Polypeptide having high affinity with receptor of integrin alpha v beta3

An integrin and affinity technology, applied in the direction of peptides, drug combinations, tripeptide components, etc., to achieve the effect of low synthesis cost

Active Publication Date: 2013-04-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A potential limitation of LM609 is that it can only prevent αvβ3-mediated ang...

Method used

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  • Polypeptide having high affinity with receptor of integrin alpha v beta3
  • Polypeptide having high affinity with receptor of integrin alpha v beta3
  • Polypeptide having high affinity with receptor of integrin alpha v beta3

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Synthesis of RWR

[0023] First use R-D-Arg (fluorenylmethoxycarbonyl-arginine-king resin) 0.36 / 2mmol5.55g, add raw material L-Trp2.106g, use HBTU[2-(7-azobenzotriazole )-Tetramethyluronium hexafluorophosphate] 1.44g reaction time half an hour, cap removal time 40 minutes, then add raw material L-Arg 2.6g, condensing agent HBTU1.44g reaction time half an hour, cap removal time 40 minutes. Then purify : Dissolve the sample in acetonitrile, load the sample to the C18 preparative column, perform gradient elution with HPLC, collect the liquid, and test the purity of the liquid. Qualified samples were rotary evaporated and freeze-dried in a lyophilizer to obtain 200 mg of RWR.

[0024] The sequence is: Arg-Trp-Arg

[0025] It can be seen from the mass spectrum that the molecular weight of RWR is 517.61-1=516.61. There is an absorption peak of the peptide at 284nm in the ultraviolet spectrum.

Embodiment 2

[0027] Synthesis of RKY

[0028] First use R-D-Tyr (fluorenyl methaneoxycarbonyl-arginine-king resin) 0.33 / 2mmol6.06g, add raw material D-Lys1.88g, condensing agent with HBTU1.44g reaction time 25 minutes, uncapping time 30 minutes, and then Add 2.6g of D-Arg as raw material, 1.44g of HBTU as condensing agent, the reaction time is half an hour, and the capping time is 30 minutes. Then purify: dissolve the sample in acetonitrile, load the sample to the C18 preparative column, use HPLC for gradient elution, collect the liquid, and detect liquid purity. Qualified samples were rotary evaporated and freeze-dried in a lyophilizer to obtain 200 mg of RKY.

[0029] The sequence is: Arg-Lys-Tyr.

[0030] It can be seen from the mass spectrum that the molecular weight of Arg-Lys-Tyr is 466.56-1=465.56. There is an absorption peak of the peptide at 273nm in the ultraviolet spectrum.

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Abstract

The invention belongs to the fields of bioengineering pharmacy, protein polypeptide drugs and biomedical engineering and relates to a polypeptide having high affinity with a receptor of integrin alpha v beta3 and application of the polypeptide. The sequence of the polypeptide is Arg-Trp-Arg or Arg-Lys-Tyr. The polypeptide disclosed by the invention has higher affinity with the integrin alpha v beta3 than the traditional RGD (Arginine-Glycine-Aspartic acid) peptide and can be used in diagnosis and treatment of cancer.

Description

technical field [0001] The invention belongs to the fields of bioengineering pharmacy, protein polypeptide medicine and biomedical engineering, and relates to a polypeptide with high affinity for integrin receptor αvβ3 and its application, for example, in cancer diagnosis and treatment. Background technique [0002] The integrin family is a family of membrane receptors composed of many proteins with similar structures and functions. Dimeric glycoprotein is an important receptor on the cell surface with both adhesion and signal transduction functions. 24 integrins composed of 18 α subunits and 8 β subunits have been discovered, and α and β subunits jointly determine the receptor specificity of integrins. Integrins combine with the extracellular matrix (extracellular matix, ECM) through the extracellular domain, and combine with the cytoskeleton, signal transduction molecules and other proteins through the intracellular segment, and mediate the bidirectional signal transmissi...

Claims

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Application Information

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IPC IPC(8): C07K5/09A61K38/06A61P35/00G01N33/68
Inventor 顾月清艾观华董雪牛淼淼
Owner CHINA PHARM UNIV
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