Toward the discovery of new antifungal agents: the design and validation of a novel 2'P-RNA probe and high throughput screening assay against 2'-phosphotransferase Tpt1p

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Abstract

We report the solid-phase synthesis of novel 2'P-RNA probes for use in fluorescence polarization (FP) ligand binding assays that screens for inhibitors of the yeast 2'- phosphotransferase Tpt1p. The probe was synthesized by utilizing silyl phosphoramidite chemistry and a phosphoramidite synthon containing an orthogonal (DMT) protecting group at its 2'-position. Regioselective removal of the 2'-DMT group and phosphitylation of the unmasked 2'-hydroxyl group afforded the desired 2'P-RNA sequence.

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Lackey, J. G., Ron, D., Damha, M. J., & Harding, H. P. (2008). Toward the discovery of new antifungal agents: the design and validation of a novel 2’P-RNA probe and high throughput screening assay against 2’-phosphotransferase Tpt1p. Nucleic Acids Symposium Series (2004), (52), 475–476. https://doi.org/10.1093/nass/nrn241

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