05--indicated that ACSL1, ABCA1, DHCR24, ACAT2, ACACA, ABCG1, ACAD9, ACACB, IDI1, PPARG, SCD, SCARB1, HMGCS1, EBP, DHCR7, FASN, HMGCR, and GPAM were down-regulated upon G treatment; whereas NR1H2, PPARA, INSIG2, CPTP1, APOE, VLDLR, ABCC2
, and SREBF2 were activated after exposure to G (Fig.
, and ABCB1 (also known as multidrug resistance-associated proteins: MRP1, MRP2, and MDR1), are the most well-characterized ABC transporters.
Association between ABCC2
gene haplotypes and tenofovir-inducedproximal tubulopathy.
Genetic polymorphisms in CYP3A5, CYP3A4 (cytochrome P450, family 3, subfamily A, polypeptide 4), MDR1, UGT1A9, ABCC2
[ATPbinding cassette, sub-family C (CFTR/MRP), member 2; formerly known as MRP2], and TPMT (thiopurine S-methyltransferase) have an impact on tacrolimus, MPA, and azathioprine metabolism and transport, respectively.
Effect of the ATP- binding cassette drug transporters ABCB1, ABCG2, and ABCC2
on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/-(triple-knockout) and wild-type mice.
Both organic anions and xenobiotics in the blood use the same organic anion transporters (OATs) for entry into proximal tubule cells and they then exit these cells through ATP dependent ABCC2
(MRP2) and ABCC4 (MRP4), cassette transporters located at the luminal membrane of the cells (Sekine et al.
Bilirubin conjugates are then actively secreted into the canaliculi by ABCC2
[membrane ATP-binding cassette subfamily C (CFTR/MRP) member 2].
For example, the anticancer drug irinotecan is not only metabolized by UGT1A1 but is also a substrate for transporter molecules coded by ABCB1, ABCC2
, ABCG2, and SLCO1B1 (4).
variants CYP450 CYP1A2 6 CYP2A6 7 CYP2B6 10 CYP2C19 12 CYP2C8 4 CYP2C9 10 CYP2D6 18 CYP2E1 1 CYP2J2 5 CYP3A4 2 CYP3A5 8 Non-CYP enzymes CDA 2 DPYD 6 FMO2 1 FMO3 2 GSTP1 2 NAT1 12 NAT2 7 TPMT 5 UGT1A1 9 Transporters ABCB1 6 ABCC2
6 SLCO1B1 9 SLCO2B1 1 SLC15A2 4 SLC22A1 6 SLC22A2 4 (a) Variants tested include SNPs, insertions, deletions, triallelic variants, and nucleotide repeats.
Nrf2-dependent and -independent induction of ABC transporters ABCC1, ABCC2
, and ABCG2 in HepG2 cells under oxidative stress.
Although the differentiation-dependent and sterol-regulated induction of ABCA1 and ABCG1 is well established (7), parallel transcript profiling, using our Human ABC Transporter TaqMan Low-Density Array, revealed several additional differentiation-dependent ABC transporters and novel LXR/RXR-regulated ABC transporters, including ABCB1 (MDR1), ABCB9, ABCB11 (BSEP), ABCC2
(MRP2), ABCC5 (MRP5), ABCD1 (ALD), ABCD4, and ABCG2.
The primers were: ABCB1, 3977 5'-GCTCGTCCCCTTGTTAG-ACAGCC-3' 3999 and 4186 5-CGTGCCATGCTCCTTGACTCTGC-3' 4164; ABCC1, 4381 5'-CCTGGAGCTGGCCCACCTGA-3' 4400 and 4551 5'-GCTGCCGTGGCCTCATCCAA-3 4532; ABCC2
, 2075 5-GCAGCAGGTCAGAGTGTGGTTTC-3' 2097 and 2383 5-GTGATTCT-TCCACAAGCCCCAGG-3' 2361; GAPDH, 961 5-AACAGCGACACCCA-CTCaC-3' 980 and 1045 5'-CATACCAGGAAATGAGCTTGACAA-3' 1022.