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A polypeptide having cxcr4 protein agonistic activity and its application and pharmaceutical composition

A composition and drug technology, applied in the field of polypeptides with CXCR4 protein agonistic activity and their applications and pharmaceutical compositions, can solve the problems of lack of treatment methods

Active Publication Date: 2021-11-09
黄子为
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Neurological diseases such as multiple sclerosis, Alzheimer's disease, Parkinson's disease, Sandhoff disease, Tay-Sachs disease and stroke still lack effective treatments

Method used

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  • A polypeptide having cxcr4 protein agonistic activity and its application and pharmaceutical composition
  • A polypeptide having cxcr4 protein agonistic activity and its application and pharmaceutical composition
  • A polypeptide having cxcr4 protein agonistic activity and its application and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Example 1: Synthesis of H0001

[0083] Adopt Fmoc solid-phase synthesis method to synthesize, and concrete preparation method is as follows:

[0084] Weigh 357mg of Rink Amide-MBHA resin with a substitution degree of 0.28mmol / g in a solid phase reactor, add DCM to swell for 30min, then add 20% PIP / DMF solution for deprotection twice, the first time is 5min, and the second time is 20min . Wash several times with DCM and DMF respectively, and drain. It was detected by Kaiser test, and the resin or solution showed blue color, indicating that it had been deprotected.

[0085] Add Fmoc-D-Pro-OH (169mg, 0.5mmol), DIC (103mg, 0.5mmol), HOBt (68mg, 0.5mmol), DMF (4mL) into the solid phase reactor, and react at room temperature for 2h. After the coupling is completed, wash with DCM and DMF several times, and drain. Then use the Kaiser test to detect, and proceed to the next step after the detection is passed. Wash and dry the resin to obtain Fmoc-Pro-Rink Amide-MBHA resin. ...

Embodiment 2

[0088] The synthesis of embodiment 2 H0006

[0089] Weigh 357mg of Rink Amide-MBHA resin with a substitution degree of 0.28mmol / g in a solid phase reactor, add DCM to swell for 30min, then add 20% PIP / DMF solution for deprotection twice, the first time is 5min, and the second time is 20min . Wash several times with DCM and DMF respectively, and drain. It was detected by Kaiser test, and the resin or solution showed blue color, indicating that it had been deprotected.

[0090]Add Fmoc-Lys(Dde)-OH (266mg, 0.5mmol), DIC (103mg, 0.5mmol), HOBt (68mg, 0.5mmol), DMF (4mL) into the solid phase reactor, and react at room temperature for 2h. After the coupling is completed, the resin is washed and dried to obtain Fmoc-Lys(Dde)-Rink Amide-MBHA resin. The Kaiser test is used for detection, and the next reaction is carried out after the detection is passed. Add 20% PIP / DMF solution for deprotection twice, the first time is 5 minutes, the second time is 20 minutes, and the Fmoc protect...

Embodiment 3

[0095] Embodiment 3: polypeptide compound of the present invention

[0096] The amino acid sequence of the CXCR4 activity regulating polypeptide is shown in Table 1, and was synthesized according to the method described in Example 1 or Example 2.

[0097] Table 1 CXCR4 activity regulating polypeptide and its amino acid sequence

[0098]

[0099] a Italics represent D-type amino acids

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PUM

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Abstract

The invention relates to the technical field of biomedicine, in particular to a polypeptide with CXCR4 protein activating activity and its application and pharmaceutical composition. The fragments in the polypeptide are selected from the polypeptide sequences derived from vMIP-II consisting of any arrangement of 3 amino acids to the full-length sequence, and the polypeptide sequences derived from SDF-1α (CXCL12) consisting of any arrangement of 3 amino acids to the full-length sequence peptide sequence. The polypeptide of the invention can effectively induce the migration of SupT1 cells, and can trigger the increase of intracellular calcium flow after being combined with CXCR4, indicating that the polypeptide has CXCR4 protein agonist activity and can be used as a CXCR4 protein agonist.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a polypeptide with CXCR4 protein activating activity and its application and pharmaceutical composition. Background technique [0002] Chemokine receptor CXCR4 belongs to the G protein-coupled receptor (G-protein-coupled receptor, GPCR) superfamily. Similar to other G protein-coupled receptors, CXCR4 consists of an extracellular N-terminus, seven transmembrane helices, three extracellular loop regions connecting the transmembrane helices, three intracellular loop regions, and an intracellular C-terminus. Unlike other chemokine receptors, only two endogenous natural ligands of CXCR4 have been found, namely chemokine stromal cell-derived factor (SDF-1α, CXCL12) and ubiquitin. After SDF-1α binds to the receptor CXCR4, it can activate multiple downstream signaling pathways, mediate cell proliferation, migration, homing, memory and transport of hematopoietic and lymphoid stem cel...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K19/00G01N33/68G01N33/574A61K38/19A61P25/28A61P25/00A61P35/00A61P37/00A61P31/18
CPCA61K38/00C07K14/522C07K2319/00G01N33/574G01N33/68
Inventor 黄子为
Owner 黄子为
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