Pub. Date : 2006 Jan
PMID : 16454695
17 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
1 | Topotecan is a substrate for multidrug resistance associated protein 4. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
2 | This study aimed to investigate whether overexpression of human MRP4 rendered resistance to TPT by examining the cytotoxicity profiles using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazonium bromide (MTT) assay and cellular accumulation of TPT in HepG2 cells stably overexpressing MRP4. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
3 | This study aimed to investigate whether overexpression of human MRP4 rendered resistance to TPT by examining the cytotoxicity profiles using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazonium bromide (MTT) assay and cellular accumulation of TPT in HepG2 cells stably overexpressing MRP4. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
4 | The intracellular accumulation of TPT and paclitaxel (a PgP substrate) by V/HepG2 and MRP4/HepG2 cells was determined by incubation of TPT with the cells and the amounts of the drug in cells were determined by validated HPLC methods. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
5 | The study demonstrated that MRP4 conferred a 12.03- and 6.86-fold resistance to TPT in the 4- and 48-hr drug-exposure MTT assay, respectively. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
6 | BSO, MK-571, celecoxib, or diclofenac sensitised MRP4/HepG2 cells to TPT cytotoxicity and partially reversed MRP4-mediated resistance to TPT. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
7 | BSO, MK-571, celecoxib, or diclofenac sensitised MRP4/HepG2 cells to TPT cytotoxicity and partially reversed MRP4-mediated resistance to TPT. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
8 | In addition, the accumulation of TPT was significantly reduced in MRP4/HepG2 cells compared to V/HepG2 cells, and one-binding site model was found the best fit for the MRP4-mediated efflux of TPT, with an estimated K(m) of 1.66 microM and V(max) of 0.341 ng/min/106 cells. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
9 | In addition, the accumulation of TPT was significantly reduced in MRP4/HepG2 cells compared to V/HepG2 cells, and one-binding site model was found the best fit for the MRP4-mediated efflux of TPT, with an estimated K(m) of 1.66 microM and V(max) of 0.341 ng/min/106 cells. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
10 | In addition, the accumulation of TPT was significantly reduced in MRP4/HepG2 cells compared to V/HepG2 cells, and one-binding site model was found the best fit for the MRP4-mediated efflux of TPT, with an estimated K(m) of 1.66 microM and V(max) of 0.341 ng/min/106 cells. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
11 | In addition, the accumulation of TPT was significantly reduced in MRP4/HepG2 cells compared to V/HepG2 cells, and one-binding site model was found the best fit for the MRP4-mediated efflux of TPT, with an estimated K(m) of 1.66 microM and V(max) of 0.341 ng/min/106 cells. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
12 | Preincubation of MRP4/HepG2 cells with BSO (200 microM) for 24 hr, celecoxib (50 microM), or MK-571 (100 microM) for 2 hr significantly increased the accumulation of TPT over 10 min in MRP4/HepG2 cells by 28.0%, 37.3% and 32.5% (P < 0.05), respectively. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
13 | Preincubation of MRP4/HepG2 cells with BSO (200 microM) for 24 hr, celecoxib (50 microM), or MK-571 (100 microM) for 2 hr significantly increased the accumulation of TPT over 10 min in MRP4/HepG2 cells by 28.0%, 37.3% and 32.5% (P < 0.05), respectively. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
14 | These findings indicate that MRP4 confers resistance to TPT and TPT is the substrate for MRP4. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
15 | These findings indicate that MRP4 confers resistance to TPT and TPT is the substrate for MRP4. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
16 | These findings indicate that MRP4 confers resistance to TPT and TPT is the substrate for MRP4. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |
17 | Further studies are needed to explore the role of MRP4 in resistance to, toxicity and pharmacokinetics of TPT in cancer patients. | Topotecan | ATP binding cassette subfamily C member 4 | Homo sapiens |