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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 |
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