Reference - Detail
| RRC ID | 41825 |
|---|---|
| Author | Nakumura T, Sakaeda T, Ohmoto N, Moriya Y, Komoto C, Shirakawa T, Gotoh A, Matsuo M, Okmura K. |
| Title | Gene expression profiles of ABC transporters and cytochrome P450 3A in Caco-2 and human colorectal cancer cell lines. |
| Journal | Pharm Res |
| Abstract |
PURPOSE:The mRNA levels of MDR1 (P-glycoprotein), multidrug resistance-associated proteins (MRP1, MRP2), cytochrome P450 3A (CYP3A) and villin in human colorectal cell lines (HCT-15, LoVo DLD-1, HCT-116 and SW620) were quantitatively compared with those in Caco-2 cells. METHODS:The mRNA levels were determined by real time quantitative polymerase chain reaction and expressed as the relative concen trations of MDR1 mRNA to glyceraldehyde-3-phosphate dehydro genase (GAPDH) mRNA. RESULTSl MDR1 mRNA was expressed in HCT-15 LoVo and DLD-1 cells at similar or lower level to Caco-2. The expression of MRP mRNA in the cell lines tested was comparable with Caco-2. MRP. mRNA was detected only in HCT-116 and SW620 at significantly lower level than Caco-2. CYP3A mRNA was detected in HCT-15 LoVo, DLD-1 and SW620 at similar level to Caco-2. CONCLUSIONS:HCT-15 LoVo and DLD-1 cells express proteins important for regulating the intestinal absorption of drugs, i.e., MDR1 MRP1 and CYP3A, whereas HCT-116 and SW620 cells were not acceptable for evaluation of absorption properties of drug candidates |
| Volume | 20(2) |
| Pages | 324-7 |
| Published | 2003-2-1 |
| DOI | 10.1023/a:1022251910820 |
| PMID | 12636175 |
| MeSH | ATP-Binding Cassette Transporters / biosynthesis* ATP-Binding Cassette Transporters / genetics Aryl Hydrocarbon Hydroxylases / biosynthesis* Aryl Hydrocarbon Hydroxylases / genetics Caco-2 Cells Colorectal Neoplasms / enzymology Colorectal Neoplasms / metabolism* Cytochrome P-450 CYP3A Gene Expression Profiling* / methods Gene Expression Regulation, Neoplastic Humans Oxidoreductases, N-Demethylating / biosynthesis* Oxidoreductases, N-Demethylating / genetics RNA, Messenger / biosynthesis RNA, Messenger / genetics Tumor Cells, Cultured |
| IF | 3.242 |
| Times Cited | 27 |
| WOS Category | CHEMISTRY, MULTIDISCIPLINARY PHARMACOLOGY & PHARMACY |
| Resource | |
| Human and Animal Cells | CACO-2(RCB0988) |