PMID: 11904219Mar 21, 2002Paper

Inhibition of nuclear import by backbone cyclic peptidomimetics derived from the HIV-1 MA NLS sequence

Biochimica Et Biophysica Acta
Elana Hariton-GazalAbraham Loyter

Abstract

In the present work we have constructed a series of backbone cyclic peptides, which differed in the amino acid residues located at the C-terminal position of the previously described BCvir peptide (A. Friedler, N. Zakai, O. Karni, Y.C. Broder, L. Baraz, M. Kotler, A. Loyter, C. Gilon, Biochemistry 37 (1998)). BCvir is a cyclic peptide, derived from the nuclear localization signal (NLS) of the human immunodeficiency virus type 1 matrix protein. The majority of the cyclic peptides described here inhibited nuclear import in vitro. The most potent inhibitors were those bearing bulky hydrophobic amino acids such as Leu, Phe or Nal (naphthyl Ala) at the C-terminus. On the other hand, peptides bearing polar amino acid residues such as Asn, Cys or a reduced amide bond were not inhibitory. The present studies demonstrate the importance of a bulky hydrophobic C-terminal side chain and an exocyclic amide bond preceding it, to the inhibitory activity of the NLS-derived BC peptides. Being only inhibitory, these BC peptides resemble classic receptor antagonists.

References

Aug 14, 1986·Nature·D S GoldfarbR D Kornberg
Jul 19, 1994·Proceedings of the National Academy of Sciences of the United States of America·U von SchwedlerD Trono
Jul 1, 1996·Journal of Peptide Science : an Official Publication of the European Peptide Society·G BitanC Gilon
Sep 2, 1997·Proceedings of the National Academy of Sciences of the United States of America·P GallayD Trono

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Citations

Mar 24, 2011·Future Medicinal Chemistry·Hadar Benyamini, Assaf Friedler
Dec 2, 2004·Journal of Molecular Biology·Joseph RosenbluhAbraham Loyter
Oct 27, 2010·Bioorganic & Medicinal Chemistry·Zvi HayoukaAssaf Friedler
Aug 20, 2010·Biochimica Et Biophysica Acta·Aviad LevinMichael Bukrinsky
Jul 5, 2003·Organic Letters·Seung Bum ParkRobert F Standaert
Oct 25, 2003·Journal of Cell Science·Elana Hariton-GazalAbraham Loyter

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