[<18>F] AlF marked positron emission tomography (PET) polypeptide probe and preparation method thereof

Abstract

The invention discloses a [<18>F] AlF marked positron emission tomography (PET) polypeptide probe and a preparation method thereof. The probe comprises TMTP1 polypeptide and NOTA, which are connected together, and the structural formulae of the TMTP1 polypeptide and the NOTA are shown in the description. According to the [<18>F] AlF marked positron emission tomography (PET) polypeptide probe and the preparation method thereof, a glycine is added to the TMTP1, and a G-TMTP1 polypeptide is designed, so that the polypeptide does not influence the biological activity after being radioactively marked; furthermore, 18F is taken as a radionuclide, and the G-TMTP1 polypeptide is marked by utilizing a [<18>F] AlF-NOTA method, so that the obtained [<18>F] AlF-marked PET polypeptide probe has excellent pharmacokinetics properties, the background cleaning rate is high, the liver uptake rate is low, in-vivo stability is good, the uptake rate of tumor site is high, highly metastatic tumor can be diagnosed specifically, and the polypeptide probe can be applied to diagnosis or therapeutic evaluation of highly metastatic malignant tumor.

Description

technical field [0001] The invention belongs to the field of radiolabeled compounds, in particular 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 in the world will reach 15 million each year (the World Health Organization recently published "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 only discovered in the late stages of cancer. Tumor metastasis is an important biological characteristic of malignant tumors. It is the main reason for the failure of tumor treatment and the main cause of death of tumor patients. About 70% of the newly diagnosed cancer patients can control their disease through surgery, adjuva...

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, and growth hormone inhibition. radiolabeled peptides such as peptides (M.Fani, H.R.Maecke, S.M.Okarvi, Radiolabeled peptides: valuable tools for the detection and treatment of cancer, Theranostics, 2012, 2(5):481-501), but so far there is no can be widely applied 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.

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