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Novel ring-shape small-peptide BA and its use

A cyclic, molecular weight technology, applied in the field of biomedicine, can solve the problems of high cost, easy degradation, short half-life, etc., and achieve the effects of simple structure, strong activity and convenient artificial synthesis.

Active Publication Date: 2009-08-05
KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, peptide drugs also have certain disadvantages, such as easy degradation in the body, short half-life, high cost, etc.

Method used

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  • Novel ring-shape small-peptide BA and its use
  • Novel ring-shape small-peptide BA and its use
  • Novel ring-shape small-peptide BA and its use

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Comparison scheme
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Embodiment Construction

[0027] The substantive content of the present invention is further described below with embodiment, but content of the present invention is not limited thereto.

[0028] The amino acid sequence of the cyclic small peptide BA is:

[0029] Cys Trp Thr Lys Ser Ile Pro Pro Lys Pro Cys

[0030] 5 10

[0031] Preparation of cyclic small peptide BA and its transformation method as a template:

[0032] I. The preparation method of the cyclic small peptide BA: Synthesize its complete sequence with an automatic peptide synthesizer. Reversed phase C by HPLC 18 Column desalting and purification.

[0033] II. Molecular weight determination adopts fast atom bombardment mass spectrometry (Fast atom bombardment massspectrometry, FAB-MS), with glycerol: m-nitrobenzyl alcohol: dimethyl sulfoxide (1:1:I, V:V:V, volume ratio) as substrate, Cs + As the bombardment particles, the current is 1μA and the emission voltage is 25Kv.

[0034] III. The purity of the cyclic small ...

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Abstract

The invention relates to a cyclic small peptide BA, which belongs to the technical field of biomedicine. The cyclic small peptide BA of the present invention has a molecular weight of 1259.56 Daltons and an isoelectric point of 4.44, has certain serine protease inhibitor activity, and has no enzyme activity. Its full sequence is: Cys Trp Thr Lys Ser Ile Pro Pro Lys Pro Cys (CWTKSIPPKPC), the first cysteine ​​and the eleventh cysteine ​​form an intramolecular disulfide bond. The cyclic small peptide BA is used as a template for drug design and for the preparation of drugs for treating tumors. Using the cyclic small peptide BA as a template, different amino acids are added to its amino terminal and carbonyl terminal respectively to obtain cyclic small peptide BA1 and cyclic small peptide BA2 with antibacterial activity or serine protease inhibitor activity, and as a preparation therapy Tumor, gastritis, pancreatitis drug application. The invention also has the advantages of simple sequence, convenient synthesis and the like.

Description

Technical field: [0001] The invention provides a cyclic small peptide BA, which belongs to the technical field of biomedicine. Background technique: [0002] Serine protease and its analogues such as Kallikrein and tryptase play an important role in the occurrence of tumors, rheumatoid arthritis and many inflammations (such as rhinitis, conjunctivitis, asthma, gastroenteritis, and cardiovascular system inflammation). Clinical trials have proved that its inhibitors are effective therapeutic drugs. On the other hand, there is currently no effective drug for the treatment of herpes virus infection clinically. New research has found that inhibiting herpes virus serine protease is an effective treatment. The long-term use and abuse of "traditional antibiotics" has led to the emergence of many drug-resistant bacteria. So people began to search for new antimicrobial drugs. Studies in recent years have found that polypeptide antibiotics not only have broad-spectrum and high-effic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K7/08A61K38/08A61K38/10A61K38/16A61P35/00A61P1/04A61P1/18
Inventor 赖仞李建许李东升
Owner KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI