Peptide radioactive medicine comprising iRGD sequence

A radiopharmaceutical and radioactive technology, applied in the field of polypeptide radiopharmaceuticals

Inactive Publication Date: 2012-07-25
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
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  • Peptide radioactive medicine comprising iRGD sequence
  • Peptide radioactive medicine comprising iRGD sequence
  • Peptide radioactive medicine comprising iRGD sequence

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[0048] A polypeptide radiopharmaceutical containing an iRGD sequence, which is based on the polypeptide iRGD, modified and complexed with metal ions or labeled with a positron nuclide. The sequence of the polypeptide (peptide) contains or or available for integrin alpha v beta 3 Or the diagnosis and treatment of neuropilin-1 receptor-related diseases.

[0049] 1. Polypeptide synthesis

[0050] Polypeptides were synthesized by solid-phase synthesis, using 9-fluorenylmethoxycarbonyl (Fmoc) chemical protection strategy, wherein, Fmoc-Cys (Acm), Fmoc-Arg (pbf), Fmoc-Gly, Fmoc-Asp (OtBu), Fmoc -Lys(Boc), Fmoc-Pro, are all purchased from Bachem Company; [2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HBTU ) was purchased from Richelieu Biotechnoligies; 1-hydroxybenzotriazole (HOBT) was purchased from Sigma; diisopropylethylamine (DIPEA) was purchased from Aldrich. Weigh 1 equiv Wang resin and remove the Fmoc protecting group. Dissolve 4equiv Fmo...

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Abstract

The invention provides a peptide radioactive medicine comprising an iRGD sequence. The sequence of the peptide comprises CRGDKGPDC or CRGDRGPDC or CRGDKGPEC and is formed by marking through coupling radioactive metal nuclides or positron nuclides, the peptide radioactive medicine comprising the iRGD sequence has three functions of molecular target integrin alpha v beta 3 receptor, Neuropilin-l receptor and cellular transduction, and the peptide radioactive medicine comprising the iRGD sequence can be used as a diagnostic medicine capable of greatly increasing the target/non-target ratio, so that the sensitivity can be effectively improved, and the development quality can be improved, and the peptide radioactive medicine can be used as a therapeutic medicine capable of obviously improving the treatment effect.

Description

technical field [0001] The present invention relates to the field of radiopharmaceuticals, in particular to polypeptide radiopharmaceuticals containing iRGD sequence. Background technique [0002] Angiogenesis, the process of generating new blood vessels on the basis of existing blood vessels, is the basis of tumor growth and metastasis. Integrin alpha v beta 3 Plays an important role in the process of angiogenesis. As one of the molecular markers related to neovascularization, it is highly expressed on the surface of neovascular endothelial cells and some tumor cells (neuroblastoma, osteosarcoma, glioblastoma, breast tumor and prostate cancer, etc.), while No or low expression in existing blood vessels and normal tissues. Integrin alpha v beta 3 Highly restricted expression during tumor growth and metastasis makes it a very attractive target for tumor diagnosis and therapy. [0003] Integrin alpha v beta 3 It plays a role mainly by binding to ligands containing RGD...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61P35/00A61K101/02
Inventor 韩彦江吴湖炳王全师
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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