公开(公告)号：US20070123465A1

公开(公告)日：2007-05-31

申请号：US11629883

申请日：2005-06-17

申请人： Knut Adermann ,  Frank Kirchhoff ,  Jan Munch ,  Axel Schulz ,  Wolf-Georg Forssmann

发明人： Knut Adermann ,  Frank Kirchhoff ,  Jan Munch ,  Axel Schulz ,  Wolf-Georg Forssmann

IPC分类号： A61K38/16 ,  C07K14/16

CPC分类号： A61K38/16 ,  C07K14/8121

摘要： The invention relates to oligomeric peptides with biological activity against HIV infection having the amino acid sequence (Z1-LE-X1-IP—X2—X3—X4—P—X5—X6—X7—X8—X9—X10—K—X11—X12—X13—X14—X15-Z2)n, wherein n indicates the number of monomeric peptide chains, whereby n is 2, 3 or 4; X1 is a lysine, alanine, or aspartic acid; X2 is a cysteine, methionine or isoleucine; X3 is a serine, cysteine, lysine or glycine; X4 is an isoleucine, alanine, phenylalanine or cysteine; X5 is a proline, D-proline or a substituted L- or D-proline; X6 is a cysteine or glutamic acid; X7 is an amino acid with a hydrophobic or an aromatic side chain or cysteine; X8 is an amino acid with a hydrophobic or an aromatic side chain or cysteine; X9 is an amino acid with an aromatic side chain; X10 is a glycine, alanine or asparagine; X11 is a proline, aspartic acid, octahydroindolyl-2-carboxylic acid or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; X12 is a phenylalanine, alanine, glycine, glutamic acid or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; X13 is an amino acid with a hydrophobic or an aromatic side chain; X14 is an amino acid with a hydrophobic or an aromatic side chain; X15 is a phenylalanine or deletion; Z1 is NH2 or a sequence of 1 to 10 amino acid residues; Z2 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 X12 is alanine, glycine, glutamic acid, or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid than X13, X14 and X15 are phenylalanine, valine and phenylalanine respectively; and/or (b) if X12 is phenylalanine, than X13, X14 and X15 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)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.

公开(公告)号：US07037896B1

公开(公告)日：2006-05-02

申请号：US10111427

申请日：2000-11-08

申请人： Frank Kirchhoff ,  Jan Münch ,  Ludger Ständker ,  Wolf-Georg Forssmann

发明人： Frank Kirchhoff ,  Jan Münch ,  Ludger Ständker ,  Wolf-Georg Forssmann

IPC分类号： A61K38/16 ,  C07K7/08 ,  C07K2/00 ,  A61K38/00 ,  A61K38/02

CPC分类号： C07K7/08 ,  A61K38/00

摘要： A peptide having the following amino acid sequence: Z1-LEAIPMSIPPEVKFNKPFVF-Z2 (VIRIP) and its biologically active fragments and/or variants and/or derivatives, especially amidated, acetylated, sulfated, polyethylene glycol (PEG) modified, phosphorylated and/or glycosylated derivatives, and peptides obtainable by multiple synthesis which have the biological activity of VIRIP; wherein Z1 and Z2 are independently a sequence of from 0 to 10 amino acid residues, and if Z1 or Z2=zero amino acid residues, then Z1=H and/or Z2=COOH.

摘要翻译： 具有以下氨基酸序列的肽：<？in-line-formula description =“In-line Formulas”end =“lead”？> Z 1 -leAIPMSIPPEVKFNKPFVF-Z 2 （VIRIP）<？in-line-formula description =“In-line Formulas”end =“tail”？>及其生物活性片段和/或变体和/或衍生物，特别是酰胺化，乙酰化，硫酸化，聚乙二醇 （PEG）修饰的，磷酸化和/或糖基化衍生物，以及可通过多重合成获得的具有VIRIP生物学活性的肽; 其中Z 1和Z 2独立地是0至10个氨基酸残基的序列，并且如果Z 1或Z 2 0个氨基酸残基，则Z 1 = H和/或Z 2 = COOH。