申请人:HOX THERAPEUTICS LIMITED
公开号:US10494412B2
公开(公告)日:2019-12-03
The present invention relates to novel 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 a peptide comprising the amino acid sequence (I): Y1X1X2KWX3X4X5X6X7Y2 (I) wherein the sequence X1 to X7 is an amino acid sequence comprising at least 7 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, W, PQT, H, R1 and absent; X2 is an amino acid with an aromatic side chain or cysteine; X3 is a hydrophobic amino acid X4 is an amino acid with a charged side chain; X5 is an amino acid with a basic side chain; X6 is an amino acid or absent; X7 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, provided that at least one of Y1 and Y2 is present.
本发明涉及新型多肽,它能损害依赖于 PBX 的基因转录调控,因此可用于治疗或预防细胞分裂异常的疾病。特别是,本发明提供了一种包含氨基酸序列(I)的多肽:Y1X1X2KWX3X4X5X6X7Y2 (I) 其中序列 X1 至 X7 是由至少 7 个氨基酸组成的氨基酸序列,可任选在本文定义的 9 个氨基酸位置中的一个或多个位置之间被一个或两个氨基酸残基打断;X1 选自 W、T、PE、KQI、W、PQT、H、R1 和无;X2 是具有芳香族侧链或半胱氨酸的氨基酸;X3 是疏水性氨基酸; X4 是带电荷侧链的氨基酸; X5 是带碱性侧链的氨基酸; X6 是一种氨基酸或不存在; X7 是一种或多种氨基酸或不存在; Y1 和 Y2 要么不存在,要么是由碱性氨基酸阳离子聚合物组成的肽,条件是至少存在 Y1 和 Y2 中的一种。