Preparation method of polypeptide

A technology of crude peptide and peptide resin, which is applied in the field of large-scale preparation of anti-tumor polypeptide ATAP-M8, can solve the problems of inability to realize large-scale synthesis, achieve the effect of avoiding oxidation and improving product purity

Active Publication Date: 2018-07-31
北京爱泰浦生物医药科技有限责任公司
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Problems solved by technology

[0006] Due to its long amino acid sequence, active conformation α-helix and intramolecular disulfide

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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Example Embodiment

[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 polypeptide or pharmaceutically acceptable salts. The method comprises the following steps of 1, synthesizing a full-protection peptide sequence on a solid phase carrier, and obtaining peptide resin; 2, adopting a lysate for pyrolyzing the peptide resin, and obtaining crude peptide; 3, adopting an iodine oxidation method for directly performing a disulfide bond cyclization reaction on the crude peptide. The preparation method is applicable to preparing the polypeptide in large scale, and the preparation scale can reach the hectogram scale to thekilogram scale.

Description

technical field [0001] The invention relates to a preparation method of polypeptide, in particular to a large-scale preparation method of anti-tumor polypeptide ATAP-M8. Background technique [0002] ATAP-M8 is a novel amphipathic tail-anchor polypeptide derived from Bfl-1 (amino acid 147-175), which is fused with the iRGD structural sequence that is highly expressed on the surface of many tumor cells and highly binds to the integrin receptor (Integrin). Modified fusion polypeptide. It can effectively identify cancer cells and normal cells, direct the peptide into the tumor cell area, specifically kill tumor cells and reduce damage to normal cells. ATAP-M8 is a brand-new polypeptide anticancer drug, which can specifically recognize the mitochondrial membrane of cells, locate holes in the mitochondrial membrane through a special amphipathic helical structure, physically destroy the mitochondrial structure, and induce cell apoptosis. [0003] ATAP-M8 contains 38 amino acid r...

Claims

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Application Information

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IPC IPC(8): C07K19/00C07K1/04C07K1/06
CPCC07K14/00C07K14/70546C07K2319/00Y02P20/55
Inventor 史卫国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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