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Dual inhibitors of the human blood-brain barrier drug efflux transporters P-glycoprotein and ABCG2 based on the antiviral azidothymidine

Bioorg. Med. Chem.. 2017-10; 
Namanja-MaglianoHilda A, BohnKelsey, AgrawalNeha, WilloughbyMeghan E, HrycynaChristine A, Chmielewski
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Biochemicals … 2. Experimental section. 2.1. Materials. AZT and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) were purchased from AK Scientific (Union City, CA). 4- dimethylaminopyridine (DMAP) was purchased from GenScript (Piscataway, NJ) … Get A Quote

摘要

The brain provides a sanctuary site for HIV due, in part, to poor penetration of antiretroviral agents at the blood-brain barrier. This lack of penetration is partially attributed to drug efflux transporters such as P-glycoprotein (P-gp) and ABCG2. Inhibition of both ABCG2 and P-gp is critical for enhancing drug accumulation into the brain. In this work, we have developed a class of homodimers based on the HIV reverse transcriptase inhibitor azidothymidine (AZT) that effectively inhibits P-gp and ABCG2. These agents block transporter mediated efflux of the P-gp substrate calcein-AM and the ABCG2 substrate mitoxantrone. The homodimers function by interacting with the transporter drug binding sites as demon... More

关键词

ABCG2,AZT,Blood-brain barrier,Inhibition,P-glycopro