ATP-binding cassette subfamily B member 1 (ABCB1) and subfamily C member 10 (ABCC10) are not primary resistance factors for cabazitaxel.
Rishil J Kathawala, Yi-Jun Wang, Suneet Shukla, Yun-Kai Zhang, Saeed Alqahtani, Amal Kaddoumi, Suresh V Ambudkar, Charles R Ashby, Zhe-Sheng Chen
文献索引:Chin. J. Cancer 34 , 115-20, (2015)
全文:HTML全文
摘要
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.
相关化合物
相关文献:
2015-01-03
[Vaccine 33(2) , 346-53, (2014)]
2014-01-01
[BMC Biotechnol. 14 , 962, (2015)]
2015-06-01
[Bioresour. Technol. 185 , 185-93, (2015)]
2015-06-01
[Bioresour. Technol. 185 , 49-55, (2015)]
2014-12-01
[Growth Factors 32(6) , 236-46, (2014)]