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Tripeptide inhibitor for adenomatous polyposis coli/APC-stimulated guanine nucleotide exchange factor (APC/Asef) interaction and application thereof

A peptide inhibitor, P1-E-A-L-P2 technology, applied in the field of peptides, can solve the problems of APC full-length, limited application, difficult transfection, etc.

Active Publication Date: 2021-01-12
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Floquet et al. used the method of gene induction to restore full-length APC, but the application of this method was greatly limited due to the long length of APC and the difficulty of transfection.

Method used

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  • Tripeptide inhibitor for adenomatous polyposis coli/APC-stimulated guanine nucleotide exchange factor (APC/Asef) interaction and application thereof
  • Tripeptide inhibitor for adenomatous polyposis coli/APC-stimulated guanine nucleotide exchange factor (APC/Asef) interaction and application thereof
  • Tripeptide inhibitor for adenomatous polyposis coli/APC-stimulated guanine nucleotide exchange factor (APC/Asef) interaction and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1 Solid phase synthesis, cleavage, purification and identification of polypeptide 1

[0056] 1.1 Solid phase synthesis of polypeptide 1

[0057] The present invention utilizes a polypeptide synthesizer to synthesize polypeptide 1 (39901-94-5)-ESL-(1003-03-8) by a solid-phase synthesis method: using DMF as a solvent, the concentration of amino acid solutions in which various α-amino groups are protected by Fmoc 0.25mol / L, the concentration of HBTU solution and HOBt solution is 0.33mol / L, the concentration of piperidine solution is 200ml / L, and the concentration of DIEA solution is 174.2ml / L.

[0058] 1.1.1 Activated resin

[0059] Take 1g of Fmoc (fluorenebenzyloxycarbonyl)-protected butyramide resin and put it into the reactor, add an appropriate amount of dichloromethane to expand the resin, remove excess dichloromethane in the reactor by suction filtration, and put the expanded resin back into the reactor. Add 6.00mL of N,N-dimethylformamide solution contain...

Embodiment 2

[0066] Example 2 Prepare polypeptide 2(39901-94-5)-ESL-(51-67-2) according to the same method as in Example 1, the solid purity is greater than 98%, ESI: 570.57[M-H] - ;

Embodiment 3

[0067] Example 3 Polypeptide 3(31462-59-6)-ESL-(122-11-2) was prepared according to the same method as in Example 1, the solid purity was greater than 98%, ESI: 744.8[M-H] - ;

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Abstract

The invention provides a tripeptide inhibitor for adenomatous polyposis coli / APC-stimulated guanine nucleotide exchange factor (APC / Asef) interaction. The tripeptide inhibitor comprises an amino acidsequence as shown by a formula (1) and salt thereof: formula (1): P<1>X1-X2-X3-P<2>. A novel tripeptide provided by the invention exerts an anti-tumor effect by inhibiting the APC / Asef protein reaction in cancer cells. An N end and a C end of the polypeptide are terminated, and can form a strong hydrophobic effect with APC protein; moreover, amino acid with carboxyl and contained in the polypeptide can form a strong electrostatic effect with basic amino acid in the APC protein, and the stereo configuration of the tripeptide can fits an APC protein pocket, so that the APC / Asef interaction can be strongly inhibited, and the anti-tumor treatment effect is achieved. The anti-tumor peptide disclosed by the invention has broad spectrum, has the effects of inhibiting and killing various cancer cells, and is short in peptide chain length, is high in anti-tumor activity, is stable and not prone to inactivate.

Description

technical field [0001] The invention belongs to the field of polypeptides, and more specifically relates to a class of anti-tumor tripeptide compounds and applications thereof. Background technique [0002] The interaction between specific intracellular proteins constitutes a variety of intracellular signal transduction pathways, which are crucial to the survival of normal cells and cancer cells, and are an important source of drug targets. Studies have found that there is a specific protein-protein interaction in cancer cells—the truncated APC (Adenomatous Polyposis Coli) / Asef (APC-stimulated guanine nucleotide exchange factor) protein interaction, which It plays an important role in the occurrence and development of tumors and can become a new drug target for cancer treatment. [0003] APC is involved in regulating processes such as cell adhesion and cell migration under physiological conditions. Clinical studies have confirmed that in patients with colon cancer, breast ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/093C07K14/47A61K38/06A61K38/17A61P35/00A61P35/02
CPCC07K5/0819C07K14/4705A61P35/00A61P35/02A61K38/00
Inventor 张健杨秀岩阮聪钟杰
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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