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A kind of dual-enzyme system probe and its application

An enzyme system and probe technology, applied in the field of nuclear medicine, can solve the problems of tumor cell mutation, resistance, poor prognosis, etc.

Active Publication Date: 2022-05-17
PEKING UNIV FIRST HOSPITAL
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  • Abstract
  • Description
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Problems solved by technology

Prostate cancer lesions can be treated with radiotherapy and surgery, and endocrine therapy for advanced prostate cancer can also achieve very good results, but castration resistant prostate cancer (CRPC) is not sensitive to endocrine therapy and radiotherapy , and the prognosis is very poor; nuclide-targeted therapy has shown an effective control rate of up to 80% in the targeted therapy for advanced castration-resistant prostate cancer, but the slow treatment cycle will lead to tumor cell mutations, which in turn produce resistance. sex

Method used

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  • A kind of dual-enzyme system probe and its application
  • A kind of dual-enzyme system probe and its application
  • A kind of dual-enzyme system probe and its application

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Embodiment Construction

[0063] Preferred embodiments of the present invention will be described in more detail below. Although preferred embodiments of the present invention are described below, it should be understood that the present invention can be embodied in various forms and should not be limited by the embodiments set forth herein.

[0064] Preparation of Probe A, Probe B, Probe C and Probe D

[0065] The specific structure of Probe A-D is as follows figure 2 shown. Synthetic steps such as image 3 shown. Coupling of amino acids was performed according to standard Fmoc solid phase synthesis.

[0066] image 3A general route for the preparation of Probes A-D is shown. Reaction conditions: (a) Fmoc-L-aspartic acid 4-tert-butyl ester, HATU and DIPEA in DCM; (b) TFA in DCM; (c) 2-chlorotriphenyl chloride resin and DIPEA in DMF / DCM solution; (d) DMF solution of 20% piperidine, DMF solution of Fmoc-L-valine, HBTU, HOBt and DIPEA; (e) DMF solution of 20% piperidine, N-Fmoc-L-glucose DMF ...

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Abstract

The invention belongs to the field of nuclear medicine, and relates to a dual-enzyme system probe and its application. The probe has a structure shown in formula I, wherein QD is a fluorescent group or a drug group; L is a linker with a structure shown in formula II; T is a PSMA-specific targeting group; Z is H, a nuclide chelate chelating group, radionuclide or nuclide chelating group with radionuclide chelated. The present invention is based on the prostate-specific membrane antigen PSMA targeting and Caspase-3 recognition strategy to deliver the dual-enzyme system nuclear medicine probe of drug molecules, which can target prostate cancer for radiotherapy sensitization treatment, and help to solve castration-resistant prostate It is expected to realize intraoperative navigation of prostate cancer. It provides more efficient tools for the detection and treatment of tumor therapy, and has broad application prospects.

Description

technical field [0001] The invention belongs to the field of nuclear medicine, and in particular relates to a dual-enzyme system probe and its application. Background technique [0002] Prostate cancer is the second most lethal malignancy among men, and ranks first in cancer incidence in Western developed countries. With the continuous development of my country's economy and society, the problem of population aging is prominent, the process of urbanization and industrialization is accelerating, and unhealthy lifestyles and chronic infection factors are gradually accumulating. The incidence and mortality of prostate cancer are increasing every year. Prostate cancer lesions can be treated with radiotherapy and surgery, and endocrine therapy for advanced prostate cancer can also achieve very good results, but castration resistant prostate cancer (CRPC) is not sensitive to endocrine therapy and radiotherapy , and the prognosis is very poor; nuclide-targeted therapy has shown an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/02C07K1/13A61K51/08A61K49/00A61K47/64A61P35/00
CPCC07K7/02A61K51/08A61K49/0056A61K47/64A61P35/00
Inventor 杨兴刘昭飞徐红闯王琰璞张宁范岩杨志高献书
Owner PEKING UNIV FIRST HOSPITAL
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