The invention relates to a Pin1
protein targeted antagonistic polypeptide, a targeted antagonistic polypeptide nano-
micelle as well as a preparation method and application of the targeted antagonistic polypeptide nano-
micelle. The Pin1
protein targeted antagonistic polypeptide comprises a targeted antagonistic polypeptide and a
cell-penetrating
peptide which are connected in sequence, the
amino acid sequence of the targeted antagonistic polypeptide comprises any one of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4 or SEQ ID NO: 5; the
amino acid sequence of the
cell-penetrating
peptide comprises SEQ ID NO: 6. The Pin1
protein targeted antagonistic polypeptide can efficiently cross
cell membranes and nuclear membranes, is specifically combined with the Pin1 protein in human metastatic pancreatic
adenocarcinoma cells, antagonizes the biological function of the Pin1 protein and kills
tumor cells. Meanwhile, the Pin1
protein targeting antagonistic polypeptide is combined with
gemcitabine, so that the sensitivity of a mixed in-situ tumor model of human metastatic pancreatic
adenocarcinoma cells and
cancer-related fibroblasts to
gemcitabine can be enhanced, the anti-
cancer effect of a single
drug is amplified, and the anti-tumor effect of 1 + 1 > 2 is generated.