Simple mimetics of a nuclear localization signal (NLS) |
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Authors: | Park Seung Bum Ho Thai H Reedy Brian M Connolly Michael D Standaert Robert F |
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Affiliation: | University of Illinois at Chicago, Department of Chemistry (M/C 111), 845 West Taylor Street, Room 4500, Chicago, Illinois 60607, USA. |
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Abstract: | [reaction: see text] Molecular modeling was used to design mimetics of the HIV-1 matrix protein nuclear localization signal (NLS) in which a scaffold of two resorcinol units joined by a diamide linker presents 3-aminopropyl ethers in place of lysine side chains. Prospective mimetics with linkers of 6, 8, 10, or 12 atoms were synthesized and compared in a competition assay for binding to the nuclear import receptor subunit karyopherin alpha, showing the 10-atom linker to be best and shorter ones ineffective. |
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