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Polypeptide with tumor vessel targeting, molecular probe and preparation method and application of polypeptide and molecular probe

A technology of tumor blood vessels and molecular probes, applied in the direction of in vivo radioactive preparations, preparations for in vivo experiments, and pharmaceutical formulations, can solve problems such as difficult metabolism, achieve enhanced hydrophilicity, overcome easy metabolism, and reduce steric hindrance Effect

Active Publication Date: 2017-11-03
WUXI PEOPLES HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In view of this, the purpose of the present invention is to provide a polypeptide with tumor blood vessel targeting, which can obviously solve the problem of difficult metabolism in vivo, and at the same time facilitate nuclide labeling, and has the effect of obviously improving the pharmacokinetic performance of molecular probes in vivo. features

Method used

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  • Polypeptide with tumor vessel targeting, molecular probe and preparation method and application of polypeptide and molecular probe
  • Polypeptide with tumor vessel targeting, molecular probe and preparation method and application of polypeptide and molecular probe
  • Polypeptide with tumor vessel targeting, molecular probe and preparation method and application of polypeptide and molecular probe

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preparation example Construction

[0056] The present invention also provides a preparation method of the single photon or positron molecular probe, comprising the following steps:

[0057] 1) Mixing the bifunctional chelating agent solution and the polypeptide solution at a molar ratio of 1 to 10:1 and then performing a chelation reaction to obtain a labeling precursor solution;

[0058] 2) Mix the labeled precursor solution obtained in step 1) with the nuclide solution for single-photon imaging or the nuclide solution for positron imaging according to a molar ratio of (10-1.1): 1 to perform a chelation reaction to obtain a single-photon imaging nuclide solution. or positron molecular probes.

[0059] In the invention, the bifunctional chelating agent solution and the polypeptide solution are mixed according to the molar ratio of 1-10:1, and then the chelating reaction is carried out to obtain the labeling precursor solution.

[0060] In the present invention, the buffer solution of the bifunctional chelating...

Embodiment 1

[0077] The single-photon tracer described in this example uses the bifunctional chelating agent p-SCN-Bn-DTPA as a linker to carry out single-photon nuclide detection of a polypeptide compound with the amino acid sequence GGGRDNIFLLWQR (GR13). 99 Tc m Marking, the specific steps include:

[0078] 1) Preparation of labeled precursor p-SCN-Bn-DTPA-GR13:

[0079] Dissolve 3.00mg GR13 and 1.02mg p-SCN-Bn-DTPA (molar ratio 1:1.2) in 1mL DMF, and stir in a water bath at 37°C overnight after nitrogen sealing.

[0080] The reacted mixed solution was eluted by preparative HPLC gradient, the conditions are as follows:

[0081] Preparative reversed-phase C18 column (Xbridge, 19×150mm, Waters);

[0082] Waters 2998 diode array UV detector;

[0083] BioScan radioactivity detector;

[0084] Waters2545 binary high pressure gradient pump;

[0085] The mobile phase is: A, an acetonitrile solution containing 0.1% trifluoroacetic acid (TFA); B, an aqueous solution containing 0.1% TFA;

[...

Embodiment 2

[0113] The PET tracer described in this example uses the bifunctional chelating agent p-SCN-Bn-NODA as a linker to conduct positron nuclides on a polypeptide compound with the amino acid sequence GGGRDNIFLLWQR (GR13). 18 F mark, the specific steps include:

[0114] 1) Preparation of labeled precursor p-SCN-Bn-NODA-GR13: Dissolve 4mg GR13 and 0.6mg p-SCN-Bn-NODA (molar ratio 1:1.2) in 1mL DMF, and stir overnight in a water bath at 37°C after nitrogen sealing . After the reaction, use preparative HPLC to purify, the conditions are as follows:

[0115] Preparative reversed-phase C18 column (Xbridge, 19×150mm, Waters);

[0116] Waters 2998 diode array UV detector;

[0117] BioScan radioactivity detector;

[0118] Waters2545 binary high pressure gradient pump;

[0119] The mobile phase is: A, an acetonitrile solution containing 0.1% trifluoroacetic acid (TFA); B, an aqueous solution containing 0.1% TFA;

[0120] Gradient elution: 5% A and 95% B in 0-2 minutes increased to 65%...

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Abstract

The invention provides a polypeptide with tumor vessel targeting, a molecular probe and a preparation method and application of the polypeptide and the molecular probe, and belongs to the technical field of diagnostic imaging agents. The polypeptide has an amino acid sequence as shown in a sequence table Seq ID No. 1. The single-photon or positive-electron molecular probe has a structure as shown in X-N-G, wherein X is a single-photon developing nuclide or a positive-electron developing nuclide; N is a dual-functional chelating agent; and G is the polypeptide. The fluorescent molecular probe has a structure as shown in X-G, wherein X is fluorescent nuclide; and G is the polypeptide. By the modified polypeptide, the abdomen background can be reduced obviously, and the picture contrast is improved. The obtained molecular probe is simple to prepare, low in price and high in target-to-nontarget ratio.

Description

technical field [0001] The invention belongs to the technical field of diagnostic imaging agents, and specifically relates to a polypeptide with tumor blood vessel targeting, a molecular probe, a preparation method and application thereof. Background technique [0002] Cancer is a disease that seriously threatens human health. Early diagnosis and treatment of cancer can reduce the pain, mental and economic burden of patients, and strive for an early recovery of cancer patients. At present, most targeted drugs used for diagnosis and treatment are monoclonal fragments, which have poor tumor penetration ability and cannot be specifically captured by the monocyte-macrophage system. Peptides have small amount, low immunogenicity, good tissue penetration ability and high affinity for tumor tissue. The research of targeted drugs has always been a hot spot in tumor diagnosis and treatment. [0003] In 1971, Folkman first proposed that tumor growth is dependent on blood vessels. Tum...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61K49/00
CPCA61K49/0056A61K51/088
Inventor 朱宝陈飞蒋孟军邵科晶肖翼春王俊超浦晓佳徐新
Owner WUXI PEOPLES HOSPITAL
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