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    • 1. 发明授权
    • Peptides impairing PBX dependent gene regulation
    • 损害PBX依赖性基因调控的肽
    • US07728105B2
    • 2010-06-01
    • US10538723
    • 2003-12-12
    • Richard George Leonard MorganRuth PettengellNicolas Pierre Benoît ForrazColin Patrick McGuckin
    • Richard George Leonard MorganRuth PettengellNicolas Pierre Benoît ForrazColin Patrick McGuckin
    • C07K14/00
    • C07K14/4702A61K38/08
    • The present invention relates to peptides which impair PBX-dependent regulation of gene transcription. In particular, the invention provides the use of a peptide comprising the amino acid sequence X1 X2 X3 W M X4 X5 X6 X7, wherein the sequence X1 to X7 is an amino acid sequence comprising at least 9 amino acids, which may optionally be interrupted by one or two amino acid residues between one or more of the 9 amino acid positions defined herein; X1 is selected from W, T, PE, KQI, VV, PQT, H, RI and absent; X2 is an amino acid with an aromatic side chain; X3 is P or D; X4 is an amino acid with a basic side chain; X5 is an amino acid with a charged side chain; X6 is an amino acid with a charged side chain; and X7 is an amino acid with a basic side chain or Serine; in the manufacture of a medicament for treating or preventing a disorder in which aberrant cell division occurs.
    • 本发明涉及削弱基因转录的PBX依赖性调节的肽。 特别地,本发明提供了包含氨基酸序列X1 X2 X3 WM X4 X5 X6 X7的肽的用途,其中序列X1至X7是包含至少9个氨基酸的氨基酸序列,其可任选地被一个 或在本文定义的9个氨基酸位置中的一个或多个之间的两个氨基酸残基; X1选自W,T,PE,KQI,VV,PQT,H,RI和不存在; X2是具有芳香侧链的氨基酸; X3是P或D; X4是具有碱性侧链的氨基酸; X5是具有带电侧链的氨基酸; X6是具有带电侧链的氨基酸; X7是具有碱性侧链或丝氨酸的氨基酸; 在制备用于治疗或预防发生异常细胞分裂的病症的药物中。
    • 4. 发明申请
    • Gene Regulation
    • US20090286738A1
    • 2009-11-19
    • US11993978
    • 2006-06-28
    • Richard George Leonard MorganJastinder Sohal
    • Richard George Leonard MorganJastinder Sohal
    • A61K38/03A61K38/04A61P35/00C12N5/00
    • A61K38/10A61K38/08C07K14/47
    • The present invention relates to peptides, which impair PBX-dependent regulation of gene transcription and thus have utility in the treatment or prevention of disorders in which aberrant cell division occurs. In particular, the invention provides peptides comprising the amino acid sequence (I), Y1 X1 X2 X3 W X4 X5 X6 X7 X8 Y2 (I) wherein the sequence X1 to X8 is an amino acid sequence comprising at least 8 amino acids, which may optionally be interrupted by one or two amino acid residues between one or more of the 9 amino acid positions defined herein; X1 is selected from W, T, PE, KQI, VV, PQT, H, RI and absent; X2 is an amino acid with an aromatic side chain or cysteine; X3 is P or D; X4 is a hydrophobic amino acid X5 is an amino acid with a charged side chain; X6 is an amino acid with a basic side chain; X7 is a polar hydrophilic amino acid; X8 is one or more amino acids or absent; and Y1 and Y2 are each either absent or a peptide comprising a cationic polymer of basic amino acids, such that at least one Of Y1 and Y2 is present; and peptides comprising the amino acid sequence (II): Y3 X1 X2 X3 W X4 X5 X6 X7 X8 Y4 (II) wherein The sequence X1 to X8 is an amino acid sequence comprising at least 8 amino acids, which may optionally be interrupted by one or two amino acid residues between one or more of the 9 amino acid positions defined herein; X1 is selected from W, T, PE, KQI, VV, PQT, H, RI and absent; X2 is an amino acid with an aromatic side chain; X3 is P or D; X4 is a hydrophobic amino acid X5 is an amino acid with a charged side chain; X6 is an amino acid with a basic side chain; X7 is a polar hydrophilic amino acid; X8 is one or more amino acids or absent; and Y3 and Y4 are each either absent or a peptide comprising a sequence comprising a cell penetration moiety, such that at least one of Y3 and Y4 is present; wherein at least the N-terminal and C-terminal amino acids of said peptide is in the D-conformation.