Integrin receptor alpha-v-beta-3 related 5-peptide

一种整合素、肿瘤的技术，应用在体内试验用的配制品、肽、药物组合等方向，能够解决化药缺少肿瘤细胞特异性、器官毒性等问题

Active Publication Date: 2015-07-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, cancer has become one of the main causes of human death, and chemotherapy is still the main method for treating cancer. However, due to the lack of specificity of traditional chemical drugs for tumor cells, it has caused some organ toxicity to patients.

Method used

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  • Integrin receptor alpha-v-beta-3 related 5-peptide
  • Integrin receptor alpha-v-beta-3 related 5-peptide
  • Integrin receptor alpha-v-beta-3 related 5-peptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] 5-peptide synthesis

[0023] 1: Coupling

[0024] Swell Fmoc-Met-Rink amide MBHA resin (Fmoc-Met-Rink amide-rink amino resin) 0.33 / 2mmol6.06g in dimethylformamide, 10ml / g resin, then use 20% six Hydropyridine / dimethylformamide solution removes the Fmoc protecting group (hereinafter referred to as decapping), washes the resin after decapping with dimethylformamide, adds raw material Fmoc-Asn(tBU)-OH 2.3g, condensing agent Use HBTU 1.44g, the reaction time is 30 minutes, and the Kaiser method is used for detection. If the test result is negative, it means that the coupling reaction is completed, and then the capping is carried out for 30 minutes. If the test result is still positive, it means that the coupling reaction is not completed. Or the reaction is not complete, it is necessary to prolong the coupling time or re-feed the coupling until the coupling reaction is completed. Repeat the above operations, sequentially coupling; Fmoc-D-Arg(Pbf)-OH; Fmoc-Trp-OH; Fmoc-Arg...

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Abstract

The invention belongs to the technical field of biomedicine production or the fields of protein polypeptide drugs and biomedical engineering, and in particular relates to a polypeptide which has high affinity with an integrin receptor and an application of the polypeptide like cancer diagnosis and treatment. The polypeptide is composed of five amino acids, and the sequence is arginine-tryptophan-arginine-asparagine-methionine (Arg-Trp-Arg-Asn-Met). On the basis of an in-vitro flow cytometry affinity determination experiment, the polypeptide disclosed by the invention has quite strong targeting on high-expression cells of the integrin receptor, and through an in-vitro laser confocal cell uptake experiment, the polypeptide can be targeted to high-expression tumor cells of the integrin receptor alpha-v-beta-3 and can basically avoid targeting on low-expression tumor cells and normal cells of the integrin receptor alpha-v-beta-3. An in-vitro cytotoxicity result shows that the 5-peptide disclosed by the invention is basically free from toxicity on cells, and the 5-peptide has a good application prospect in the diagnosis and the treatment of cancers.

Description

technical field [0001] The invention belongs to the field of bioengineering pharmaceutical technology, protein polypeptide medicine and biomedical engineering, and specifically relates to a polypeptide with high affinity for integrin receptor αvβ3 and its application, for example, in cancer diagnosis and treatment. Background technique [0002] At present, cancer has become one of the main causes of human death, and chemotherapy is still the main method to treat cancer. However, due to the lack of specificity of traditional chemical drugs against tumor cells, it has caused some organ toxicity to patients. [0003] Integrins are widely expressed in cells in the body, and most cells can express more than one integrin on the surface. These integrins not only participate in the growth, differentiation and apoptosis of some cells, but H plays a role It also plays a very important role in the pathological process. The integrin family includes 18 α subtypes and 8 β subtypes, and t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C12Q1/04A61K47/48A61P35/00
CPCA61K49/0041A61K49/0056A61P35/00C07K7/06G01N33/57492C07K14/70557G01N33/574
Inventor 顾月清张聪颖赵梦路王茜田彩平刘雨溪
Owner CHINA PHARM UNIV
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