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Fluorescent probe for detecting cancer

A fluorescent probe, breast cancer technology, applied in the field of fluorescent probes

Pending Publication Date: 2021-10-01
THE UNIV OF TOKYO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, many malignancies cannot be detected with high sensitivity / specificity by these fluorescent probes due to the lack of significant difference in aminopeptidase activity between cancer and normal tissues

Method used

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  • Fluorescent probe for detecting cancer
  • Fluorescent probe for detecting cancer
  • Fluorescent probe for detecting cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0168] Screening of glycosidase-reactive fluorescent probes for the detection of breast cancer and benign

[0169] Using 12 kinds of glycosidase reactive fluorescent probes synthesized above (refer to figure 1 ), the screening for detection of breast cancer and benignity was performed according to the following procedure.

[0170] 200 μL of a PBS solution of each fluorescent probe at a concentration of 50 μM was added to each well of the breast clinical specimen, and the 540 nm at 1, 3, 5, 10, 20, and 30 minutes were obtained using a Maestro in vivo imaging system (PerkinElmer). fluorescence images. For each fluorescence intensity value, regions of interest (Regions Of Interest, ROIs) were obtained on the Maestro software and quantified and compared. Filter settings use Ex / Em=465-30nm / 515nm long-pass.

[0171] show the result in figure 2 .

[0172] figure 2 A shows the results of screening using fluorescent probes of surgically resected human breast specimens.

[01...

Embodiment 2

[0187] Breast Tumor Imaging Using HMRef-a-D-Man

[0188] Imaging was performed using glycosidase-reactive fluorescent probe 5 (HMRef-a-D-Man) (concentration: 50 mM) under the following conditions.

[0189] 3 mL of the above-mentioned fluorescent probe solution in PBS was added to a petri dish containing a clinical breast specimen (a specimen in which a normal part and a tumor part were mixed), and fluorescence images at various times were obtained. Next, fluorescence images of DCIS and FA clinical specimens were obtained using the Maestro in vivo imaging system (PerkinElmer). Each filter setting uses Ex / Em=465-30nm / 515nm long-pass. Fluorescence images of clinical specimens of IDC were obtained using a portable imaging device manufactured by Homme equivalent to the Maestro in vivo imaging system.

[0190] show the result in Figure 7-8 .

[0191] Figure 7 a shows the imaging results of surgically resected IDC (breast cancer).

[0192] After spreading the probe, only th...

Embodiment 3

[0200] Difference between benign and breast cancer using HMRef-α-D-Man and GGT probes in combination

[0201] Two-color imaging was performed using a combination of glycosidase-reactive fluorescent probe 5 (HMRef-α-D-Man) (concentration: 50 μM) and GGT probe gGlu-2-OMeSiR600 (concentration: 50 μM) under the following conditions .

[0202] Add 200 μL of the PBS solution of the fluorescent probe of the above-mentioned concentration to each well where the breast clinical specimen is placed, and use the Maestroin in vivo imaging system (PerkinElmer) to obtain the 540nm and Fluorescence image at 640nm. For each fluorescence intensity value, regions of interest (ROIs) were obtained on Maestro software and quantified and compared. For the glycosidase-reactive fluorescent probe 5, Ex / Em=465-30nm / 515nm long-pass was used for the filter setting. For the GGT probe, Ex / Em=570-40nm / 610nm long-pass was used.

[0203] show the result in Figure 9 .

[0204] Figure 9 a shows a fluor...

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Abstract

To provide a fluorescent probe capable of detecting breast cancer, lung cancer, and squamous cell cancer. A fluorescent probe for detecting breast cancer and benign tumors of the breast, the probe containing a compound represented by general formula (I) or a salt thereof.

Description

technical field [0001] The present invention relates to fluorescent probes capable of specifically detecting cancer. More specifically, the present invention relates to fluorescent probes capable of detecting malignant and benign tumors of the breast, lung adenocarcinoma or lung squamous cell carcinoma. Background technique [0002] Methods for evaluating enzyme activity in malignant tissue can provide information on effective biomarkers to guide cancer detection. Fluorescence-induced detection of cancer is one of the most promising approaches for improving the efficiency of local excision surgery. The research group of the present inventors has so far developed an active aminopeptidase-reactive fluorescent probe (Non-Patent Document 1), which successfully detects human breast cancer within a few minutes by locally spraying the probe solution and esophageal cancer (Non-Patent Documents 2 and 3). [0003] However, many malignant tumors cannot be detected with high sensitiv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D407/04C07F7/10G01N21/64A61K49/00C12Q1/34
CPCC12Q1/34C07D407/04C07F7/0816C07D493/10G01N2333/924G01N33/582G01N2800/7028G01N33/57415C09B57/00C09B11/22C07H17/04G01N33/533G01N33/5005G01N21/6486C12Q1/37G01N2333/9108C07H17/06G01N21/6428G01N21/6456
Inventor 浦野泰照神谷真子藤田恭平
Owner THE UNIV OF TOKYO
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