Polypeptide, and synthesis method and application thereof

A synthesis method and sequence technology, applied in the field of peptides and their synthesis, can solve the problems of limiting clinical application potential and test failure, and achieve the effects of excellent in vivo stability, small in vivo side effects, and enhanced performance

Active Publication Date: 2020-08-25
陕西未来多肽生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, so far, no MDM2 antagonists targeting this target have been approved for marketing, and some inhibitors have limited their clinical application potential due to limited efficacy in preclinical studies. Potential drugs at the point of failure in clinical trials due to toxic effects

Method used

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  • Polypeptide, and synthesis method and application thereof
  • Polypeptide, and synthesis method and application thereof
  • Polypeptide, and synthesis method and application thereof

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Experimental program
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Embodiment 1

[0046] Experimental Materials and Instruments

[0047] Table 1 Experimental reagents and manufacturers

[0048]

[0049]

[0050] Table 2 Experimental equipment and manufacturers

[0051] equipment manufacturer Full wavelength microplate reader Tecan Flow Cytometry Beckman Laser scanning confocal microscope CLSMFV1200Olympus Chemiluminescence Imaging System Shanghai Qinxiang Scientific Instrument Co., Ltd.

[0052] 1. D Preparation of MSNs

[0053] Step 1: According to the designed sequence, carry out amino acid weighing; use Boc chemical solid-phase peptide synthesis method or Fmoc method to synthesize D PMI β , D PMI β The sequence is: D T D A D W D Y D A D N D f D E. D K D L D L D R.

[0054] Step 2: use DiscoveryStudio2.5 software to D PMI β Flip along the X axis with Cartesian coordinates to get the mirror counterpart L PMI β .

[0055] Step 3: Put L PMI β Topologically grafted onto the α-helical ...

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Abstract

The present invention discloses a polypeptide, and a synthesis method and an application thereof. An amino acid sequence of the polypeptide is shown in SEQ ID NO.1. The synthesis method of the polypeptide consists of the following steps: flipping <D>PMI<beta> along an X axis with Cartesian coordinates to obtain a mirror image counterpart <L>PMI<beta>; grafting the <L>PMI<beta> topology onto an alpha helix region of Apamin to obtain the Apamin grafted with the <L>PMI<beta>; converting the Apamin of the <L>PMI<beta> into Apamin of the <D>PMI<beta>; asparagine at 2nd position in the Apamin ring of the <D>PMI<beta> is mutated to arginine and D-enantiomeric small protein supermolecule nanoparticles are self-assembled under action of hydrophobic interaction and hydrogen bonding; after two-step disulfide bond oxidation, the target polypeptide DMSN is chemically synthesized by Fmoc, and the amino acid sequence of the target peptide DMSN is shown in the SEQ ID NO.1. The polypeptide is used to inhibit growth of cancer cells, has long-acting in vivo circulation time, and has advantages of strong specificity, high targeting, and in-vivo side effects compared with traditional small molecule drugs of the target.

Description

technical field [0001] The invention belongs to the field of biomedicine and anticancer, and in particular relates to a polypeptide and its synthesis method and application. Background technique [0002] Malignant tumors have become one of the major diseases that are increasingly common and seriously threaten human life and quality of life. Primary hepatic carcinoma (PHC) is a malignant tumor caused by abnormal proliferation of liver cells. It has high malignancy, rapid disease progression, poor prognosis, and often endangers the lives of patients. Its mortality rate ranks fifth among malignant tumors in my country. Colorectal cancer and liver cancer are both digestive tract tumors, and are among the top 10 malignant tumors in my country. It can be seen that digestive tract tumors closely related to diet have seriously threatened the health of Chinese residents. At present, the clinical treatment methods for liver cancer and colorectal cancer at home and abroad are mainly s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K38/10A61P35/00
CPCA61K38/00A61P35/00C07K7/08
Inventor 何旺骁闫瑾高汝青
Owner 陕西未来多肽生物科技有限公司
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