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Solid phase synthesis method for thymosin beta 4

A solid-phase synthesis, thymosin technology, applied in the field of biochemistry, can solve the problems of difficulty in purification, affecting the condensation rate of amino acids, increasing the probability of amino acid racemization, etc., achieving the effects of less impurities, shortening synthesis time, and easy separation and purification.

Inactive Publication Date: 2009-04-22
ADLAI NORTYE BIOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for long-chain peptides with more than 30 amino acids, solid-phase linking of amino acids one by one will encounter some serious problems. After the peptide reaches a certain length and conditions, it will generate folds or sheets on the solid-phase resin carrier. In the secondary structure, the peptide chains are cross-linked or polymerized, so that the active amino sites are hidden or buried, which increases the steric hindrance and greatly affects the condensation rate of amino acids. The probability of spinning is correspondingly greatly increased, which makes the product more impurity and extremely difficult to purify

Method used

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  • Solid phase synthesis method for thymosin beta 4
  • Solid phase synthesis method for thymosin beta 4

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: the preparation of Fmoc-Ser (tBu)-king resin

[0042] Operation: (1) Put 12.5g (5mmol) of King Resin (Tianjin Nankai Hecheng Technology Co., Ltd.) in a peptide synthesis reactor, wash with N,N-dimethylformamide (DMF), add DMF to swell for 30min Afterwards, 3.8g of Fmoc-Ser(tBu)-OH was dissolved in 50ml of DMF and added to the reactor, 3.2ml of pyridine was added, and 2.8ml of 2,6-dichlorobenzoyl chloride was added dropwise. After the dropwise addition, the reaction was carried out at room temperature After 2 hours, wash three times with DMF, once with methanol, three times with dichloromethane, three times with methanol, and dry to obtain 14.3 g of Fmoc-Ser(tBu)-King resin.

Embodiment 2

[0043] Example 2: Fmoc-Thr(tBu)-Ile-Glu(OtBu)-Gln(Trt)-Glu(OtBu)-Lys(Boc)-Gln(Trt)-Ala-Gly-Glu(OtBu)-Ser(tBu )-Wang resin (A peptide fully protected resin) preparation

[0044] Operation: (1) Put 14.3g of Fmoc-Ser(tBu)-King resin in the polypeptide synthesis reactor, wash with 80ml of dichloromethane and methanol for 2 times alternately, 2 minutes each time, and drain. Add 80 ml of 20% piperidine / DMF solution, stir at room temperature for 20 minutes, and drain. The resin was alternately washed 3 times with 80 ml of dichloromethane and methanol for 2 minutes each time, and then drained.

[0045] (2) 8.0 g of Fmoc protected amino acids and O-benzotriazole-N, N, N', N'-tetramethyluronium tetrafluoroborate (TBTU, Shanghai Yanchang Biochemical Technology Development Co., Ltd.) were used in 50 ml After the DMF solution was dissolved, 4.4 ml of N,N-diisopropylethylamine was added, mixed evenly, added to the resin, and stirred at room temperature for 3 hours.

[0046] (3) Drain. T...

Embodiment 3

[0051] Embodiment 3: Preparation of Fmoc-Glu(OtBu)-2-chlororityl chloride resin

[0052]Operation: 100g (120mmol) of 2-chlororityl chloride resin was added to a 1000ml solid-phase synthesis reactor, 204g of Fmoc-Glu(OtBu)-OH was dissolved in 600ml of dichloromethane, and N,N-diisopropylethylamine ( DIEA) 167ml, stirred and mixed evenly, added to the solid-phase synthesis reactor, and reacted at room temperature for 1 hour. Drain. The resin was alternately washed 3 times with 800 ml of dichloromethane and methanol, 2 minutes each time, and then drained. 143.7 g of Fmoc-Glu(OtBu)-2-chlorotrityl chloride resin was obtained.

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Abstract

The invention relates to a solid phase synthesis method for extrasin beta4. A large long chain peptide is decomposed into a plurality of parts of small short chain peptides; short peptide chain fragments with full protection side chains are obtained through the synthesis; and then various short peptide chain fragment units are assembled to obtain a final long peptide product. The method has the advantages that the method avoids the crosslinking polymerization problem of a long peptide generated in the synthesis process; in addition, a plurality of short peptide fragments can be synchronously synthesized in parallel, which greatly shortens the total synthesis time; moreover, short peptides can obtain an intermediate product with higher relative purity, thereby ensuring that the final product has relatively fewer impurities and the impurities are easy to separate and purify.

Description

technical field [0001] The invention belongs to the technical field of biochemistry, and relates to a solid phase synthesis method of thymosin β4. Background technique [0002] Thymosin β4 chemical name: N-acetyl-seryl-aspartyl-lysyl-prolyl-aspartyl-methionyl-alanyl-glutamyl-isoleucyl- Glutamyl-Lysyl-Phenylalanyl-Aspartyl-Lysyl-Seryl-Lysyl-Leucyl-Lysyl-Lysyl-Threonyl-Glutamyl- Threonyl-Glutamyl-Glutamyl-Lysyl-Asparaginyl-Prolyl-Leucyl-Prolyl-Seryl-Lysyl-Glutamyl-Threonyl - Isoleucyl-Glutamyl-Glutamyl-Glutamyl-Lysyl-Glutamyl-Alanyl-Glycyl-Glutamyl-Serine. [0003] The sequence of the peptide is: [0004] Ac-Ser-Asp-Lys-Pro-Asp-Met-Ala-Glu-Ile-Glu-Lys-Phe-Asp-Lys-Ser-Lys-Leu-Lys-Lys-Thr-Glu-Thr-Gln-Glu- Lys-Asn-Pro-Leu-Pro-Ser-Lys-Glu-Thr-Ile-Glu-Gln-Glu-Lys-Gln-Ala-Gly-Glu-Ser-OH [0005] Molecular formula: C 212 h 350 N 56 o 78 S [0006] Molecular weight: 4963.49 [0007] Thymosin-β4 is the hidden protein of actin, which acts as the power source of actin depolyme...

Claims

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Application Information

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IPC IPC(8): C07K14/66C07K14/47C07K1/04
CPCY02P20/55
Inventor 赵德中李新宇
Owner ADLAI NORTYE BIOPHARMA CO LTD
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