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Bicyclic peptide nuclide ligands and probes targeting Nectin-4

A bicyclic peptide and nuclide technology, applied in the field of nuclear medicine, can solve the problems of good tissue permeability, large molecular weight of monoclonal antibody, poor cell membrane permeability, etc., achieve high tumor to muscle uptake ratio, good clinical application prospects, good Effects on metabolic performance in vivo

Active Publication Date: 2022-03-04
PEKING UNIV FIRST HOSPITAL
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Problems solved by technology

[0004] The currently reported Nectin-4 targeting nuclear medicine diagnostic reagents are radionuclides 89 Zr and 18 F-labeled Nectin-4 monoclonal antibody (AGS-22M6), but due to the defects of large molecular weight of monoclonal antibody, long metabolism time in vivo, high blood background, and poor cell membrane penetration, the monoclonal antibody is directly used in Conventional clinical molecular imaging reagents have certain limitations, while small molecule drugs have a short half-life in vivo circulation and good tissue permeability, which have natural advantages in clinical transformation

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Embodiment Construction

[0038] Preferred embodiments of the present invention will be described in more detail below. Although preferred embodiments of the present invention are described below, it should be understood that the present invention can be embodied in various forms and should not be limited by the embodiments set forth herein.

[0039] Nectin-4 targeting ligand synthesis

[0040] Preparation of Ligand DXJ187

[0041] The specific structure of DXJ187 is as follows figure 1 shown. The synthetic steps of compound DXJ187 are as follows figure 2 As shown, the precursor polypeptide resin 187resin was purchased from Shanghai Chueptide Biotechnology Company, and other reagents were purchased from reagent companies without purification. The purchased resin was deprotected after coupling with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid tri-tert-butyl ester, followed by the cyclization linker TATA The reaction affords compound 187. The synthetic route of the above-mentioned DO...

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Abstract

The invention belongs to the field of nuclear medicine, and relates to a Nectin-4 targeting bicyclic peptide nuclide ligand and a probe. The ligand has a structure as shown in a formula I, wherein X is Lys or Arg; r is a group as shown in a formula II, a formula III, a formula IV or a formula V. The probe provided by the invention has higher tumor uptake and higher tumor to muscle uptake ratio, and has a good clinical application prospect.

Description

technical field [0001] The invention belongs to the field of nuclear medicine, and in particular relates to a bicyclic peptide nuclide ligand targeting Nectin-4 and a bicyclic peptide nuclide probe targeting Nectin-4 formed by the ligand. Background technique [0002] Cell Adhesion Molecular (CAM) is a class of cell membrane surface glycoprotein molecules that mediate cell-cell and cell-extracellular matrix interactions. It plays an important role in physiological processes and is also involved in cell signal transduction processes. Therefore, the abnormal expression of CAM can reflect the pathological changes of the body to a certain extent. CAM can be roughly divided into selectin (Selectin) family, integrin family (Integrin), cadherin family (Cadherin) and immunoglobulin superfamily (Immunoglobulin superfamily, IgSF). The expression of most CAMs in the body is not specific, and there is no significant difference in the expression of cells in various tissues. However, t...

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Application Information

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IPC IPC(8): C07K7/08C07K1/13A61K51/08A61P35/00A61K101/02A61K101/00A61K103/10A61K103/20A61K103/32A61K103/30A61K103/40
CPCC07K7/08A61K51/08A61P35/00
Inventor 杨兴段小江朱华张宁杨志张建华张卓晨
Owner PEKING UNIV FIRST HOSPITAL
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