ArticleAngewandte Chemie (International ed. in English)2021
Interaction with Ribosomal Proteins Accompanies Stress Induction of the Anticancer Metallodrug BOLD-100/KP1339 in the Endoplasmic Reticulum.
Article in Angewandte Chemie (International ed. in English), 2021. 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, 61 citations in OpenAlex.
- BOLD-100 treatment induces systemic lipid crosstalk in metastatic colorectal carcinoma patients in a combination treatment with FOLFOX.iScience · 2026Article
- Proteome-Wide Target Identification Using Reactive Metallo-Scaffolds (r-mS): A Platform for Metallodrug Discovery.Angewandte Chemie (International ed. in English) · 2026Article
- Exploring chemical space for iridium(iii) complexes: a direct-to-biology (D2B) approach to identifying anticancer and antibacterial agents.Chemical science · 2026Article
- BOLD-100 in Combination with FOLFOX Is a Broadly Effective Therapeutic Strategy for Gastric Cancer.International journal of molecular sciences · 2026Article
- Leveraging Morphological Profiling for Mechanistic Elucidation of Metal-Based Anticancer Compounds.JACS Au · 2026Article
- Combinational studies of BOLD-100/KP1339 with established chemotherapeutics in gastrointestinal multicellular tumor spheroids.Cancer chemotherapy and pharmacology · 2026Article
- Yeast Phenomic Analysis Reveals DNA Repair, pH Homeostasis, and Ribosomal Biogenesis as Modulators of Anticancer Ruthenium Complex KP1019.International journal of molecular sciences · 2026Article
- Naphthoquinone-derived tridentate Ru(II) and Os(II) organometallics with exceptional cytotoxicity: synthesis, characterization, stability in aqueous solution and biologicalDalton transactions (Cambridge, England : 2003) · 2026Article
- Methods for the Investigation of Protein-Ligands Interactions.Advances in experimental medicine and biology · 2026Review
- Identification of AICD-associated transcriptomic markers in major depressive disorder.Frontiers in psychiatry · 2026Article
- Momordicine I induces ER stress and inhibits OSCC by targeting ribosomal proteins.Journal of Zhejiang University. Science. B · 2025Article
- Therapeutic potential of BOLD-100, a GRP78 inhibitor, enhanced by ATR inhibition in pancreatic ductal adenocarcinoma.Cell communication and signaling : CCS · 2025Article
- Unraveling BOLD-100 synergistic potential in pleural mesothelioma treatment: an in vitro study.Investigational new drugs · 2025Article
- Metal-based immunogenic cell death inducers for cancer immunotherapy.Chemical science · 2025Review
- Metal-detection based techniques and their applications in metallobiology.Chemical science · 2024Review
- Complexes of Ruthenium(II) as Promising Dual-Active Agents against Cancer and Viral Infections.Pharmaceuticals (Basel, Switzerland) · 2023Review
- The Lipid Metabolism as Target and Modulator of BOLD-100 Anticancer Activity: Crosstalk with Histone Acetylation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2023Article
- Exploring the Potential of Metal-Based Candidate Drugs as Modulators of the Cytoskeleton.Chembiochem : a European journal of chemical biology · 2023Review
- From the Discovery of Targets to Delivery Systems: How to Decipher and Improve the Metallodrugs' Actions at a Molecular Level.Pharmaceutics · 2023Review
- A monoadduct generating Ru(ii) complex induces ribosome biogenesis stress and is a molecular mimic of phenanthriplatin.RSC chemical biology · 2023Article
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The ruthenium-based anticancer agent BOLD-100/KP1339 has shown promising results in several in vitro and in vivo tumour models as well as in early clinical trials. However, its mode of action remains to be fully elucidated. Recent evidence identified stress induction in the endoplasmic reticulum (ER) and concomitant down-modulation of HSPA5 (GRP78) as key drug effects. By exploiting the naturally formed adduct between BOLD-100 and human serum albumin as an immobilization strategy, we were able to perform target-profiling experiments that revealed the ribosomal proteins RPL10, RPL24, and the transcription factor GTF2I as potential interactors of this ruthenium(III) anticancer agent. Integrating these findings with proteomic profiling and transcriptomic experiments supported ribosomal disturbance and concomitant induction of ER stress. The formation of polyribosomes and ER swelling of treated cancer cells revealed by TEM validated this finding. Thus, the direct interaction of BOLD-100 with ribosomal proteins seems to accompany ER stress-induction and modulation of GRP78 in cancer cells.
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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.