PSMA-targeted fluorescent molecular probe as well as preparation method and application thereof

Abstract

The invention relates to the technical field of disease detection, in particular to a PSMA-targeted fluorescent molecular probe as well as a preparation method and application thereof. In the fluorescent molecular probe, a target head is a small molecule inhibitor or an oligopeptide substrate of PSMA; the load is a fluorophore; and an albumin binding group is contained or not contained. According to the fluorescent molecular probe disclosed by the invention, the binding capacity of the probe and PSMA is enhanced, which increases PSMA-mediated internalization; the half-life period is long, and the tumor enrichment time is long, so that accumulation of the targeting probe in prostate tumor tissue is increased; tumor fluorescence signals are obvious and stable in a relatively long time; and the fluorescent molecular probe disclosed by the invention shows excellent TBR in in-vivo and in-vitro imaging.

Description

technical field [0001] The invention belongs to the technical field of fluorescent molecular probes, and in particular relates to a fluorescent molecular probe targeting PSMA and its preparation method and application. Background technique [0002] Prostate cancer (PCa) is the most common malignancy in men and the third leading cause of cancer-related death in men worldwide. According to statistics, about 1-2% of men die of prostate cancer at present. As human beings enter an aging society, this disease that threatens the health of men around the world will become increasingly serious. Although the technology of early diagnosis and treatment of prostate cancer has developed rapidly in recent years, there are still many patients who reappeared with elevated serum prostate specific antigen (PSA) or imaging progression after initial treatment. Treatment options for prostate cancer include surgery, radiation therapy, and endocrine therapy. Patients diagnosed with early-stage ...

AI Technical Summary

Problems solved by technology

[0008] 1) Small molecule fluorescent probes have a short half-life, fast metabolism, and short residence time in tumors, making it difficult to achieve ideal TBR;

[0009] 2) Antibody-based fluorescent probes have a long half-life and slow clearance, and the large molecular weight of the antibody leads to poor tumor tissue permeability. After injection, delayed imaging (delayed for 2-4 days) is required to achieve the ideal TBR, resulting in increased nursing costs and difficulty

In addition, monoclonal antibodies are potentially immunogenic and prone to safety issues;

[0010] 3) It cannot well meet the requirements of intraoperative tumor-specific imaging, and there is a large room for improvement in sensitivity and specificity

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