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Integrin alpha 6 target polypeptide and application

A technology for targeting peptides and integrins, which can be applied to peptides, preparations for in vivo experiments, radioactive preparations in vivo, etc. It can solve the problems of lack of targeting peptides and achieve the effect of good affinity.

Active Publication Date: 2018-05-04
广州珺柏诺医疗科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the prior art, there is a lack of corresponding targeting peptides

Method used

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  • Integrin alpha 6 target polypeptide and application
  • Integrin alpha 6 target polypeptide and application
  • Integrin alpha 6 target polypeptide and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0024] The integrin α6 targeting polypeptide has the motif RWYXXXA (SEQ ID NO: 1).

[0025] As a further improvement of the above integrin α6 targeting polypeptide, the motif is selected from: RWYAENA (SEQ ID NO: 2), RWYDANA (SEQ ID NO: 3) or RWYDEAA (SEQ ID NO: 4).

[0026] As a further improvement of the above-mentioned integrin α6 targeting polypeptide, the C-terminal and / or N-terminal of the motif may optionally be connected with 1-3 amino acids.

[0027] As a further improvement of the above-mentioned integrin α6 targeting polypeptide, a Cys is connected to both ends of the motif.

[0028] As a further improvement of the above-mentioned integrin α6 targeting polypeptide, the polypeptide forms a cyclic peptide through Cys at both ends.

[0029] The amino acids in the above polypeptides can be either L-form or D-form.

[0030] A targeted diagnosis or screening reagent, including an imaging agent coupled with the above-mentioned integrin α6 targeting polypeptide.

[0031]...

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Abstract

The invention discloses integrin alpha 6 target polypeptide and application, and the sequence motif of the polypeptide is RWYXXXA. The integrin alpha 6 target polypeptide has very good affinity with integrin alpha 6, is relatively stable in vivo, and can serve as a target carrier. The integrin alpha 6 target polypeptide can be applied to molecular imaging of multiple kinds of integrin alpha 6 overexpression tumors, and has an important value in the molecular imaging of tumors. By coupling the polypeptide with a molecular imaging probe, the molecular imaging can be carried out on the multiple kinds of integrin alpha 6 overexpression tumors, and can be applied to diagnosis and screening of tumors very well.

Description

technical field [0001] The invention relates to a class of targeting peptides and applications thereof, in particular to integrin α6 targeting polypeptides and applications. Background technique [0002] Integrin is a membrane protein with a large extracellular region, which is conducive to the approach and binding of molecular probes, so it is an ideal target for tumor molecular imaging and tumor-targeted therapy. Integrins are composed of 18 a subunits and 8 beta subunits to form 24 heterodimers. Integrins overexpressed in tumors mainly include αvβ3, αvβ5, α5β1, α4β1, α2β1, α3β1, αvβ6, α6β4 and α6β1. Among them, RGD polypeptide molecular probes targeting integrin αvβ3 and tumor-targeted therapeutic drugs are the most widely studied. Integrin αvβ3 is overexpressed in tumor neovascularization and low in normal tissue blood vessels, so the RGD polypeptide molecular probe can judge the situation of tumor angiogenesis. At present, researchers have successfully developed a va...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K51/08A61K49/00A61K101/02
CPCA61K49/0034A61K49/0056A61K51/088C07K7/06
Inventor 曾木圣冯国开王茜林燕珠
Owner 广州珺柏诺医疗科技有限公司
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