ArticleBritish journal of pharmacology2013
Targeting the ABCG2-overexpressing multidrug resistant (MDR) cancer cells by PPARγ agonists.
Article in British journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 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
21 citing papers in PubMed, 34 citations in OpenAlex.
- Pharmacokinetic Interaction Between Telmisartan and Rosuvastatin/Ezetimibe After Multiple Oral Administration in Healthy Subjects.Advances in therapy · 2021Trial
- Telmisartan increases systemic exposure to rosuvastatin after single and multiple doses, and in vitro studies show telmisartan inhibits ABCG2-mediated transport of rosuvastatin.European journal of clinical pharmacology · 2016Trial
- ABCG2-autophagy regulatory axis in cancer stem cells: implication in cancer metastasis, recurrence and chemotherapy resistance.Cell communication and signaling : CCS · 2026Review
- Influence of Gut Microbiota-Derived Butyrate on Intestinal Uric Acid Excretion and Hyperuricemia Regulation byInternational journal of molecular sciences · 2025Article
- ATP-Binding Cassette Subfamily G Member 2 in Acute Myeloid Leukemia: A New Molecular Target?Biomedicines · 2024Review
- Article
- A Cross-Talk about Radioresistance in Lung Cancer-How to Improve Radiosensitivity According to Chinese Medicine and Medicaments That Commonly Occur in Pharmacies.International journal of molecular sciences · 2023Review
- Telmisartan anti-cancer activities mechanism through targeting N-cadherin by mimicking ADH-1 function.Journal of cellular and molecular medicine · 2022Article
- Multidrug efflux transporter ABCG2: expression and regulation.Cellular and molecular life sciences : CMLS · 2021Review
- PI3K/AKT pathway as a key link modulates the multidrug resistance of cancers.Cell death & disease · 2020Review
- Alleviation of Multidrug Resistance by Flavonoid and Non-Flavonoid Compounds in Breast, Lung, Colorectal and Prostate Cancer.International journal of molecular sciences · 2020Review
- Bergenin as a Novel Urate-Lowering Therapeutic Strategy for Hyperuricemia.Frontiers in cell and developmental biology · 2020Article
- Unraveling the journey of cancer stem cells from origin to metastasis.Biochimica et biophysica acta. Reviews on cancer · 2019Review
- Cariprazine, A Dopamine D₂/D₃ Receptor Partial Agonist, Modulates ABCG2-Mediated Multidrug Resistance in Cancer.Cancers · 2018Article
- A Synergistic Anti-Cancer Effect of Troglitazone and Lovastatin in a Human Anaplastic Thyroid Cancer Cell Line and in a Mouse Xenograft Model.International journal of molecular sciences · 2018Article
- Beyond Competitive Inhibition: Regulation of ABC Transporters by Kinases and Protein-Protein Interactions as Potential Mechanisms of Drug-Drug Interactions.Drug metabolism and disposition: the biological fate of chemicals · 2018Review
- Soluble uric acid increases PDZK1 and ABCG2 expression in human intestinal cell lines via the TLR4-NLRP3 inflammasome and PI3K/Akt signaling pathway.Arthritis research & therapy · 2018Article
- Identification and characterization of biomarkers and their functions for Lapatinib-resistant breast cancer.Medical oncology (Northwood, London, England) · 2017Article
- Targeting cancer stem cell-specific markers and/or associated signaling pathways for overcoming cancer drug resistance.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2016Review
- Pelitinib (EKB-569) targets the up-regulation of ABCB1 and ABCG2 induced by hyperthermia to eradicate lung cancer.British journal of pharmacology · 2015Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeMultidrug resistance (MDR), usually mediated by overexpression of efflux transporters such as P-gp, ABCG2 and/or MRP1, remains a major obstacle hindering successful cancer chemotherapy. There has been great interest in the development of inhibitors towards these transporters to circumvent resistance. However, since the inhibition of transporter is not specific to cancer cells, a decrease in the cytotoxic drug dosing may be needed to prevent excess toxicity, thus undermining the potential benefit brought about by a drug efflux inhibitor. The design of potent MDR modulators specific towards resistant cancer cells and devoid of drug-drug interactions will be needed to effect MDR reversal. EXPERIMENTAL APPROACH: Recent evidence suggests that the PTEN/PI3K/Akt pathway may be exploited to alter ABCG2 subcellular localization, thereby circumventing MDR. Three PPARγ agonists (telmisartan, pioglitazone and rosiglitazone) that have been used in the clinics were tested for their effect on the PTEN/PI3K/Akt pathway and possible reversal of ABCG2-mediated drug resistance. KEY
resultsThe PPARγ agonists were found to be weak ABCG2 inhibitors by drug efflux assay. They were also shown to elevate the reduced PTEN expression in a resistant and ABCG2-overexpressing cell model, which inhibit the PI3K-Akt pathway and lead to the relocalization of ABCG2 from the plasma membrane to the cytoplasma, thus apparently circumventing the ABCG2-mediated MDR. CONCLUSIONS AND IMPLICATIONS: Since this PPARγ/PTEN/PI3K/Akt pathway regulating ABCG2 is only functional in drug-resistant cancer cells with PTEN loss, the PPARγ agonists identified may represent promising agents targeting resistant cells for MDR reversal.
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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.