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1-sphingosine phosphate receptor 3 agonist as well as preparation method and application thereof

A sphingosine phosphate and agonist technology, applied in the field of biomedicine, can solve problems such as limited value, and achieve the effects of enhancing cell entry ability, excellent water solubility and permeability, and good cell membrane permeability

Pending Publication Date: 2020-08-07
NINGBO FIRST HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, GPS-725.017 is insoluble in water, which greatly limits its value in basic research and clinical transformation

Method used

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  • 1-sphingosine phosphate receptor 3 agonist as well as preparation method and application thereof
  • 1-sphingosine phosphate receptor 3 agonist as well as preparation method and application thereof
  • 1-sphingosine phosphate receptor 3 agonist as well as preparation method and application thereof

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Embodiment 1

[0050] The sphingosine-1-phosphate receptor 3 agonist GLD-001 of the present invention is entrusted to Nanjing GenScript Biotechnology Co., Ltd. to synthesize; its preparation method includes the following steps:

[0051] (1) Polypeptide G{Nle}RPY was synthesized by Fmoc solid-phase synthesis method;

[0052] Specifically, including:

[0053] (a) Feed 2-chlorotrityl chloride resin into the solid-phase synthesis reaction tube, add dichloromethane (DCM), and oscillate for 30 minutes to swell the resin;

[0054] (b) After removing the dichloromethane in the solid-phase synthesis reaction tube, add excess Fmoc-protected tyrosine, then add N,N-dimethylformamide (DMF) to fully dissolve, then add excess diiso Propylethylamine (DIEA), shake for 1h, finally block with methanol, and extract N,N-dimethylformamide;

[0055] (c) Add deprotection solution (DMF containing 20% ​​piperidine) to the solid-phase synthesis reaction tube, remove the reaction solution after fully shaking, and add...

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Abstract

The invention discloses a sphingosine 1-phosphate receptor 3 agonist as well as a preparation method and the application thereof. The S1PR3 agonist comprises a polypeptide, and a water solubility enhancing part and a permeability enhancing part which are sequentially coupled to the N end of the polypeptide, the polypeptide has an amino acid sequence as shown in SEQ ID No. 1. A water solubility enhancing part and a permeability enhancing part are sequentially coupled to the N end of the polypeptide, the 1-sphingosine phosphate receptor 3 agonist has good cell membrane permeability through the permeability enhancing part, and the intracellular capacity of the polypeptide is enhanced; due to the water solubility enhancing part, the sphingosine 1-phosphate receptor 3 agonist has excellent water solubility, and the solubility of the sphingosine 1-phosphate receptor 3 agonist in ultrapure water can reach 5mg / mL. The sphingosine 1-phosphate receptor 3 agonist disclosed by the invention has excellent water solubility and permeability, and the application of the sphingosine 1-phosphate receptor 3 agonist in fundamental research and clinical transformation is greatly expanded.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a sphingosine-1-phosphate receptor 3 agonist and a preparation method and application thereof. Background technique [0002] Sphingosine-1-phosphate receptors (S1PRs) are a class of seven transmembrane G protein-coupled receptors, which interact with the natural ligand sphingosine-1-phosphate (Sphingosine-1-phosphate, After the combination of S1P), it can initiate the cell transmembrane signal transduction effect, and then widely participate in physiological processes such as angiogenesis, cell proliferation and immune regulation in the human body. Among them, sphingosine-1-phosphate receptor 3 (S1PR3), as a key member of the S1PRs superfamily, is widely expressed in endothelial cells, vascular smooth muscle cells, and macrophages, and activates the mitogen-activated protein kinase (MAPKs) signaling pathway , thereby regulating angiogenesis and immune inflammator...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/04C07K1/06A61K47/60A61K47/54A61K38/08A61P37/02A61P9/14A61P35/00
CPCA61K38/08A61K47/542A61K47/60A61P9/14A61P35/00A61P37/02C07K7/06
Inventor 郑君刚黄长顺王俊王伟飞曹刚陈轶尘徐磊周海东宗一卢子会卢剑
Owner NINGBO FIRST HOSPITAL
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