Use and modification method of modified peptide in preparation of drug for inhibiting insulin secretion from pancreatic islets

Abstract

The invention belongs to the technical field of peptide modification, and discloses the use and modification method of a modified peptide in the preparation of a drug for inhibiting insulin secretion from pancreatic islets. The selective blocking of COX 52‑69 the end of; for closed COX 52‑69 N-terminal acetylation and C-terminal amidation modification; methylation modification on the amide bond between valine and leucine, and addition of cysteine ​​at both ends of the polypeptide, and make it through two The sulfur bonds connect into rings, forming a rigid molecule. The present invention transforms the original linear polypeptide into a circular polypeptide COX 52‑69 , so that in the past, only the way of injection can be changed to oral administration, and it also has the function of inhibiting glucose-induced insulin secretion. Modified cyclic peptides, realizing oral administration route, and more linear peptide COX 52‑69 It has the same function of inhibiting insulin secretion from pancreatic islets. The oral administration route of the polypeptide is realized.

Description

technical field [0001] The invention belongs to the technical field of peptide modification, and in particular relates to the use and modification method of a modified peptide in the preparation of a drug for inhibiting insulin secretion from pancreatic islets. Background technique [0002] Currently, the short peptide COX 52-69 It is a polypeptide containing 18 amino acids. It was originally isolated and purified from the small intestine of pigs. After the amino acid sequence alignment, it was found that it completely overlapped with the 52nd to 69th of cytochrome oxidase VIII, so it was named COX 52-69 . Its sequence is LLPAGWVLSHLDSYKKRE. COX obtained by biochemical separation and purification 52-69 The functional experiment of the polypeptide found that the polypeptide can inhibit the secretion of insulin caused by glucose. This discovery has applied for a Chinese invention patent on October 11, 2013, and the application number is 201310471571.9. Afterwards, the shor...

AI Technical Summary

Problems solved by technology

[0004] (1) Linear peptide COX synthesized by solid-phase synthesis 52-69 Inability to function by oral administration;

[0005] (2) There is no linear peptide COX in the prior art 52-69 Methods for modifying the molecular structure that affect COX 52-69 Applications

[0009] Due to their instability and low bioavailability, peptide drugs are mostly administered by injection, which brings great pain to patients

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