Radionuclide < 99m > Tc labeled LncRNA HOTAIR targeting probe, preparation method and developer

A radionuclide and targeting technology, which is applied in the preparation of radioactive preparations, radioactive carriers, and sugar derivatives in vivo, can solve the problems of inability to timely and accurately reflect cancer detection results, and inability to realize tumor cell gene detection.

Pending Publication Date: 2021-06-08
GENERAL HOSPITAL OF NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Since the formation of a tumor is a complex process involving multiple factors, which is related to multiple gene mutations, chromosomal translocations, deletions, and amplifications, when using the technical solutions provided by the prior art, the inventors found that the prior art cannot achieve The genetic detection of tumor cells, but only through the variation of body anatomy, cannot reflect the detection results of cancer in a timely and accurate manner

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  • Radionuclide &lt; 99m &gt; Tc labeled LncRNA HOTAIR targeting probe, preparation method and developer
  • Radionuclide &lt; 99m &gt; Tc labeled LncRNA HOTAIR targeting probe, preparation method and developer
  • Radionuclide &lt; 99m &gt; Tc labeled LncRNA HOTAIR targeting probe, preparation method and developer

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Embodiment 1

[0047] Embodiments of the present invention provide a radionuclide 99m Tc-labeled LncRNA HOTAIR targeting probe, the antisense oligonucleotide sequence of the targeting probe is sequence 1, and the synthetic structure of the targeting probe is 5'-ASON-(CH2)6-NH2-3', refer to figure 1 shown;

[0048] Wherein, the two ends of the sequence 1 are respectively modified with 2′ methylation, and the two ends of the sequence 2 are respectively modified with two bases thiolation;

[0049] A primary amine structure is connected to the 3' end, and (CH2)6 is used as a linker between NH2 in the primary amine structure and the backbone of sequence 1.

Embodiment 2

[0051] Embodiments of the present invention provide a radionuclide 99m Tc-labeled LncRNA HOTAIR targeting probe, the targeting probe at least includes a basic structure and a labeling structure, the antisense oligonucleotide sequence of the basic structure is sequence 1, and the synthetic structure of the targeting probe is 5'-ASON-( CH2)6-NH2-3', the labeled radionuclide of the labeled structure is 99m Tc;

[0052] Wherein, the two ends of the sequence 1 are respectively modified with 2′ methylation, and the two ends of the sequence 2 are respectively modified with two bases thiolation;

[0053] A primary amine structure is connected to the 3' end, and (CH2)6 is used as a linker between NH2 in the primary amine structure and the backbone of sequence 1.

[0054] Optionally, the radionuclide is attached to the synthetic structure via the bifunctional chelator HYNIC;

[0055] The synthetic structure of the targeting probe is 99m Tc-HYNIC-ASON.

[0056] LncRNA HOTAIR Targeti...

Embodiment 3

[0071] Embodiments of the present invention provide a radionuclide 99m The preparation method of the Tc-labeled LncRNA HOTAIR targeting probe, the method comprises:

[0072] Step 1: Mix targeted probe A and HYNIC solution, and place in the dark for 1 hour;

[0073] Step 2: Collect the mixed solution of targeting probe A and HYNIC solution by centrifugation to obtain chelating agent-linked targeting probe A; wherein, the synthetic structure of targeting probe A is 5'-ASON-(CH2)6-NH2 -3';

[0074] Step 3: Add radionuclide, stannous chloride dihydrate solution and Tricnie solution to the targeting probe A connected with the chelating agent in sequence, and react for 30 minutes;

[0075] Step 4: After the reaction solution is purified with Sephadex G25, the reaction product is collected, and the peak tube of the reaction product is the radionuclide-labeled targeting probe B.

[0076] Optionally, the radionuclide is 99m Tc, the synthetic structure of targeting probe B is 99m T...

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Abstract

The invention discloses a radionuclide < 99m > Tc labeled LncRNAHOTAIR targeting probe, a preparation method and a developer, and belongs to the technical field of nuclide labeling and molecular imaging. An antisense oligonucleotide sequence of the targeting probe is a sequence 1, and a synthetic structure of the targeting probe is 5 '-ASON-(CH2)6-NH2-3'; wherein two ends of the sequence 1 are respectively modified by 2'methylation, and two ends of sequence 2 are respectively modified by two basic group sulfo groups; a primary amine structure is connected to 3'end of the sequence 1, and (CH2)6 is used as a linker between NH2 in the primary amine structure and a skeleton of the sequence 1. As ASON can be efficiently, specifically and irreversibly complementarily combined with a target, the LncRNAHOTAIR targeting probe can promptly and accurately reflect cancer detection results.

Description

technical field [0001] The invention relates to the technical field of nuclide labeling and molecular imaging, in particular to a radionuclide 99m Tc-labeled LncRNA HOTAIR targeting probe, preparation method and imaging agent. Background technique [0002] Early diagnosis and treatment of malignant tumors is one of the important issues to be solved urgently. Early detection of cancer can lead to early treatment of cancer and reduce cancer mortality. [0003] Existing technologies mainly use traditional imaging equipment, such as MRI, CT, and ultrasound, to detect variations in body anatomy, thereby achieving early detection of cancer; [0004] Since the formation of a tumor is a complex process involving multiple factors, which is related to multiple gene mutations, chromosomal translocations, deletions, and amplifications, when using the technical solutions provided by the prior art, the inventors found that the prior art cannot achieve The genetic detection of tumor cell...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H23/00C07H1/00A61K51/04A61K103/10
CPCC07H23/00C07H1/00A61K51/0482A61K51/0491C07B2200/05
Inventor 赵倩任炯羽张福禄冯薛烟于亚萍王蓉
Owner GENERAL HOSPITAL OF NINGXIA MEDICAL UNIV
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