AI Article Synopsis
- The effectiveness of drugs that target lymphocytes, such as anticancer and antiretroviral medications, relies on their levels within cells, which can be influenced by ABC transporter proteins.
- Gene expression analysis of six key ABC transporters (MDR1, MRP1, MRP3, MRP4, MRP5, and BCRP) in lymphocytes revealed that MRP1 and MRP5 were most expressed in adults, while BCRP and MRP4 had higher levels at birth compared to after one month.
- The study found that HIV infection and antiretroviral treatments did not significantly affect the expression of these transporters, suggesting that certain drugs for newborns, like zidovudine, may not
Article Abstract
The efficacy of drugs acting on lymphocytes like anticancer, immunosuppressive, and antiretroviral drugs depends on their intracellular concentrations, which could be modulated by membrane efflux pumps belonging to the ABC transporter superfamily. The gene expression profiles of 6 main ABC transporters (MDR1, MRP1, MRP3, MRP4, MRP5, and BCRP) were established in lymphocytes from birth to adulthood using blood samples from 57 children and 15 adults (34 and 5 HIV-infected, respectively). Gene expression levels were quantified by quantitative RT-PCR. In adults, the MRP1 gene had the highest expression, followed by the MRP5 gene. BCRP and MRP4 genes were significantly higher expressed at birth than after 1 month of life. Neither HIV infection nor antiretroviral therapies modulated the gene expression profiles of ABC transporters. In conclusion, drugs that are substrates of BCRP and MRP4, like zidovudine, may have an altered efficacy in newborns.
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| http://dx.doi.org/10.1177/0091270009343696 | DOI Listing |
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