GPC3 receptor targeted polypeptide radioactive diagnosis or therapeutic drug

A radioactive and drug technology, applied in the directions of radioactive preparations, radioactive carriers, and drug combinations in vivo, can solve the problem of no effective treatment method for advanced liver cancer, and achieve the effect of improving the effective rate

Inactive Publication Date: 2017-08-08
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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Problems solved by technology

At present, there are many treatment methods for early liver cells, such as surgery, radiofrequency ablation, chemotherapy and biological immunotherapy, while there is no effective treatment for advanced liver cancer

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  • GPC3 receptor targeted polypeptide radioactive diagnosis or therapeutic drug
  • GPC3 receptor targeted polypeptide radioactive diagnosis or therapeutic drug
  • GPC3 receptor targeted polypeptide radioactive diagnosis or therapeutic drug

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Embodiment Construction

[0032] The present invention relates to a new GPC3 receptor-targeted polypeptide radioactive diagnostic and therapeutic drug. The polypeptide contains RLNVGGTYFLTTRQ (SEQ ID NO.1) sequence, which has the function of molecularly targeting GPC3 receptors and can be used for GPC3 receptor-positive Diagnosis and treatment of hepatocellular carcinoma. The preparation method of the polypeptide radiodiagnostic and therapeutic drug is as follows:

[0033] 1. Synthesis of polypeptide (RLNVGGTYFLTTRQ)

[0034] Polypeptides were synthesized by solid-phase 9-fluorenylmethoxycarbonyl (Fmoc) peptide chemical synthesis. Using chlorotriphenyl chloride resin as a carrier, the Fmoc amino protection strategy was used to synthesize the polypeptide in solid phase. The amino acid sequence is: RLNVGGTYFLTTRQ. The connection between the first amino acid and the resin adopts the symmetrical anhydride method, and after the reaction is completed, the remaining active sites on the resin are blocked wit...

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Abstract

The invention relates to a GPC3 (glypican-3) receptor targeted polypeptide radioactive diagnosis or therapeutic drug. The GPC3 receptor targeted polypeptide radioactive diagnosis or therapeutic drug includes: polypeptide with an amino acid sequence shown as SEQ ID NO:1; and a radionuclide or positron-emitting nuclide marker coupled to the polypeptide. The invention adopts the radionuclide labeled polypeptide as a hepatocellular carcinoma specific targeting molecular probe to show the expression situation of the GPC3 receptor in hepatocellular carcinoma tumor tissue on a living body level, and improves the effective rate of hepatocellular carcinoma oncotherapy. For lung cancer, melanoma and other GPC3 receptor-positive tumors, the GPC3 receptor targeted polypeptide can also be used for preparation of drugs for diagnosis or treatment of lung cancer and melanoma.

Description

technical field [0001] The invention relates to a GPC3 receptor-targeted diagnostic and therapeutic drug, in particular to a GPC3 receptor-targeted polypeptide radioactive diagnostic and therapeutic drug. Background technique [0002] Liver cancer is one of the most common malignant tumors in my country. Conventional imaging diagnostic techniques mainly include B-ultrasound, CT and MRI. It has good application value, but there are still some deficiencies in differential diagnosis, systemic staging and early efficacy evaluation. At present, there is no standard chemotherapy regimen for advanced hepatocellular carcinoma in the world. Traditional combined chemotherapy has no certain effect on prolonging the survival of patients with advanced hepatocellular carcinoma. The curative effect is mostly less than 20% and the side effects are large. [0003] Positron emission tomography / computerized tomography (PET / CT) is a new type of nuclear medicine imaging technology developed and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K47/64A61P35/00
CPCA61K51/088
Inventor 吴湖炳王珍韩彦江王全师黄顺王猛
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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