Tumor molecular probe for targeting cervical cancer and application thereof

A molecular probe and tumor technology, applied in the field of biomedicine, can solve the problems of drug treatment failure and tumor resistance, and achieve the effects of high radioactive specific activity, high labeling rate, and high radiochemical purity

Active Publication Date: 2021-06-22
PEKING UNIV FIRST HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, a large number of basic and clinical studies suggest that using single-target drugs as a treatment plan may cause drug resistance in tumors, resulting in drug treatment failure.

Method used

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  • Tumor molecular probe for targeting cervical cancer and application thereof
  • Tumor molecular probe for targeting cervical cancer and application thereof
  • Tumor molecular probe for targeting cervical cancer and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1, tumor molecular probe 99m Tc-MAG 3 - Preparation and characterization of Pep-1

[0034] This embodiment intends to use SnCI 2 Reduction method pair with MAG 3 Modified Pep-1 polypeptide (ACGEMGWVRCGGGS-Ahx-KK) (product of Beijing Zhongke Yaguang Technology Co., Ltd., item number is C17282601) (MAG 3 The modification is at the last amino acid K of the C-terminal of the Pep-1 polypeptide, hereinafter referred to as MAG 3 -Pep-1 polypeptide) 99m Tc labeling, set the main labeling variables, and explore the most suitable labeling conditions. Study design marker variables include reaction temperature, pH, SnCI 2 Content and sodium tartrate content of the four variables were explored one by one, and the labeling conditions with a labeling rate higher than 95% were screened out. And apply the labeling conditions to label, purify, and then characterize the product, including in vitro stability in physiological saline, in vitro stability in bovine serum albu...

Embodiment 2

[0074] Embodiment 2, evaluation 99m Tc-MAG 3 - Imaging application value of Pep-1 in cervical cancer subcutaneous tumor-bearing mice

[0075] This example will evaluate the preparation of probes 99m Tc-MAG 3 - Imaging effect of Pep-1 on subcutaneous tumors in vivo. Firstly, the Pep-1 polypeptide was modified with fluorescein isothiocyanate (FITC), and then qualitatively and quantitatively evaluated HeLa (human cervical cancer cell line) detection of FITC-Pep-1 by cell fluorescence staining and flow cytometry fluorescence respectively. The uptake capacity of needles; by radioactive cell uptake experiments, set 99m Tc-MAG 3 -Pep-1, 99m Tc-MAG 3 -Pep-1+MAG 3 -Pep-1 (blocking group) and Na 99m TCO 4 (Negative control) to evaluate the HeLa pair 99m Tc-MAG 3 - Selected specificity of the Pep-1 probe; assessed by cell saturation binding assay 99m Tc-MAG 3 - Pep-1 affinity for HeLa. Prepare animal models, including HeLa and HepG2 tumor-bearing mice, perform static SPECT...

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Abstract

The invention discloses a tumor molecular probe for targeting cervical cancer and application of the tumor molecular probe. The invention provides a method for preparing the tumor molecular probe, which comprises the following step: performing 99mTc labeling on MAG3 modified Pep-1 polypeptide to obtain the tumor molecular probe. According to the 99mTc-MAG3-Pep-1 probe synthesized and prepared according to the invention, the 99mTc-MAG3-Pep-1 probe has very strong in-vitro stability through detection, and in addition, the invention also explores the development application value of the probe on a subcutaneous tumor-bearing (cervical cancer) mouse model so as to better reveal the biological performance and potential application prospect of the molecular probe. The 99mTc-MAG3-Pep-1 molecular probe with high labeling rate, high radioactivity specific activity and high radiochemical purity is prepared from three aspects of nuclear medicine, basic medicine and clinical transformation, and a good foundation is laid for further animal experiment research and clinical transformation.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a tumor molecular probe targeting cervical cancer and its application. Background technique [0002] Malignant tumor is a kind of disease affected by multiple factors, multiple gene changes and multi-stage progression, which seriously threatens human life, health and quality of life. Therefore, the study of changes in the tumor microenvironment has always been the focus and focus of oncology research. Small molecule peptides have the advantages of small molecular weight, clear chemical structure, controllable sequence, high activity, and low toxicity, and have long been concerned and favored by materials science and pharmacy. In recent years, in the field of molecular tumor and imaging research, peptides have gradually been widely used in research strategies for diagnosis and disease treatment because of their good assembly properties. At the same time, related transformation results ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08C07K7/06C07K1/13
CPCA61K51/08C07K7/06
Inventor 王荣福杜毓菁陈钊范岩张建华康磊闫平张春丽
Owner PEKING UNIV FIRST HOSPITAL
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