Simple mimetics of a nuclear localization signal (NLS)

Org Lett. 2003 Jul 10;5(14):2437-40. doi: 10.1021/ol034640t.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Molecular Mimicry*
  • Nuclear Localization Signals*

Substances

  • Nuclear Localization Signals