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• W2003264942 abstract "HIV gene expression is crucially dependent on binding of the viral Tat protein to the transactivation RNA response element. A number of synthetic Tat‐transactivation responsive element interaction inhibitors of peptide/peptoid nature were described as potential antiviral drug prototypes. We present a new class of peptidomimetic inhibitors, conjugates of l ‐arginine with aminoglycosides. Using a gel‐shift assay and affinity chromatography on an l ‐arginine column we found that these compounds bind specifically to the transactivation responsive element RNA in vitro with K d values in the range of 20–400 nM, which is comparable to the K d of native Tat bound to the transactivation responsive element (10–12 nM). Confocal microscopy studies demonstrated that fluorescein‐labelled conjugate penetrates into live cells. High affinity to the transactivation responsive element, low toxicity, and relative simplicity of synthesis make these compounds attractive candidates for antiviral drug design." @default.
• W2003264942 created "2016-06-24" @default.
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• W2003264942 date "1999-02-19" @default.
• W2003264942 modified "2023-10-13" @default.
• W2003264942 title "Arginine‐aminoglycoside conjugates that bind to HIV transactivation responsive element RNA in vitro" @default.
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• W2003264942 doi "https://doi.org/10.1016/s0014-5793(99)00092-7" @default.
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