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Eph kinase polypeptide inhibitor and application thereof

A technology of kinase inhibition and amino acid, applied in the biological field, to achieve the effect of inhibiting tumor angiogenesis, high stability, and efficient inhibition

Active Publication Date: 2016-08-31
ZHUHAI NOBEL INST OF BIOMEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no small-molecule anti-tumor drug that inhibits the binding of ephrin ligands to Eph receptors to inhibit the activity of Eph kinase

Method used

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  • Eph kinase polypeptide inhibitor and application thereof
  • Eph kinase polypeptide inhibitor and application thereof
  • Eph kinase polypeptide inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1 Polypeptide compound of the present invention and its synthesis

[0045] The amino acid sequence of Eph kinase polypeptide inhibitor NI-E-00005 is: Tyr-Asn-Tyr-Leu-Phe-Ser-Pro-Asn-Gly-Pro-Ile-Ala-His-Ala-Trp-NH 2 (SEQ ID NO:5), synthesized by the following route.

[0046]

[0047] 1. It is synthesized by Fmoc solid-phase synthesis method.

[0048] Weigh 714mg 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. Add Fmoc-Trp(Boc)-OH (426mg, 1mmol), HOBt (135mg, 1mmol), DIC (126mg, 1mmol), DMF (6mL) into the solid phase reactor, and react at room temperature for 2h. Wash and dry the resin to obtain Fmoc-Trp(Boc)-Rink Amide-MBHA resin. Add 20% PIP / DMF solution for deprotection twice, the first time is 5 minutes, the sec...

Embodiment 2

[0051] Embodiment 2 Polypeptide compound of the present invention and synthesis

[0052] Amino acid sequence of Eph kinase polypeptide inhibitor NI-E-00013 Tyr-Asn-Tyr-Leu-Phe-Ser-Pro-Asn-Gly-Pro-Ile-Ala-His-Ala-Trp-Ahx-Lys(Biotin)- NH 2 (SEQ ID NO:6), synthesized by the following route.

[0053]

[0054] 1. It is synthesized by Fmoc solid-phase synthesis method.

[0055] Weigh 357 mg of Rink Amide-MBHA resin with a substitution degree of 0.28 mmol / g in a solid phase reactor, add DCM to swell for 30 min, then add 20% PIP / DMF solution for deprotection twice, and react for 5 min and 20 min respectively. Wash several times with DCM and DMF respectively, and drain. Add Fmoc-Lys(Biotin)-OH (297.4mg, 0.5mmol), HOBt (67.5mg, 0.5mmol), DIC (63mg, 0.5mmol), DMF (4mL) to the solid phase reactor, and react in the dark for 2h at room temperature . Wash and dry the resin to obtain Fmoc-Lys(Biotin)-Rink Amide-MBHA resin. Then add 20% PIP / DMF solution twice for deprotection, and rea...

Embodiment 3

[0058] Embodiment 3 The polypeptide compound of the present invention

[0059] The amino acid sequence of the Eph kinase polypeptide inhibitor is shown in Table 1, and was synthesized according to the method described in Example 1 or Example 2.

[0060] Table 1 Eph Kinase Polypeptide Inhibitors

[0061]

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PUM

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Abstract

The invention belongs to the technical field of biology and specifically discloses an Eph kinase polypeptide inhibitor and application thereof. The polypeptide disclosed by the invention is as shown in formula I. The polypeptide disclosed by the invention has a highly efficient inhibiting effect on Eph kinase, has higher stability and can be used for preparing medicine for treating or preventing Eph kinase abnormal expression related diseases. The polypeptide disclosed by the invention inhibits formation of tumor vasculature through inhibiting abnormal expression of Eph kinase, thereby playing the effect of anti-tumor growth, and the polypeptide can be used for preparing medicine for treating cancer.

Description

technical field [0001] The invention belongs to the field of biotechnology, in particular to an Eph kinase polypeptide inhibitor and its application. Background technique [0002] Angiogenesis is a process involving the accumulation of newly formed hemangioblasts into the original vascular plexus, and then undergoes proliferation, migration, sprouting and other reconstructions to form new blood vessels and vascular networks. Under physiological or pathological conditions, angiogenesis is related to processes such as embryonic development and growth, inflammatory response, wound healing, and the occurrence of tumor-diabetic retina. Angiogenesis is one of the necessary conditions for tumor growth and metastasis. It not only provides the necessary oxygen and nutrients for tumor growth, but also excretes metabolites. Therefore, anti-tumor angiogenesis has become a new strategy for tumor treatment. [0003] The receptor tyrosine kinase Eph and its ligand ephrins play important ...

Claims

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Application Information

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IPC IPC(8): C07K7/08A61K38/10A61P35/00A61P35/02A61P9/00A61P25/00
Inventor 黄子为
Owner ZHUHAI NOBEL INST OF BIOMEDICINE CO LTD
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