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
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 syn...
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| Published in | Nucleic Acids Symposium Series Vol. 52; no. 1; pp. 475 - 476 |
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| Main Authors | , , , |
| Format | Journal Article |
| Language | English |
| Published |
Oxford University Press
01.09.2008
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| Online Access | Get full text |
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| Abstract | 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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| AbstractList | 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 |
| Author | Ron, David Lackey, Jeremy G. Damha, Masad J. Harding, Heather P. |
| Author_xml | – sequence: 1 givenname: Jeremy G. surname: Lackey fullname: Lackey, Jeremy G. organization: 1 Department of Chemistry, McGill University, Montreal, QC, Canada H3A 2K6 and 2Kimmel Center for Biology and Medicine of the Skirball Institute and 3Department of Pharmacology, New York University School of Medicine, New York, New York 10016, USA – sequence: 2 givenname: David surname: Ron fullname: Ron, David organization: 1 Department of Chemistry, McGill University, Montreal, QC, Canada H3A 2K6 and 2Kimmel Center for Biology and Medicine of the Skirball Institute and 3Department of Pharmacology, New York University School of Medicine, New York, New York 10016, USA – sequence: 3 givenname: Masad J. surname: Damha fullname: Damha, Masad J. email: masad.damha@mcgill.ca organization: 1 Department of Chemistry, McGill University, Montreal, QC, Canada H3A 2K6 and 2Kimmel Center for Biology and Medicine of the Skirball Institute and 3Department of Pharmacology, New York University School of Medicine, New York, New York 10016, USA – sequence: 4 givenname: Heather P. surname: Harding fullname: Harding, Heather P. email: harding@saturn.med.nyu.edu organization: 1 Department of Chemistry, McGill University, Montreal, QC, Canada H3A 2K6 and 2Kimmel Center for Biology and Medicine of the Skirball Institute and 3Department of Pharmacology, New York University School of Medicine, New York, New York 10016, USA |
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| Copyright | 2008 Oxford University Press 2008 |
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| DOI | 10.1093/nass/nrn241 |
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We report the solid-phase synthesis of novel 2′P-RNA probes for use in fluorescence polarization (FP) ligand binding assays that screens for... |
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| Title | 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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