| Title |
Reversal of efflux of an anticancer drug in human drug-resistant breast cancer cells by inhibition of protein kinase Cα (PKCα) activity
|
|---|---|
| Published in |
Tumor Biology, September 2015
|
| DOI | 10.1007/s13277-015-3963-4 |
| Pubmed ID | |
| Authors |
Chan Woo Kim, Daisuke Asai, Jeong-Hun Kang, Akihiro Kishimura, Takeshi Mori, Yoshiki Katayama |
| 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. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Science communicators (journalists, bloggers, editors) | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 12 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 12 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 4 | 33% |
| Student > Bachelor | 2 | 17% |
| Professor > Associate Professor | 1 | 8% |
| Student > Master | 1 | 8% |
| Unknown | 4 | 33% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 4 | 33% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 17% |
| Chemical Engineering | 1 | 8% |
| Social Sciences | 1 | 8% |
| Chemistry | 1 | 8% |
| Other | 0 | 0% |
| Unknown | 3 | 25% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 06 September 2015.
All research outputs
#18,425,370
of 22,826,360 outputs
Outputs from Tumor Biology
#1,369
of 2,622 outputs
Outputs of similar age
#192,636
of 267,081 outputs
Outputs of similar age from Tumor Biology
#90
of 209 outputs
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