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Chemokine receptor 5 antagonist and pharmaceutical composition

A chemokine receptor and antagonist technology, which is applied in the field of small molecule active peptides as the antagonists, can solve the problems of inability to locate the target, interfere with phage panning, lack of further verification by animal experiments, etc.

Inactive Publication Date: 2015-07-29
钟英强 +1
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Problems solved by technology

[0005] However, the main disadvantage of the above experimental scheme is that the whole cell is used as the target antigen, and many membrane proteins and surface molecules on the cell surface will interfere with phage panning. The binding of body, also can't localize its specific action target
In addition, the experiment was mainly conducted at the cellular level, lacking further verification by animal experiments

Method used

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  • Chemokine receptor 5 antagonist and pharmaceutical composition
  • Chemokine receptor 5 antagonist and pharmaceutical composition
  • Chemokine receptor 5 antagonist and pharmaceutical composition

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Embodiment Construction

[0016] Phage display technology is one of the commonly used technologies for the development of peptide drugs. Its conditions are very mature and commercial kits are available for sale. The key to research and development lies in the selection of target molecules and the verification of subsequent effects.

[0017] Studies have found that the physiological function of CCR5 is mainly realized through the N-terminus of the extracellular part and the second extracellular loop. The present invention checks the amino acid sequences of the first and second extracellular loops of rat CCR5 in the protein database, and the polypeptide biological The company conducts artificial synthesis, coats them in six-well plates, and pans the phage 7-peptide library to obtain heptapeptides that specifically bind to the first and second extracellular loops of CCR5. This protocol can directly locate the molecular structure of CCR5, avoiding the interference of other factors, and after the two heptape...

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Abstract

The invention provides a chemokine receptor 5 antagonist and a pharmaceutical composition. By a phage display technology, screening is carried out to obtain two small molecular active peptides, amino acid sequences of which are respectively GHWKVWL and HYIDFRW. The two polypeptides have a function of antagonizing a chemokine receptor 5 (CCR5) and have high medicinal value. The target molecule is directly located to a molecular structure of CCR5. The studied two heptapeptides are respectively against the first extracellular loop (ECL1) and the second extracellular loop (ECL2) of CCR5. The antagonistic mechanism is definite, and in vitro verification is successful. The invention provides an experimental basis for treatment effect observation of an animal model in the later period.

Description

technical field [0001] The invention relates to an antagonist of chemokine receptor 5 (CCR5) and a pharmaceutical composition containing the antagonist, in particular to a small molecule active peptide screened by phage display technology as the antagonist. Background technique [0002] Chemokine receptor 5 (CCR5) is a receptor for β chemokines, which has the function of regulating the migration, proliferation and immunity of T cells and monocyte / macrophage cell lines. CCR5 and its ligands mediate the chemotactic recruitment process of CCR5+ immune cells, which is closely related to the occurrence of various inflammatory diseases, such as multiple sclerosis, rheumatoid arthritis, atherosclerosis, transplant rejection and autoimmune diseases. In addition, CCR5 is also an important co-receptor when human immunodeficiency virus type 1 (HIV-I) invades the human body, and participates in the fusion process of virus and cell membrane: gp120 mainly interacts with its N-terminus and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C12N15/11A61K38/08A61P29/00A61P19/02A61P9/10A61P37/06A61P37/02A61P25/00
Inventor 钟英强刘思雪
Owner 钟英强
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