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A molecular imaging probe and its application

A molecular imaging and probe technology, applied in molecular imaging probes and its application fields, can solve the problems of difficult and precise resection of tumor tissue, decreased tumor sensitivity, complex detection methods of kits, etc., to improve postoperative quality of life and enhance Imaging sensitivity, the effect of real-time high-sensitivity imaging

Active Publication Date: 2021-02-09
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, surgical resection of tumor is the main method, and the bladder tissue is removed as a whole, and the quality of life of patients after surgery is severely reduced; partial resection or minimally invasive surgery, some small lesions are difficult to find, and there are situations such as missed cuts and multiple cuts.
The specificity and sensitivity of existing preoperative diagnostic techniques such as B-ultrasound, CT, and MRI need to be improved: for tumors < 8mm, the sensitivity decreases, and it is difficult to image at the molecular level, and can only provide preoperative diagnosis, and cannot achieve surgical diagnosis. real-time imaging navigation
Surgical resection for bladder cancer patients, whether it is open or minimally invasive surgery, depends on the results of preoperative diagnosis. The operation is highly dependent on the doctor's experience, and it is difficult to accurately remove tumor tissue, especially invasive tumors. For small lesions It is even more difficult to find, which leads to a high recurrence rate after surgery.
CN103361403A discloses a kit for detecting bladder cancer-related risk genes. The kit includes a pair of specific primers and a specific fluorescent probe for simultaneously detecting the SNP site rs9642880 on the MYC gene and the SNP site rs2294008 on the PSCA gene. Aiming at conventional components used for fluorescent quantitative PCR detection, the invention assesses the risk of individuals suffering from bladder cancer by simultaneously detecting the genotypes of single nucleotide polymorphisms with MYC and PSCA, but the kit detects Complicated means, unable to achieve tumor localization and imaging

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  • A molecular imaging probe and its application
  • A molecular imaging probe and its application
  • A molecular imaging probe and its application

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Example 1 Preparation of Molecular Imaging Probes

[0041] In this example, molecular imaging probes were prepared by the following methods:

[0042] The molecular imaging probe uses RGD as the specific targeting recognition part, uses GPAKLVFFCT as the response assembly retention part, and the side chain near-infrared fluorescent dye molecule is IR783. The molecular structure is shown in formula I. The synthesis and preparation steps are as follows:

[0043] (1) Adopt the Fmoc solid-phase synthesis method, select the modified density of Wang resin as 0.35mM, synthesize the polypeptide on the resin, remove the Fmoc protection of the amino terminal with the DMF solution of hexahydropyridine, and use the carboxyl group of the next amino acid with 4 -Methylmorpholine and benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate in DMF for activation, followed by condensation with the deprotected first amino acid, repeated The above steps until the condensation of all...

Embodiment 2

[0047] Example 2 Preparation of Molecular Imaging Probes

[0048] In this example, molecular imaging probes were prepared by the following methods:

[0049] The molecular imaging probe uses RGD as the specific targeting recognition part, and uses GPVKLVFFCT as the response assembly retention part. The side chain near-infrared fluorescent dye molecule is IR783. The molecular structure is shown in formula I. The synthesis and preparation steps are as follows:

[0050] (1) Adopt the Fmoc solid-phase synthesis method, select the modified density of Wang resin as 0.35mM, synthesize the polypeptide on the resin, remove the Fmoc protection of the amino terminal with the DMF solution of hexahydropyridine, and use the carboxyl group of the next amino acid with 4 -Methylmorpholine and benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate in DMF for activation, followed by condensation with the deprotected first amino acid, repeated The above steps until the condensation of all...

Embodiment 3

[0054] Example 3 Preparation of Molecular Imaging Probes

[0055] In this example, molecular imaging probes were prepared by the following methods:

[0056] The molecular imaging probe uses RGD as the specific targeting recognition part, uses GPLKLVFFCT as the response assembly retention part, and the side chain near-infrared fluorescent dye molecule is IR783. The molecular structure is shown in formula I. The synthesis and preparation steps are as follows:

[0057] (1) Adopt the Fmoc solid-phase synthesis method, select the modified density of Wang resin as 0.35mM, synthesize the polypeptide on the resin, remove the Fmoc protection of the amino terminal with the DMF solution of hexahydropyridine, and use the carboxyl group of the next amino acid with 4 -Methylmorpholine and benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate in DMF for activation, followed by condensation with the deprotected first amino acid, repeated The above steps until the condensation of all...

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Abstract

The present invention provides a molecular imaging probe, which is a polypeptide molecule, including a specific targeting part at one end, a response assembly retaining part in the middle and a chromogenic part of the side chain; wherein, the The response assembly retention part includes a response sequence and an assembly sequence, the response sequence is SEQ ID NO.1, the assembly sequence is SEQ ID NO.2, and the molecular imaging probe recognizes tumor cells through a specific targeting part, through "Assembly retention effect" assembles and stays in the tumor microenvironment to achieve high-quantity and long-term imaging in tumor tissue. Through near-infrared light excitation, stable and long-term intraoperative imaging and navigation at tumor lesions can be achieved, and tumor positioning can be visualized, improving The accuracy of tumor resection greatly improves the success rate of surgery, reduces the recurrence rate after surgery, and improves the quality of life of patients after surgery.

Description

technical field [0001] The invention relates to the technical field of molecular imaging, in particular to a molecular imaging probe and its application. Background technique [0002] Molecular imaging is a science that uses imaging methods to display specific molecules at the tissue level, cells and subcellular levels, reflects the changes at the molecular level in the living state, and conducts qualitative and quantitative research on its biological behavior in imaging. Therefore, molecular imaging is the product of the combination of molecular biology technology and modern medical imaging, while classic imaging diagnosis (X-ray, CT, MR, ultrasound, etc.) mainly shows the final effect of some molecular changes, with anatomical diseases with anatomical changes; and molecular imaging, through the development of new tools, reagents and methods, to detect abnormalities at the cellular and molecular levels during the disease process, to detect abnormalities before diseases with...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K19/00C07K7/06C09K11/06A61K49/00
CPCA61K49/0021A61K49/0056C07K7/06C07K2319/33C09K11/06C09K2211/1007C09K2211/1029C09K2211/1088
Inventor 王浩李莉莉
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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