Pub. Date : 2014
PMID : 24621983
10 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | ABCB1 1199G>A genetic polymorphism (Rs2229109) influences the intracellular accumulation of tacrolimus in HEK293 and K562 recombinant cell lines. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | OBJECTIVE: ATP-binding cassette, subfamily B, member 1 (ABCB1) transporter, or P-glycoprotein, is an efflux protein implicated in the absorption and the distribution of various compounds, including tacrolimus and cyclosporine A. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | OBJECTIVE: ATP-binding cassette, subfamily B, member 1 (ABCB1) transporter, or P-glycoprotein, is an efflux protein implicated in the absorption and the distribution of various compounds, including tacrolimus and cyclosporine A. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | OBJECTIVE: ATP-binding cassette, subfamily B, member 1 (ABCB1) transporter, or P-glycoprotein, is an efflux protein implicated in the absorption and the distribution of various compounds, including tacrolimus and cyclosporine A. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 5 | In vivo studies suggest an association between the ABCB1 1199G>A single nucleotide polymorphism (SNP) and tacrolimus intracellular accumulation. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 6 | The impact of the 1199G>A SNP on ABCB1 activity towards rhodamine (Rh123), doxorubicin, vinblastine, tacrolimus and cyclosporine A was assessed by accumulation, cytotoxicity and/or kinetic experiments. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 7 | RESULTS: Tacrolimus accumulation was strongly decreased in cells overexpressing the wild-type protein (1199G) compared to control cells, confirming the ability of ABCB1 to transport tacrolimus. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 8 | RESULTS: Tacrolimus accumulation was strongly decreased in cells overexpressing the wild-type protein (1199G) compared to control cells, confirming the ability of ABCB1 to transport tacrolimus. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 9 | CONCLUSION: ABCB1 encoded by the 1199G wild-type allele transports more efficiently tacrolimus in comparison to the 1199A variant protein. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 10 | This observation indicates that the amino-acid substitution (Ser400Asn) encoded by the 1199A allele drastically decreases the ability of ABCB1 to drive the efflux of tacrolimus in a substrate-specific manner, in agreement with our previously published clinical data. | Tacrolimus | ATP binding cassette subfamily B member 1 | Homo sapiens |