Inhibition of nuclear import by backbone cyclic peptide analogs

A backbone cyclic peptide for inhibiting transfer of macromolecules from the cell cytoplasm to the cell nucleus, wherein the macromolecules enter the nucleus by the mediation of a nuclear localization signal and the peptide is of the formula I:

• wherein n denotes an integer from 1 to 10 or may be zero, with the proviso that when n is zero NH is also absent;
• m denotes an integer from 1 to 10;
• R denotes lysine or glutamine;
• AA and AA2 independently denote an amino acid residue which may be the same or different.

A composition comprising a suitable carrier, and a backbone cyclic peptide in an amount sufficient to inhibit transfer of macromolecules from the cell cytoplasm to the cell nucleus, wherein the backbone cyclic peptide is of the formula I:

• wherein n denotes an integer from 1 to 10 or may be zero, with the proviso that when n is zero NH is also absent;
• m denotes an integer from 1 to 10;
• R denotes lysine or glutamine;
• AA and AA2 independently denote an amino acid residue which may be the same or different.

A method for inhibiting transfer of macromolecules from the cell cytoplasm to the cell nucleus, wherein said macromolecules enter the nucleus by mediation of a nuclear localization signal,

• said method comprising contacting the cell with a cyclic peptide of formula I:
• for a time and under conditions effective to inhibit transfer of said macromolecules from the cell cytoplasm to the cell nucleus, wherein n denotes an integer from 1 to 10 or may be zero, with the proviso that when n is zero NH is also absent;
• m denotes an integer from 1 to 10;
• R denotes lysine or glutamine;
• AA and AA2 independently denote an amino acid residue which may be the same or different.