Radioactive metal element labeled micromolecular cyclopeptide, composition and application of micromolecular cyclopeptide

A metal element and radioactive technology, applied in the field of medicine, can solve the problems of lack of clinical application prospects, short fluorescence imaging distance, poor tissue penetration, etc., and achieve the effect of good tissue penetration, fast blood clearance, and high intake

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] Using Cy5.5 for cyclic peptide c(KAHWGFTLD)NH 2 Carry out labeling, and use the markers to perform optical imaging on various living tumor models, but the fluorescent imaging distance of the markers is short, the tissue penetration is poor, the sensitivity is not high, and it is difficult to localize the expression in deep tissues, so it can only be used as a simple animal model Basic research, lack of clinical application prospects

Method used

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  • Radioactive metal element labeled micromolecular cyclopeptide, composition and application of micromolecular cyclopeptide
  • Radioactive metal element labeled micromolecular cyclopeptide, composition and application of micromolecular cyclopeptide
  • Radioactive metal element labeled micromolecular cyclopeptide, composition and application of micromolecular cyclopeptide

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Embodiment Construction

[0039] The radioactive metal element-labeled small molecule cyclic peptide, the composition containing the small molecule cyclic peptide and the application of the present invention will be described in detail below with reference to the accompanying drawings.

[0040]

[0041] Select c(KAHWGFTLD)NH 2 (i.e. C6) as a small molecule cyclic peptide, NOTA is a chelating ligand, 68 Ga is labeled as a radioactive metal element.

[0042] 1.c(KAHWGFTLD)NH 2 -NOTA- 68 Ga (C6-NOTA- 68 Ga) Preparation

[0043] Step 1: To c(KAHWGFTLD)NH 2 -NOTA (C6-NOTA) was dissolved in sterile water for injection to prepare a 1mg / ml solution;

[0044] Step 2: Take 20 μl of the C6-NOTA solution obtained in Step 1, add 100 μl of 2-[4-(2-hydroxyethyl)-1-piperazine]ethanesulfonic acid buffer and 500 μl of freshly rinsed 68 Ga (1.5mCi), react at 100°C for 15min;

[0045] Step 3: Add 15ml of water to dilute, pass through the C18 column, rinse C18 with 10ml of water for injection to remove impurities...

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Abstract

The invention provides a radioactive metal element labeled micromolecular cyclopeptide. The radioactive metal element labeled micromolecular cyclopeptide is characterized by being a compound as shown in a formula (I), namely c(X1HWGFTLX2) -Y-Z(I), wherein c(X1HWGFTLX2) is a cyclopeptide formed by binding 8-10 amino acids; each of X1 and X2 is at least one amino acid group; Y is a chelating ligand; Z is 68Ga and is chelated with Y; the cyclopeptide contains a free amino acid which is matched with Y. The invention also provides a composition containing the micromolecular cyclopeptide and the application of the micromolecular cyclopeptide as a tumor developer. The micromolecular cyclopeptide c(X1HWGFTLX2) -Y-Z(I) is small in molecular weight, quick in blood clarification, high in tissue intake, good in penetrability, high in sensitivity, simple in radiochemical synthesis process and good clinical application prospect; as a result, good basis can be provided for the subsequent research or the clinical diagnosis of medical workers.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a small molecule cyclic peptide labeled with a radioactive metal element, a composition containing the small molecule cyclic peptide and an application of the small molecule 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 resea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/56A61K51/08A61K103/00
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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