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Abstract

The invention relates to oligomeric peptides with biological activity against HIV infection having the amino acid sequence (Z.sub.1-LE-X.sub.1-IP--X.sub.2--X.sub.3--X.sub.4--P--X.sub.5--X.sub.6--X-.sub.7--X.sub.8--X.sub.9--X.sub.10--K--X.sub.11--X.sub.12--X.sub.13--X.sub-.14--X.sub.15-Z.sub.2).sub.n, wherein n indicates the number of monomeric peptide chains, whereby n is 2, 3 or 4; X.sub.1 is a lysine, alanine, or aspartic acid; X.sub.2 is a cysteine, methionine or isoleucine; X.sub.3 is a serine, cysteine, lysine or glycine; X.sub.4 is an isoleucine, alanine, phenylalanine or cysteine; X.sub.5 is a proline, D-proline or a substituted L- or D-proline; X.sub.6 is a cysteine or glutamic acid; X.sub.7 is an amino acid with a hydrophobic or an aromatic side chain or cysteine; X.sub.8 is an amino acid with a hydrophobic or an aromatic side chain or cysteine; X.sub.9 is an amino acid with an aromatic side chain; X.sub.10 is a glycine, alanine or asparagine; X.sub.11 is a proline, aspartic acid, octahydroindolyl-2-carboxylic acid or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; X.sub.12 is a phenylalanine, alanine, glycine, glutamic acid or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; X.sub.13 is an amino acid with a hydrophobic or an aromatic side chain; X.sub.14 is an amino acid with a hydrophobic or an aromatic side chain; X.sub.15 is a phenylalanine or deletion; Z.sub.1 is NH.sub.2 or a sequence of 1 to 10 amino acid residues; Z.sub.2 is COOH or a sequence of 1 to 10 amino acid residues; and oligomeric peptides which are fragments thereof and/or derivatives, especially amidated, alkylated, acylated, sulfated, pegylated, phosphorylated and/or glycosylated derivatives, and mutants thereof; and with the proviso that (a) if X.sub.12 is alanine, glycine, glutamic acid, or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid than X.sub.13, X.sub.14 and X.sub.15 are phenylalanine, valine and phenylalanine respectively; and/or (b) if X.sub.12 is phenylalanine, than X.sub.13, X.sub.14 and X.sub.15 are valine, phenylalanine and a deletion, respectively; and (c) there are at maximum three cysteine residues in a peptide; and (d) the oligomeric peptide has not the sequence (LEAIPCSIPPEFLFGKPFVF).sub.2 (VIR-576); and (e) the monomeric peptide chains are not linked by peptide bonds between the N-terminus of one peptide chain to the C-terminus of another peptide chain.

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First Claim