PMID- 12636175 OWN - NLM STAT- MEDLINE DCOM- 20030909 LR - 20190818 IS - 0724-8741 (Print) IS - 0724-8741 (Linking) VI - 20 IP - 2 DP - 2003 Feb TI - Gene expression profiles of ABC transporters and cytochrome P450 3A in Caco-2 and human colorectal cancer cell lines. PG - 324-7 AB - 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 FAU - Nakumura, Tsutomu AU - Nakumura T AD - Department of Hospital Pharmacy, School of Medicine, Kobe University, Chuo-ku, Kobe 650-0017, Japan. FAU - Sakaeda, Toshiyuki AU - Sakaeda T FAU - Ohmoto, Nobuko AU - Ohmoto N FAU - Moriya, Yuka AU - Moriya Y FAU - Komoto, Chiho AU - Komoto C FAU - Shirakawa, Toshiro AU - Shirakawa T FAU - Gotoh, Akinobu AU - Gotoh A FAU - Matsuo, Masafumi AU - Matsuo M FAU - Okmura, Katsuhiko AU - Okmura K LA - eng PT - Comparative Study PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - United States TA - Pharm Res JT - Pharmaceutical research JID - 8406521 RN - 0 (ATP-Binding Cassette Transporters) RN - 0 (RNA, Messenger) RN - EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases) RN - EC 1.14.14.1 (Cytochrome P-450 CYP3A) RN - EC 1.5.- (Oxidoreductases, N-Demethylating) SB - IM MH - ATP-Binding Cassette Transporters/*biosynthesis/genetics MH - Aryl Hydrocarbon Hydroxylases/*biosynthesis/genetics MH - Caco-2 Cells MH - Colorectal Neoplasms/enzymology/*metabolism MH - Cytochrome P-450 CYP3A MH - *Gene Expression Profiling/methods MH - Gene Expression Regulation, Neoplastic MH - Humans MH - Oxidoreductases, N-Demethylating/*biosynthesis/genetics MH - RNA, Messenger/biosynthesis/genetics MH - Tumor Cells, Cultured EDAT- 2003/03/15 04:00 MHDA- 2003/09/10 05:00 CRDT- 2003/03/15 04:00 PHST- 2003/03/15 04:00 [pubmed] PHST- 2003/09/10 05:00 [medline] PHST- 2003/03/15 04:00 [entrez] AID - 10.1023/a:1022251910820 [doi] PST - ppublish SO - Pharm Res. 2003 Feb;20(2):324-7. doi: 10.1023/a:1022251910820.