18 f click-mark transferrin receptor targeting polypeptide t7 and its preparation method and application

A targeting peptide, 18f-tegay technology, applied in 18F click-labeled transferrin receptor targeting polypeptide T7 and its preparation and application fields, can solve the problems of low radioactive recovery rate, unfavorable automated synthesis, long time consumption and the like , to achieve the effect of high radiochemical yield, reduction of one purification process, and reduction of synthesis and purification time
CN106084004BActive Publication Date: 2020-01-14GUANGZHOU GENERAL HOSPITAL OF GUANGZHOU MILITARY COMMAND
2 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
GUANGZHOU GENERAL HOSPITAL OF GUANGZHOU MILITARY COMMAND
Publication Date
2020-01-14

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses 18F click labelling transferrin receptor targeting polypeptide T7 as well as a preparation method and application thereof. According to the preparation method, synthesis steps of click chemistry are improved, addition amount of a prosthetic group TsOTEGay is reduced, the addition amount of polypeptide T7 is appropriately increased, feeding ratio of the prosthetic group to the polypeptide T7 is adjusted to be 1:(1-2); after 18F-TEGay is synthesized through reaction, a polypeptide precursor is directly added for carrying out click reaction without carrying out HPLC purification, a 'one-pot two-step' process is adopted for synthesizing 18F-TEG-T7, and finally HPLC purification is carried out; and one purification process is reduced, the whole synthesis and purification time is greatly reduced and can be controlled to be within 120 minutes, radiochemical yield is about 28.26 minus and plus 7.43% (n=3). The optimized 'two-step one-pot' click reaction can be applied to research of 18F labelling polypeptide, and a novel tumor targeted probe can be prepared.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The present invention specifically relates to 18 F click marker transferrin receptor targeting polypeptide T7 and its preparation method and application. Background technique

[0002] Glioma is one of the most malignant brain tumors, originating from glial cells, and is the most common primary central nervous system tumor, accounting for about 42% of all brain tumors. The highly proliferative, invasive and aggressive nature of glioma makes its treatment still quite difficult. Timely and early accurate diagnosis of glioma is the key to treatment.

[0003] Transferrin Receptor (TfR) is highly expressed on the surface of tumor cells, especially glioma cells and brain capillary endothelial cells. T7 polypeptide (sequence HAIYPRH, His-Ala-Ile-Tyr-Pro-Arg-His) is a targeting polypeptide screened from cells expressing human transferrin receptor TfR by using phage display technology. The role of TfR. In the in vitro cell experiment, the T7 polypeptide has...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More