A [18f]alf-labeled pet polypeptide probe and its preparation method

Abstract

The invention discloses a [18F]AlF-labeled PET polypeptide probe and a preparation method thereof, comprising TMTP1 polypeptide and NOTA linked together, and its structural formula is as follows:. In the present invention, G-TMTP1 polypeptide is designed by adding a glycine to TMTP1 so that it does not affect its biological activity after being radiolabeled, and uses 18F as the radionuclide, and uses [18F]AlF-NOTA to mark G-TMTP1 Polypeptide, the obtained [18F]AlF-labeled PET polypeptide probe has excellent pharmacokinetic properties, fast background clearance rate, low liver uptake, good stability in vivo, high uptake in tumor sites, and high specificity for diagnosis Metastatic tumors can be used for the diagnosis or curative effect evaluation of highly metastatic malignant tumors.

Description

Technical field [0001] The invention belongs to the field of radiolabeled compounds, and specifically relates to a [ 18 F] AlF-labeled PET polypeptide probe and its preparation method. Background technique [0002] According to the current development trend of cancer, the incidence of cancer worldwide will increase by 50% in 2020, and the number of new cancer patients worldwide will reach 15 million each year (World Health Organization recently published the "World Cancer Report"). Early detection and early treatment of tumors is the most effective way to reduce the mortality of cancer patients. At present, in developing countries, 80% of cancer patients are discovered in the late stage of cancer. Tumor metastasis is an important biological feature of malignant tumors. It is the main reason for tumor treatment failure and the main cause of death of tumor patients. Among the newly diagnosed tumor patients, about 70% of the patients can be controlled by surgery, adjuvant radiother...

AI Technical Summary

Problems solved by technology

PET technology has three elements: PET probe, signal amplification, and high-sensitivity detector. Among them, PET probe is the most important, which is the first prerequisite for signal amplification and high-sensitivity detection. At present, the most widely used clinical tumor diagnosis is[ 18 F] FDG, but because of its low specificity, it is easy to cause false positives and other limitations, it can not fully meet the clinical requirements, in addition [ 18 F] FDG cannot make an accurate judgment on whether the tumor has the ability to metastasize, so the new 18 F-labeled molecular imaging probes still need to be developed urgently

[0006] The development of polypeptide PET probes is an important direction. At present, there have been a lot of researches on vasoactive intestinal peptide (VIP), octreotide, bombesin, RGD, VEGF, TNF, gastrin, growth hormone inhibition. radiolabeled peptides such as peptides (M.Fani, H.R. Maecke, S.M.Okarvi, Radiolabeledpeptides: valuable tools for the detection and treatment of cancer, Theranostics, 2012, 2(5): 481-501), but so far there is no real Can be widely used in clinical 18 F-labeled polypeptide molecular imaging probes, the main reason is that the polypeptide has a large number of active functional groups, which are sensitive to labeling conditions, the activity of the polypeptide after radiolabeling is relatively large, and the pharmacokinetic properties of the labeled probe in vivo are not ideal. , such as high liver uptake, poor in vivo stability, low tumor uptake, etc.

Images