Peralkylated oligopeptide mixtures
AssigneeTorry Pines Institute for Molecular Studies
InventorsRichard A. Houghten, John M. Ostresh
Life of this patent
Estimating the term…
Abstract
Linear peralkylated oligopeptide sets of molecules are disclosed, as are their methods of synthesis and use in acceptor binding assays. Each molecule or chain of a set contains the same number of two to about ten substituted peralkylated amino acid residues, and the member chains of a set are present in equimolar amounts. The chains of a set contain one or more predetermined peralkylated amino acid residues at one or more predetermined positions of the peralkylated oligopeptide chain. The set contains equimolar amounts of at least six different peralkylated amino acid residues at one or more of the same predetermined positions of the peralkylated oligopeptide chain.
Claims20
A set of linear peralkylated oligopeptide chains comprising a mixture of equimolar amounts of linear peralkylated oligopeptide chain members containing the same number of about two to about ten peralkylated amino acid residues in each chain, each peralkylated amino acid residue except proline having its Deptidyl amido nitrogen atom alkylated with a C.sub.1 -C.sub.7 alkyl group, the members of said set having one or more of at least six different peralkylated amino acid residues at the same one or more predetermined positions of the peralkylated oligopeptide chain, and the set having equimolar amounts of at least six different of said peralkylated amino acid residues at one or more of the same other positions of the peralkylated oligopeptide chain, the amino-terminus of each peralkylated oligopeptide being selected from the group consisting of a quaternary alkylammonium group, an amino group, an N-alkylamino, an N-alkyl-N-C.sub.1 -C.sub.18 hydrocarboyl and a pyroglutamoyl group, and the carboxy-terminus being selected from the group consisting of an alkyl carboxylic ester, mono- or di-N-alkylcarboxamide and a carboxyl group.
A library of linear peralkylated oligopeptides that comprises a plurality of sets of linear peralkylated oligopeptide chains, each set of linear peralkylated oligopeptide chains comprising a mixture of equimolar amounts of linear peralkylated oligopeptide chain members containing the same number of about two to about ten peralkylated amino acid residues in each chain, each peralkylated amino acid residue except proline having its peptidyl amido nitrogen atom alkylated with a C.sub.1 -C.sub.7 alkyl group, the members of each set having one or more of at least six different peralkylated amino acid residues at the same one or more predetermined positions of the peralkylated oligopeptide chain, and each set having equimolar amounts of at least six different of said peralkylated amino acid residues at one or more of the same other positions of the peralkylated oligopeptide chain, the amino-terminus of each peralkylated oligopeptide being selected from the group consisting of a quaternary alkylammonium group, an amino group, an N-alkylamino, an N-alkyl-N-C.sub.1 -C.sub.18 hydrocarboyl and a pyroglutamoyl group, and the carboxy-terminus being selected from the group consisting of an alkyl carboxylic ester, mono- or di-N-alkylcarboxamide and a carboxyl group, each set of said library having the same length, termini and number of chain positions occupied by equimolar mixtures of the same at least six different peralkylated amino acid residues, and each set of said library differing from the other sets in:
- (a) the position of the one or more predetermined peralkylated amino acid residue in the peralkylated oligopeptide chain,
- (b) the identity of the one or more predetermined peralkylated amino acid residue, or
- (c) both the position and identity of the one or more predetermined peralkylated amino acid residue.
A library of linear peralkylated oligopeptides that comprises a plurality of sets of linear permethylated oligopeptide chains, each set of linear permethylated oligopeptide chains comprising a mixture of equimolar amounts of linear permethylated oligopeptide chain members containing the same number of about two to about ten permethylated amino acid residues in each chain, each amino acid residue except proline having its peptidyl amido nitrogen atom alkylated with a methyl group, the members of each set having one or more of at least six different permethylated amino acid residues at the same one or more predetermined positions of the permethylated oligopeptide chain, and each set having equimolar amounts of at least six different of said permethylated amino acid residues at one or more of the same other positions of the permethylated oligopeptide chain, the amino-terminus of each permethylated oligopeptide being selected from the group consisting of a quaternary trimethylammonium group, and a pyroglutamoyl group, and the carboxy-terminus being a N-methylcarboxamide, each set of said library having the same length, termini and number of chain positions occupied by equimolar mixtures of the same at least six different permethylated amino acid residues, and each set of said library differing from the other sets in:
- (a) the position of the one or more predetermined permethylated amino acid residue in the permethylated oligopeptide chain,
- (b) the identity of the one or more predetermined permethylated amino acid residue, or
- (c) both the position and identity of the one or more predetermined permethylated amino acid residue.
Dependencies are inferred from the claim text.