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Preparation method of polypeptide

A crude peptide and peptide resin technology, which is applied in the field of large-scale preparation of anti-tumor polypeptide ATAP-M8, can solve the problem that large-scale synthesis cannot be realized.

Active Publication Date: 2021-10-22
北京爱泰浦生物医药科技有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Due to its long amino acid sequence, active conformation α-helix and intramolecular disulfide bonds, ATAP-M8 cannot be synthesized on a large scale by conventional solid-phase synthesis methods.

Method used

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  • Preparation method of polypeptide
  • Preparation method of polypeptide
  • Preparation method of polypeptide

Examples

Experimental program
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Effect test

Embodiment 1A

[0087] Example 1 Preparation of ATAP-M8 38 peptide

[0088] 1.1 Solid-phase peptide synthesis

[0089] The sand core of the reactor is cleaned, soaked in absolute ethanol overnight, then rinsed with water until clean, and finally washed twice with absolute ethanol, and drained for use. The ambient temperature is controlled at 25±2°C, and the whole process of de-Fmoc and amino acid condensation requires high-purity nitrogen bubbling.

[0090] Resin transformation: weigh 2kg of Rink Amide AM resin (degree of substitution 0.33mmol / g), add it to a 100L polypeptide synthesis reactor, weigh 25L of DCM and add it to the reactor, so that the resin is completely immersed in the DCM solvent and swelled overnight. Deprotection of Fmoc: extract 18L of 20% (v / v) piperidine / DMF solution into a drained reaction kettle, and stir for 30min. Washing: put 18L DMF into the drained reactor, stir and drain, repeat the operation 5 times.

[0091] Condensation reaction: put 240g Fmoc-Cys(Trt)-OH (...

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Abstract

The invention relates to a method for preparing a polypeptide or a pharmaceutically acceptable salt thereof, comprising the following steps: 1) synthesizing a fully protected peptide sequence on a solid phase carrier to obtain a peptide resin; 2) cracking the peptide resin with a lysate to obtain a crude 3) using iodine oxidation method to directly carry out disulfide bond cyclization reaction on the crude peptide. The preparation method is suitable for large-scale preparation of the polypeptide, and the preparation scale can reach hundreds of grams to kilograms.

Description

technical field [0001] The invention relates to a preparation method of a polypeptide, in particular to a large-scale preparation method of an anti-tumor polypeptide ATAP-M8. Background technique [0002] ATAP-M8 is a novel amphipathic tail-anchored polypeptide derived from Bfl-1 (amino acids 147-175), which is fused to the iRGD structural sequence that is highly bound to the integrin receptor (Integrin) that is highly expressed on the surface of many tumor cells. The resulting fusion polypeptide is modified. It can effectively identify cancer cells and normal cells, directionally bring the polypeptide into the tumor cell area, specifically kill tumor cells and reduce damage to normal cells. ATAP-M8 is a brand-new polypeptide anti-cancer drug, which can specifically recognize the mitochondrial membrane of cells, and locates holes in the mitochondrial membrane through a special amphiphilic helical structure, physically destroying the mitochondrial structure and inducing apop...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K19/00C07K1/04C07K1/06
CPCC07K14/00C07K14/70546C07K2319/00Y02P20/55
Inventor 刘河郭晓春杨惠仁麻建杰郭二明王兴辉
Owner 北京爱泰浦生物医药科技有限责任公司
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