Polypeptide and its use as a CCK receptor agonist/antagonist
AssigneesCentre for Regenerative Medicine & Health, Hong Kong Institute of Science & Innovation, Chinese, City University of Hong Kong
InventorsMickey Daniel Tortorella, Jufang He
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Abstract
The present invention relates to the field of chemical and pharmaceutical technologies, in particular to a polypeptide and its use as a CCK receptor agonist/antagonist. Experiments show that the polypeptide provided by the present invention has a high agonistic/antagonistic activity on CCK receptors. Compared with the polypeptide CCK4, the polypeptide according to the present invention has a longer half-life and duration of efficacy in vivo. Experiments show that the polypeptide according to the present invention produces a significant improvement on the spatial memory deficiency of senile mice, memory-deficient senile mice, and Alzheimer's mice, and thus has a great application potential.
Claims10
A polypeptide having a structure shown in Formula I or its stereoisomer, prodrug, pharmaceutically acceptable solvate or salt:
- wherein:
- X is an amide bond or a single bond;
- is or , so that the amino acid at the corresponding position is a D-type or L-type amino acid;
- R1, R2, R3 and R4 are independently selected from the group consisting of the following structures:
- and RI, RII, RIII and RIV are independently selected from the group consisting of halogen, nitro, C1-C4 alkyl, azido and cyano;
- R5 and R6 are independently selected from the group consisting of H, and substituted or unsubstituted C1-C4 alkyl;
- R7 is selected from the group consisting of the following structures:
- Biotin, AC, Fmoc, Cbz, PEG100, PEG200, PEG300, PEG400, PEG600, PEG800, PEG1000, PEG1500, PEG2000,
- provided that the polypeptide is not
Dependencies are inferred from the claim text.