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Thrombospondin1 binding peptide

机译:血压出素1结合肽

摘要

Provided is a compound that can promote angiogenesis by inhibiting the function of TSP1, and is useful for the treatment or prophylaxis of diseases such as critical limb ischemia.Specifically provided is a macrocyclic polypeptide represented by formula (I)[wherein A is selected from the linking groups Ato A; Xis a residue of an aliphatic amino acid, an aromatic amino acid, a basic amino acid, a neutral amino acid, or an acidic amino acid, or is absent; Xis a residue of an aromatic amino acid or a neutral amino acid; Xis a residue of an aliphatic amino acid, an aromatic amino acid, or a basic amino acid; Xaa4 is Ser, Thr, Ala, orS; Xis Gly or Ser; Xis a residue of a basic amino acid or a neutral amino acid; Xis a residue of a neutral amino acid or an acidic amino acid; Xis a residue of an aromatic amino acid; Xis a residue of an aliphatic amino acid, a neutral amino acid, or an aromatic amino acid; Xis a residue of a basic amino acid, an aliphatic amino acid, an aromatic amino acid, or a neutral amino acid; Xis a residue of an aromatic amino acid; and Xis a residue of an aliphatic amino acid, an aromatic amino acid, or a basic amino acid], or a pharmacologically acceptable salt thereof.
机译:提供一种能够通过抑制TSP1的功能来促进血管生成的化合物,并且可用于治疗或预防诸如临界肢体缺血的疾病。特异性提供的是由式(I)表示的大循环多肽[其中A选自A.从链接组ATO A; XIS脂族氨基酸的残基,芳族氨基酸,碱性氨基酸,中性氨基酸或酸性氨基酸,或不存在; Xis是芳族氨基酸或中性氨基酸的残基; XIS脂族氨基酸,芳族氨基酸或碱性氨基酸的残基; XAA4是SER,THR,ALA,ORS; xis gly或ser; XIS碱性氨基酸或中性氨基酸的残留物; Xis是中性氨基酸或酸性氨基酸的残留物; Xis是芳香氨基酸的残留物; XIS脂族氨基酸,中性氨基酸或芳族氨基酸的残余物; XIS碱性氨基酸,脂族氨基酸,芳族氨基酸或中性氨基酸的残基; Xis是芳香氨基酸的残留物;和Xis是脂族氨基酸,芳族氨基酸或碱性氨基酸的残留物,或其药理学上可接受的盐。

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