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Synthesis method of cyclic pentapeptide and application of cyclic pentapeptide in anti-hepatitis C medicine

A technology of cyclic pentapeptides and uses, which is applied in the field of cyclic pentapeptides and its application in anti-hepatitis C drugs, can solve the problems of disappearance, weakened antiviral efficacy, and difficulty in forming cyclized structures, etc., and achieve good structural stability, The effect of efficient combination

Active Publication Date: 2021-07-23
TIANJIN MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the actual synthesis research shows that due to the excessive tension inside the cyclic tetrapeptide structure, it is difficult to form a cyclized structure, and even after forming a cyclic structure, it may lose its binding ability in the hydrophobic channel due to the instability of the cyclized structure, resulting in Antiviral efficacy weakened or even disappeared

Method used

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  • Synthesis method of cyclic pentapeptide and application of cyclic pentapeptide in anti-hepatitis C medicine
  • Synthesis method of cyclic pentapeptide and application of cyclic pentapeptide in anti-hepatitis C medicine
  • Synthesis method of cyclic pentapeptide and application of cyclic pentapeptide in anti-hepatitis C medicine

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Embodiment Construction

[0026] In order to better understand the present invention, the present invention will be described in detail below in conjunction with specific drawings.

[0027] 1. Preparation of Cyclic Pentapeptide

[0028] 1.1 Raw materials and reagents:

[0029] (1) Protect amino acids and raw materials

[0030] Fmoc-Arg(Pbf)-OH, Fmoc-D-Tyr(tBu)-OH, Fmoc-Glu(OtBu)-OH, Fmoc-Asp(OtBu)-OH, etc.

[0031] (2) Condensation reagent

[0032] HBTU, DIEA,

[0033] (3) Solvent

[0034] DMF, DCM, acetonitrile,

[0035] (4) Resin

[0036] 2-Chlorotrityl chloride resin

[0037] (5) Deprotection reagent

[0038] piperidine

[0039] (6) Cutting reagent

[0040] Trifluoroethanol, DCM, TFA, TIS, EDT, H 2 o

[0041] (7) Nitrogen

[0042] (8) Anhydrous ether

[0043] (9) Precision electronic balance

[0044] 1.2 Synthesis process:

[0045] (1) Resin swelling

[0046] Put 2-Chlorotrityl Chloride Resin resin into the reaction tube, add DCM (15ml / g), and shake for 30min.

[0047] (2) Take the...

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Abstract

The invention provides a cyclic pentapeptide. The amino acid sequence of the cyclic pentapeptide is cyclo-5-aspartic acid-glutamic acid-arginine-tyrosine-arginine. A cyclic pentapeptide inhibitor provided by the invention has excellent structural stability, can be efficiently combined with p7 channel protein, and effectively achieves the anti-hepatitis C virus effect.

Description

technical field [0001] The invention belongs to the field of biotechnology, and relates to a novel cyclic pentapeptide and its application in anti-hepatitis C drugs. Background technique [0002] Studies have shown that p7 is an important protein that affects (hepatitis C virus) HCV infection activity. p7 exists in the endoplasmic reticulum, has the transport activity of cations, and has higher selectivity to calcium ions. It is the only ion channel protein in HCV. In the liposome ion current experiment, inhibiting the p7 protein can obviously shield the ion flow on both sides of the membrane, and knocking out the p7 protein on the viral genome or carrying out the mutation of the p7 protein R33Q or R35Q, hepatitis C virus in the extracellular supernatant The titer is obviously eliminated [1,2] . It is inferred that p7 protein acts as an ion channel and then plays a function related to the release of hepatitis C virus. Therefore, the p7 ion channel can be used as a good d...

Claims

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Application Information

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IPC IPC(8): C07K7/64A61K38/12A61P31/14
CPCC07K7/64A61P31/14A61K38/00Y02A50/30
Inventor 王树青董卫莉魏树琨欧阳波周界文
Owner TIANJIN MEDICAL UNIV
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