acta pharmaceutica Sinica. B · 2023Review
- ITGB3BP is a potential biomarker associated with poor prognosis of glioma.Journal of cellular and molecular medicine · 2022Article
- Glioma-Targeted Therapeutics: Computer-Aided Drug Design Prospective.The protein journal · 2021Review
- An Alternative Pipeline for Glioblastoma Therapeutics: A Systematic Review of Drug Repurposing in Glioblastoma.Cancers · 2021Review
- New insights into molecules and pathways of cancer metabolism and therapeutic implications.Cancer communications (London, England) · 2021Review
- Discovery of Novel IDH1 Inhibitor Through Comparative Structure-Based Virtual Screening.Frontiers in pharmacology · 2020Article
- Novel Insights for Inhibiting Mutant Heterodimer IDH1Molecular diagnosis & therapy · 2018Article
- Beyond Brooding on Oncometabolic Havoc in IDH-Mutant Gliomas and AML: Current and Future Therapeutic Strategies.Cancers · 2018Review
- Drug Repositioning in Glioblastoma: A Pathway Perspective.Frontiers in pharmacology · 2018Review
- Thiopurine Drugs Repositioned as Tyrosinase Inhibitors.International journal of molecular sciences · 2017Article
- Farnesyl phenolic enantiomers as natural MTH1 inhibitors fromOncotarget · 2017Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Isocitrate dehydrogenase (IDH) plays an indispensable role in the tricarboxylic acid cycle, and IDH mutations are present in nearly 75% of glioma and 20% of acute myeloid leukemia. One IDH1R132H inhibitor (clomifene citrate) was found by virtual screening method, which can selectively suppress mutant enzyme activities in vitro and in vivo with a dose-dependent manner. The molecular docking indicated that clomifene occupied the allosteric site of the mutant IDH1. Enzymatic kinetics also demonstrated that clomifene inhibited mutant enzyme in a non-competitive manner. Moreover, knockdown of mutant IDH1 in HT1080 cells decreased the sensitivity to clomifene. In vivo studies indicated that clomifene significantly suppressed the tumor growth of HT1080-bearing CB-17/Icr-scid mice with oral administration of 100 mg/kg and 50 mg/kg per day. In short, our findings highlight clomifene may have clinical potential in tumor therapies as a safe and effective inhibitor of mutant IDH1.
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Registered trials
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