A specific polypeptide interfering with the binding of rac1 to pak2, pharmaceutical composition thereof and application

Abstract

A specific polypeptide interfering with the binding of Rac1 and PAK2, a pharmaceutical composition thereof and application, the amino acid sequence of the specific polypeptide is shown as SEQ ID NO:1; the polypeptide blocks the binding of Rac1 and the 81-85 amino acids (EHTIH) of PAK2 protein by competitive binding, inhibits the phosphorylation of PAK2 and the activation of downstream TGF-beta, alpha-SMA and collagen I fibrosis pathway. The application discloses a pharmaceutical composition comprising the polypeptide and application of the polypeptide in preparation of a medicine for treating diabetic kidney fibrosis. In vitro cell experiments show that the polypeptide inhibits the increase of p-PAK2 and the expression of fibrosis factors induced by high glucose in vitro; animal experiments show that the polypeptide can improve the pathological damage of the kidney of diabetic mice, reduce the expression of fibrosis-related factors, and has high specificity and long-acting property, thereby providing a new direction and method for the treatment of diabetic kidney fibrosis.

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