ArticlePloS one2013
Identification of the plant compound geraniin as a novel Hsp90 inhibitor.
Article in PloS one, 2013. 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, 37 citations in OpenAlex.
- The Research Progress in Targeted Therapy for Hypertension via Heat Shock Proteins.International journal of molecular sciences · 2026Review
- Deciphering the cancer chemopreventive potential of phytochemicals: an integrative perspective on molecular targets and signaling networks.Cancer cell international · 2026Review
- Unlocking the Therapeutic Potential of Ellagitannins: A Comprehensive Review of Key Representatives.Molecules (Basel, Switzerland) · 2025Review
- Exploring the Anticancer Potential ofPlants (Basel, Switzerland) · 2023Article
- Repositioning of Quinazolinedione-Based Compounds on Soluble Epoxide Hydrolase (sEH) through 3D Structure-Based Pharmacophore Model-Driven Investigation.Molecules (Basel, Switzerland) · 2022Article
- Antibacterial activity of geraniin from sugar maple leaves: an ultrastructural study with the phytopathogenJournal of plant pathology : an international journal of the Italian Phytopathological Society · 2021Article
- Antiviral Role of Phenolic Compounds against Dengue Virus: A Review.Biomolecules · 2020Review
- Phytochemicals as modulators of M1-M2 macrophages in inflammation.Oncotarget · 2018Review
- Discovery of new molecular entities able to strongly interfere with Hsp90 C-terminal domain.Scientific reports · 2018Article
- Polyphenols as Promising Drugs against Main Breast Cancer Signatures.Antioxidants (Basel, Switzerland) · 2017Review
- Novel Benzylidene Thiazolidinedione Derivatives as Partial PPARγ Agonists and their Antidiabetic Effects on Type 2 Diabetes.Scientific reports · 2017Article
- Geraniin Inhibits LPS-Induced THP-1 Macrophages Switching to M1 Phenotype via SOCS1/NF-κB Pathway.Inflammation · 2016Article
- Targeting Cell Survival Proteins for Cancer Cell Death.Pharmaceuticals (Basel, Switzerland) · 2016Review
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Besides its function in normal cellular growth, the molecular chaperone heat shock protein 90 (Hsp90) binds to a large number of client proteins required for promoting cancer cell growth and/or survival. In an effort to discover new small molecules able to inhibit the Hsp90 ATPase and chaperoning activities, we screened, by a surface plasmon resonance assay, a small library including different plant polyphenols. The ellagitannin geraniin, was identified as the most promising molecule, showing a binding affinity to Hsp90α similar to that of 17-(allylamino)-17-demethoxygeldanamycin (17AGG). Geraniin was able to inhibit in vitro the Hsp90α ATPase activity in a dose-dependent manner, with an inhibitory efficiency comparable to that measured for 17-AAG. In addition, this compound compromised the chaperone activity of Hsp90α, monitored by the citrate synthase thermal induced aggregation assay. Geraniin decreased the viability of HeLa and Jurkat cell lines and caused an arrest in G2/M phase. We also proved that following exposure to different concentrations of geraniin, the level of expression of the client proteins c-Raf, pAkt, and EGFR was strongly down-regulated in both the cell lines. These results, along with the finding that geraniin did not exert any appreciable cytotoxicity on normal cells, encourage further studies on this compound as a promising chemical scaffold for the design of new Hsp90 inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.