ArticleTumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine2016
Reversal of efflux of an anticancer drug in human drug-resistant breast cancer cells by inhibition of protein kinase Cα (PKCα) activity.
Article in Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine, 2016. 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, 23 citations in OpenAlex.
- Article
- Evaluation of Novel Benzo-annelated 1,4-dihydropyridines as MDR Modulators in Cancer Cells.Anti-cancer agents in medicinal chemistry · 2024Article
- Protein Kinase C (PKC) Isozymes as Diagnostic and Prognostic Biomarkers and Therapeutic Targets for Cancer.Cancers · 2022Review
- Role of aurora kinase B in regulating resistance to paclitaxel in breast cancer cells.Human cell · 2022Article
- Human erythrocytes, nuclear factor kappaB (NFκB) and hydrogen sulfide (HCell cycle (Georgetown, Tex.) · 2021Article
- PKCα Inhibition as a Strategy to Sensitize Neuroblastoma Stem Cells to Etoposide by Stimulating Ferroptosis.Antioxidants (Basel, Switzerland) · 2021Article
- The specific PKC-α inhibitor chelerythrine blunts costunolide-induced eryptosis.Apoptosis : an international journal on programmed cell death · 2020Article
- Markers of MEK inhibitor resistance in low-grade serous ovarian cancer: EGFR is a potential therapeutic target.Cancer cell international · 2019Article
- Long-term exposure to carcinoma-associated fibroblasts makes breast cancer cells addictive to integrin β1.Oncotarget · 2018Article
- Identification of crucial genes and prediction of small molecules for multidrug resistance of Hodgkin's lymphomas.Cancer biomarkers : section A of Disease markers · 2018Article
- Protein Kinases C-Mediated Regulations of Drug Transporter Activity, Localization and Expression.International journal of molecular sciences · 2017Review
- 11a-N-Tosyl-5-deoxi-pterocarpan, LQB-223, a novel compound with potent antineoplastic activity toward breast cancer cells with different phenotypes.Journal of cancer research and clinical oncology · 2016Article
- Long-Term Alteration of Reactive Oxygen Species Led to Multidrug Resistance in MCF-7 Cells.Oxidative medicine and cellular longevity · 2016Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
P-glycoprotein (Pgp) is a 170-kDa transmembrane protein that mediates the efflux of anticancer drugs from cells. Pgp overexpression has a distinct role in cells exhibiting multidrug resistance (MDR). We examined reversal of drug resistance in human MDR breast cancer cells by inhibition of protein kinase Cα (PKCα) activity, which is associated with Pgp-mediated efflux of anticancer drugs. PKCα activity was confirmed by measurement of phosphorylation levels of a PKCα-specific peptide substrate (FKKQGSFAKKK-NH2), showing relatively higher basal activity in drug-resistant MCF-7/ADR cells (84 %) than that in drug-sensitive MCF-7 cells (63 %). PKCα activity was effectively suppressed by the PKC inhibitor, Ro-31-7549, and reversal of intracellular accumulation of doxorubicin was observed by inhibition of PKCα activity in MCF-7/ADR cells compared with their intrinsic drug resistance. Importantly, increased accumulation of doxorubicin could enhance the therapeutic efficacy of doxorubicin in MDR cells significantly. These results suggest a potential for overcoming MDR via inhibition of PKCα activity with conventional anticancer drugs.
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