Alpha-helix mimetics and methods relating thereto
AssigneeMolecumetics, Ltd.
InventorMichael Kahn
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Abstract
There are disclosed alpha-helix mimetics and methods relating to the same for imparting or stabilizing alpha-helicity to a peptide or protein. In one aspect, the alpha-helix mimetics contain twelve-membered rings covalently attached at the end or within the length of the peptide or protein. The alpha-helix mimetics render the resulting peptide or protein more stable with regard to thermal stability, as well as making the peptide or protein more resistant to proteolytic degradation. In addition, the alpha-helix mimetics may be used in standard peptide synthesis protocols.
Claims6
An alpha-helix mimetic having the structure:
- ##STR12## wherein R.sub.1 through R.sub.5 are independently selected from an amino acid side chain moiety and derivative thereof;
- and X and Y represent the remainder of the mimetic.
An alpha-helix modified peptide or protein, comprising a peptide or protein and an alpha-helix mimetic, the alpha-helix mimetic being covalently attached to at least one amino acid of the peptide or protein, wherein the alpha-helix mimetic has the structure:
- ##STR13## wherein R.sub.1 through R.sub.5 are independently selected from an amino acid side chain moiety and derivative thereof;
- and at least X or Y is an amino acid of the peptide or protein.
A method for imparting or stabilizing alpha-helicity to a peptide or protein, comprising covalently attaching an alpha-helix mimetic to the peptide or protein, wherein the alpha-helix mimetic has the structure:
- ##STR14## wherein R.sub.1 through R.sub.5 are independently selected from an amino acid side chain moiety and derivative thereof;
- and at least X or Y represent an amino acid of the peptide or protein.
Dependencies are inferred from the claim text.