Simple mimetics of a nuclear localization signal (NLS).
[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.
Park
Seung Bum
SB
University of Illinois at Chicago, Department of Chemistry (M/C 111), 845 West Taylor Street, Room 4500, Chicago, Illinois 60607, USA.
Ho
Thai H
TH
Reedy
Brian M
BM
Connolly
Michael D
MD
Standaert
Robert F
RF
D018716:Molecular Mimicry; D019913:Nuclear Localization Signals
D019913:Nuclear Localization Signals