Polypeptide molecular probe for detecting thrombin in vivo and preparation method of polypeptide molecular probe

A technology of molecular probe and thrombin, which is applied in the field of polypeptide molecular probe for detection of thrombin in vivo and its preparation, can solve the problems of increasing patients’ suffering, insufficient timeliness, and affecting the timeliness and accuracy of detection, etc.

Inactive Publication Date: 2020-12-22
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, most of the methods commonly used at present are in vitro methods, that is, sampling from the body and then testing outside the body. Sampling from the body increases the suffering of patients, and secondly, the timeliness of detection is not enough, which also affects the quality of life to a certain extent. timeliness and accuracy of detection

Method used

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  • Polypeptide molecular probe for detecting thrombin in vivo and preparation method of polypeptide molecular probe
  • Polypeptide molecular probe for detecting thrombin in vivo and preparation method of polypeptide molecular probe
  • Polypeptide molecular probe for detecting thrombin in vivo and preparation method of polypeptide molecular probe

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Experimental program
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Embodiment 1

[0076] Embodiment 1: the preparation of the polypeptide molecular probe shown in structural formula (1)

[0077] The preparation of the polypeptide molecular probe shown in structural formula (1) comprises the following steps:

[0078] (1) Synthesis of compound A: Add resin to the reaction vessel, then add anhydrous N,N-dimethylformamide (DMF), then add leucine (Leu), valine (Val), proline Amino acid (Pro), arginine (Arg), glycine (Gly), serine (Ser), the amino group on arginine (Arg) is protected with a sulfonyl group (Pbf), and the disulfide bond uses a tert-butyl group ( tBu) protection capping, the alcoholic hydroxyl group on serine (Ser) is protected capping with t-butyl group (tBu), the molar ratio of leucine, valine, proline, arginine, glycine, serine is 1: 1:1:1:1:1, then add di-tert-butyl dicarbonate and fluorenyl methaneoxycarbonyl chloride, react, the reaction temperature is 25 ° C, the reaction time is 4 hours, the obtained main chain polypeptide sequence is Leu-V...

Embodiment 2

[0100] Embodiment 2: the preparation of the polypeptide molecular probe shown in structural formula (1)

[0101] The preparation of the polypeptide molecular probe shown in structural formula (1) comprises the following steps:

[0102] (1) Synthesis of compound A: Add resin to the reaction vessel, then add anhydrous N,N-dimethylformamide (DMF), then add leucine (Leu), valine (Val), proline Amino acid (Pro), arginine (Arg), glycine (Gly), serine (Ser), the amino group on arginine (Arg) is protected with a sulfonyl group (Pbf), and the disulfide bond uses a tert-butyl group ( tBu) protection capping, the alcoholic hydroxyl group on serine (Ser) is protected capping with t-butyl group (tBu), the molar ratio of leucine, valine, proline, arginine, glycine, serine is 1: 1:1:1:1:1, then add di-tert-butyl dicarbonate and fluorenyl methaneoxycarbonyl chloride, react, the reaction temperature is 20°C, the reaction time is 5 hours, and the main chain polypeptide sequence obtained is Leu...

Embodiment 3

[0109] Embodiment 3: the preparation of the polypeptide molecular probe shown in structural formula (1)

[0110] The preparation of the polypeptide molecular probe shown in structural formula (1) comprises the following steps:

[0111] (1) Synthesis of compound A: Add resin to the reaction vessel, then add anhydrous N,N-dimethylformamide (DMF), then add leucine (Leu), valine (Val), proline Amino acid (Pro), arginine (Arg), glycine (Gly), serine (Ser), the amino group on arginine (Arg) is protected with a sulfonyl group (Pbf), and the disulfide bond uses a tert-butyl group ( tBu) protection capping, the alcoholic hydroxyl group on serine (Ser) is protected capping with t-butyl group (tBu), the molar ratio of leucine, valine, proline, arginine, glycine, serine is 1: 1:1:1:1:1, then add di-tert-butyl dicarbonate and fluorenyl methaneoxycarbonyl chloride, react, the reaction temperature is 20°C, the reaction time is 6 hours, and the main chain polypeptide sequence obtained is Leu...

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Abstract

The invention belongs to the technical field of chemical synthesis, and discloses a polypeptide molecular probe for detecting thrombin in vivo and a preparation method of the polypeptide molecular probe. The polypeptide molecular probe comprises a structure shown in a structural formula (1) or a derivative of the structural formula (1) or a medically acceptable salt of the structural formula (1),wherein the structural formula (1) is as shown in the specification. In the process of detecting the activity of thrombin, the polypeptide molecular probe does not need to be sampled from the body ofa patient, but can be used for carrying out real-time detection in the body of the patient, so that the sampling pain of the patient is reduced, and the timeliness and accuracy of detection are also improved. The polypeptide molecular probe can detect canceration earlier, and precious time is gained for treatment of patients.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis, and particularly relates to a polypeptide molecular probe for detecting thrombin in vivo and a preparation method thereof. Background technique [0002] Thrombin is a highly specific protease-like hydrolase that exerts biological activity by binding to the thrombin receptor on the cell surface, the protease-activated receptor (PAR), and is involved in a series of physiological and pathological processes in the body. play an important role in. Thrombin not only participates in the process of hemostasis and coagulation, inflammation, immune response, tissue repair and wound healing, but also promotes tumor growth, metastasis and angiogenesis in various ways in terms of tumors. In recent years, the role of thrombin in the development of tumors has attracted increasing attention. [0003] Clinical, laboratory, histopathological and pharmacological studies in recent years have shown that ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/16C07K1/06C07K1/04A61K49/06A61B5/055
CPCA61B5/055A61K49/06C07K7/06
Inventor 张蒙张翠兰
Owner SOUTHERN MEDICAL UNIVERSITY
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