PET (Polyethylene Terephthalate) molecular probe taking PD-L1 pathway as target spot and application of PET molecular probe

Abstract

The invention relates to the technical field of imaging molecular probes, in particular to a PET molecular probe taking a PD-L1 pathway as a target spot and application of the PET molecular probe. The PET molecular probe disclosed by the invention can be used for well carrying out in-vivo imaging on the expression level of the PD-L1 pathway in various tumor microenvironments. In an animal experiment, the tumor position of a mouse can be clearly observed within 30 minutes by using the probe, so that the probe can be quickly gathered at the tumor position, and the gathering condition of tumor cells can be observed within a relatively long time, so that the probe is good in targeting property and high in contrast ratio. The kit not only can be used for PD-L1 pathway expression detection in various tumor microenvironments, but also can assist an immunosuppressor in curative effect evaluation during immunotherapy, and provides real-time reference for treatment. The fluorescent probe can be used for non-invasive detection after being applied to an imaging agent, can be used for real-time imaging of the whole body of a living body, is simple in marking, high in contrast ratio, high in specificity and high in sensitivity, and has a relatively good clinical transformation prospect.

Description

technical field [0001] The invention relates to the technical field of imaging molecular probes, in particular to a PET molecular probe targeting PD-L1 pathway and its application. Background technique [0002] Programmed death 1 (PD-1) is a transmembrane receptor on lymphocytes, and PD-1 is mainly expressed on activated T cells and B cells. PD-1 and its ligands (Programmed Death-Ligand 1; PD-L1) are important mechanisms by which tumor cells evade the body's immune surveillance. The PD-L1 molecule is highly expressed on the membrane of many tumor cells. When it binds to PD-1 on immune cells such as T cells, tumor cells send out inhibitory signals, so that T cells cannot effectively recognize and kill tumor cells, resulting in tumor immune escape. Blocking the interaction between PD-1 and its ligand PD-L1 has emerged as a promising immunotherapy for the treatment of cancer. [0003] Drugs currently on the market targeting the PD-1 / PD-L1 pathway include monoclonal antibodies...

AI Technical Summary

Problems solved by technology

However, at present, imaging of the PD1 / PD-L1 pathway is mainly based on monoclonal antibody-based PET molecular probes. Although this type of PET molecular probe has certain imaging capabilities, the source of antibodies is expensive and the radionuclide 64 Cu, 89 Zr is not only very difficult to obtain, but also extremely expensive, which is unaffordable for both scientific research institutions and patients

PD1 / PD-L1 polypeptide PET molecular probes are currently the focus of research because of their small size, low cost and convenient labeling. 68 Ga-WL12 is used clinically, but the imaging effect is difficult to meet the clinical needs. It has the disadvantages of low targeting and poor contrast. Because the aggregation of tumor cells cannot be observed for a long time, it cannot provide a basis for treatment selection. Real-time reference; unable to perform real-time imaging of the whole body in vivo, and unable to assist in the evaluation of the curative effect of immunosuppressant immunotherapy, and there are few types of tumors that can be detected, difficult to label, and poor imaging effect on tumors

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