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Radioactive halogen marked micromolecule cyclic peptide, composition and application of radioactive halogen marked micromolecule cyclic peptide

A radioactive, small molecule technology, applied in the field of medicine, can solve the problems of difficult deep tissue localization and expression, lack of clinical application prospects, short fluorescence imaging distance, etc., and achieve high thermodynamic and dynamic stability, strong penetrability, good The effect of visualization

Inactive Publication Date: 2015-09-30
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There are currently research reports [3,4] The cyclic peptide c(KAHWGFTLD) NH2 was labeled with Cy5.5, and a variety of living tumor models were optically imaged with the marker, but the fluorescence imaging distance of the marker was short, the tissue penetration was poor, and the sensitivity was not high, so it was difficult to detect Localized expression in deep tissues can only be used as a simple animal model for basic research, lacking clinical application prospects

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  • Radioactive halogen marked micromolecule cyclic peptide, composition and application of radioactive halogen marked micromolecule cyclic peptide
  • Radioactive halogen marked micromolecule cyclic peptide, composition and application of radioactive halogen marked micromolecule cyclic peptide
  • Radioactive halogen marked micromolecule cyclic peptide, composition and application of radioactive halogen marked micromolecule cyclic peptide

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Embodiment Construction

[0031] The radioactive halogen-labeled small molecule cyclic peptides, compositions and applications of the present invention will be further described in conjunction with the accompanying drawings.

[0032]

[0033] In this example, the selected chelating ligand is NOTA, and the metal complex containing radioactive halogen is Al 18 F complex, the small molecule cyclic peptide is c(KAHWGFTLD)NH2, which is C6. In this example, c(KAHWGFTLD)NH-NOTA (C6-NOTA) was selected for labeling. C6-NOTA was synthesized by Hangzhou Zhongpei Biochemical Co., Ltd. by solid-phase synthesis.

[0034] 1. C6-NOTA-Al- 18 Preparation of F

[0035] Step 1: Using Nuclear Reactions on a Cyclotron 18 O(P,n) 18 F made [ 18 F]F - ;

[0036] Step 2: Add sterilized water for injection to C6-NOTA to dissolve, and prepare a 1 mg / ml solution;

[0037] Step 3: Take 30 μl of C6-NOTA sterile aqueous solution for injection, add 400 μl of acetonitrile, 6 μl of 2 mmol / L aluminum chloride aqueous solution, ...

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Abstract

The invention provides a radioactive halogen marked micromolecule cyclic peptide, which is characterized in that the micromolecule cyclic peptide is a chemical as shown in the formula (I): c(X1HWGFTLX2)-Y-Z (I), in the formula, c(X1HWGFTLX2) is a cyclic peptide formed by 8-10 combined amino acids, X1 and X2 are both at least one amino acid residue, Y is chelated ligand, Z is a metal compound containing radioactive halogen which is chelated with Y. The invention further provides a compound containing the micromolecule cyclic peptide, and application of the micromolecule cyclic peptide as a tumor developing agent. The radioactive halogen marked micromolecule cyclic peptide provided by the invention not only can be targeted to tumor cells, but also is high in permeability, can perform positioning expression on deep tissue, and is relatively good in clinical application prospect, and relatively good basis for later research or diagnosis on tumor can be provided for medical operators.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a radioactive halogen-labeled small molecular cyclic peptide, a composition containing the small molecular cyclic peptide and the application of the small molecular cyclic peptide as a tumor imaging agent. Background technique [0002] Tumor invasion and metastasis seriously affect the prognosis of patients, how to make an early diagnosis is a key clinical problem to be solved urgently. [0003] Matrix metalloproteinases (MMPs) are a group of Zn-containing + The most important class of proteases involved in the degradation of extracellular matrix (extra-cellular matrix, ECM). Because MMPs can decompose the basement membrane and extracellular matrix, causing tumor invasion and metastasis, and MMPs can also regulate many components in the tumor microenvironment, thereby promoting the occurrence and development of tumors. [1] Therefore, it is a hotspot in current research to pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64A61K51/08A61K101/02
Inventor 刘庆华杨敏张大志程超潘栋辉左长京张桉榆王立振徐宇平杨润琳陈飞
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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