Radioactive halogen marked micromolecule cyclic peptide, composition and application of radioactive halogen marked micromolecule cyclic peptide

Abstract

The invention provides a radioactive halogen marked micromolecule cyclic peptide, which is characterized in that the micromolecule cyclic peptide is a chemical as shown in the formula (I): c(X1HWGFTLX2)-Y-Z (I), in the formula, c(X1HWGFTLX2) is a cyclic peptide formed by 8-10 combined amino acids, X1 and X2 are both at least one amino acid residue, Y is chelated ligand, Z is a metal compound containing radioactive halogen which is chelated with Y. The invention further provides a compound containing the micromolecule cyclic peptide, and application of the micromolecule cyclic peptide as a tumor developing agent. The radioactive halogen marked micromolecule cyclic peptide provided by the invention not only can be targeted to tumor cells, but also is high in permeability, can perform positioning expression on deep tissue, and is relatively good in clinical application prospect, and relatively good basis for later research or diagnosis on tumor can be provided for medical operators.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a radioactive halogen-labeled small molecular cyclic peptide, a composition containing the small molecular cyclic peptide and the application of the small molecular cyclic peptide as a tumor imaging agent. Background technique [0002] Tumor invasion and metastasis seriously affect the prognosis of patients, how to make an early diagnosis is a key clinical problem to be solved urgently. [0003] Matrix metalloproteinases (MMPs) are a group of Zn-containing + The most important class of proteases involved in the degradation of extracellular matrix (extra-cellular matrix, ECM). Because MMPs can decompose the basement membrane and extracellular matrix, causing tumor invasion and metastasis, and MMPs can also regulate many components in the tumor microenvironment, thereby promoting the occurrence and development of tumors. [1] Therefore, it is a hotspot in current research to pr...

AI Technical Summary

Problems solved by technology

There are currently research reports [3,4] The cyclic peptide c(KAHWGFTLD) NH2 was labeled with Cy5.5, and a variety of living tumor models were optically imaged with the marker, but the fluorescence imaging distance of the marker was short, the tissue penetration was poor, and the sensitivity was not high, so it was difficult to detect Localized expression in deep tissues can only be used as a simple animal model for basic research, lacking clinical application prospects

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