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Targeted Claudin-4 developer without influence on permeability between epithelial cells

An epithelial cell and permeability technology, applied in the field of medical imaging, can solve the problems of difficult to reflect tumor biological behavior differentiation, invasion and metastasis potential evaluation prognosis, etc., and achieve the effect of reducing the interference of blocking antibodies

Inactive Publication Date: 2009-11-11
SHANDONG TUMOR HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of the above-mentioned imaging agents are positioned based on changes in cellular tissue structure at the molecular level. Therefore, it is difficult to reflect the biological behavior of the tumor (such as the differentiation, invasion and metastasis potential of the tumor) and evaluate the prognosis.

Method used

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  • Targeted Claudin-4 developer without influence on permeability between epithelial cells
  • Targeted Claudin-4 developer without influence on permeability between epithelial cells
  • Targeted Claudin-4 developer without influence on permeability between epithelial cells

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Embodiment 1

[0031] 1. Polypeptide synthesis

[0032] Synthetic raw materials and related reagents:

[0033] 1) Protect amino acid raw materials

[0034] Fmoc-L-Ala-OH, Fmoc-L-Asn(Trt)-OH, Fmoc-L-Ser(tBu)-OH, Fmoc-L-Tyr(tBu)-OH, Fmoc-L-Gly-OH, Fmoc -L-Pro-OH, Fmoc-L-Ile-OH, Fmoc-L-Leu-OH, Fmoc-L-Phe-OH, Fmoc-L-Gln(Trt)-OH (Suzhou Tianma Pharmaceutical Group Fine Chemicals Co., Ltd. Company), where the abbreviation means: Fmoc: 9-fluorenylmethoxycarbonyl; Boc: tert-butoxycarbonyl; Trt: trityl; tBU: tert-butyl.

[0035] 2) Condensation reagent

[0036] HBTU (benzotriazole-N, N, N', N'-tetramethyluronium hexafluorophosphate, Suzhou Tianma Pharmaceutical Group Fine Chemicals Co., Ltd.), HOBT (1-hydroxybenzotriazole, Suzhou Tianma Pharmaceutical Group Fine Chemicals Co., Ltd.), DIEA (Diisopropylethylamine, Sinopharm Shanghai Chemical Reagent Company), NMM (N-methylmorpholine, Suzhou Tianma Pharmaceutical Group Fine Chemicals Co., Ltd.), DIC (Diisopropylethylamine Propylcarbodiimide, Suzhou...

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Abstract

The invention discloses a targeted Claudin-4 developer without influences on permeability between epithelial cells for positron emission computed tomography, which is a F marked polypeptide consisting of 16 amino acid residues. With shortened peptide chain, the polypeptide developer of the invention have importance biological properties of avoiding influence on the permeability between the epithelial cells, increasing the basement membrane permeability of the epithelial cells, reducing antigenicity and the like. The properties enable the developer to detect tumor lesion under the condition of constant tumor tissue microenvironments (such as blood flow, oxygenation, bioactive molecule distribution, pH value and cell apoptosis body removal) and to reduce interference from repeatedly used and inducible blocking antibodies at the same time.

Description

technical field [0001] The invention belongs to the technical field of medical imaging, and in particular relates to an imaging agent suitable for positron emission tomography, that is, a targeted Claudin-4 imaging agent that has no effect on the permeability between epithelial cells, and a preparation method thereof . Background technique [0002] Positron Emission Computed Tomography (PET) is a relatively advanced medical imaging technology, and PET technology is currently the only technology that uses anatomical morphology to perform functional, metabolic and receptor imaging, with non-invasive It is one of the best means to diagnose and guide the treatment of tumors clinically. [0003] The types of imaging agents currently used for tumor PET detection include: tumor blood flow imaging agents (such as 15O water), tumor metabolism imaging agents (such as glucose metabolism imaging agents: 18FDG; amino acid metabolism imaging agents: 11C-methionine; Phospholipid metaboli...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61K101/02
Inventor 国前于金明廖湘鲁王兴武陈鲁生赵书强徐峥浦程阳纪春绍付正李敏
Owner SHANDONG TUMOR HOSPITAL
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