Title |
ATP‐binding cassette subfamily B member 1 (ABCB1) and subfamily C member 10 (ABCC10) are not primary resistance factors for cabazitaxel
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Published in |
Cancer Communications, March 2015
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DOI | 10.1186/s40880-015-0003-0 |
Pubmed ID | |
Authors |
Rishil J Kathawala, Yi-Jun Wang, Suneet Shukla, Yun-Kai Zhang, Saeed Alqahtani, Amal Kaddoumi, Suresh V Ambudkar, Charles R Ashby, Zhe-Sheng Chen |
Abstract |
ATP-binding cassette subfamily B member 1 (ABCB1) and subfamily C member 10 (ABCC10) proteins are efflux transporters that couple the energy derived from ATP hydrolysis to the translocation of toxic substances and chemotherapeutic drugs out of cells. Cabazitaxel is a novel taxane that differs from paclitaxel by its lower affinity for ATP-binding cassette (ABC) transporters. We determined the effects of cabazitaxel, a novel tubulin-binding taxane, and paclitaxel on paclitaxel-resistant, ABCB1-overexpressing KB-C2 and LLC-MDR1-WT cells and paclitaxel-resistant, ABCC10-overexpressing HEK293/ABCC10 cells by calculating the degree of drug resistance and measuring ATPase activity of the ABCB1 transporter. Decreased resistance to cabazitaxel compared with paclitaxel was observed in KB-C2, LLC-MDR1-WT, and HEK293/ABCC10 cells. Moreover, cabazitaxel had low efficacy, whereas paclitaxel had high efficacy in stimulating the ATPase activity of ABCB1, indicating a direct interaction of both drugs with the transporter. ABCB1 and ABCC10 are not primary resistance factors for cabazitaxel compared with paclitaxel, suggesting that cabazitaxel may have a low affinity for these efflux transporters. |
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Geographical breakdown
Country | Count | As % |
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Unknown | 26 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Ph. D. Student | 4 | 15% |
Student > Postgraduate | 4 | 15% |
Student > Doctoral Student | 2 | 8% |
Student > Bachelor | 2 | 8% |
Researcher | 2 | 8% |
Other | 7 | 27% |
Unknown | 5 | 19% |
Readers by discipline | Count | As % |
---|---|---|
Biochemistry, Genetics and Molecular Biology | 6 | 23% |
Pharmacology, Toxicology and Pharmaceutical Science | 5 | 19% |
Medicine and Dentistry | 5 | 19% |
Chemistry | 1 | 4% |
Unspecified | 1 | 4% |
Other | 0 | 0% |
Unknown | 8 | 31% |