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Preparation method of labeled biomacromolecules capable of being used for constructing DEL database

A bio-macromolecule and database technology, applied in the field of chemical biology, can solve the problems such as the inability to continue splicing fragments, the limitation of synthesis technology, and the limitation of library reaction types, so as to achieve the effect of expanding reaction types, simple reaction operation and good compatibility.

Pending Publication Date: 2021-07-13
苏州昆堃生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, due to the limitation of synthesis technology, the limitation of library reaction types, and in order to avoid unfavorable factors such as "inbreeding", it is usually impossible to continue splicing fragments in three to four dimensions.

Method used

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  • Preparation method of labeled biomacromolecules capable of being used for constructing DEL database

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preparation example Construction

[0020] A preparation method of a biomacromolecule modified by chemical molecular linkage, comprising the following steps:

[0021] Take type Japanese style The shown compound is dissolved in the solution, and under the action of the catalyst potassium bifluoride, in a buffer solution with a pH value of 4, the buffer solution is PBS buffer, and the generation formula later with Reaction in the same system, direct generation formula Shown compound, the chemical formula of reaction is as figure 1 Shown; Among them, R1 is a biological macromolecule, R2, R3 are small chemical molecules. Biological macromolecules refer to DNA, RNA, and protein. DNA refers to single-stranded or double-stranded DNA. Single-stranded DNA refers to a single-stranded polydeoxynucleotide containing 20-300 bases, and double-stranded DNA refers to a double-stranded deoxyribonucleic acid containing 20-300 base pairs. Generally speaking, during the reaction process, the reaction equivalent is 1 equ...

Embodiment 2

[0023] The difference between Example 2 and Example 1 is that the catalyst is sodium bifluoride, the pH value is 11, and the buffer solution is PBS buffer, which is mixed with acetonitrile at 1:1. It can be understood that the pH value is not limited to 11, but can also be 5, 6, 7, 8, 9, or 10.

Embodiment 3

[0025] A preparation method of a biomacromolecule modified by chemical molecular linkage, comprising the following steps:

[0026] Take type Japanese style The shown compound is dissolved in the solution, and under the action of the catalyst potassium bifluoride, in a buffer solution with a pH value of 4-11, the buffer solution is PBS buffer, and the generation formula later with Reaction in the same system, direct generation formula The compounds shown; wherein, R1 is a biological macromolecule, and R2 and R4 are small chemical molecules. Biological macromolecules refer to DNA, RNA, and protein. DNA refers to single-stranded or double-stranded DNA. Single-stranded DNA refers to a single-stranded polydeoxynucleotide containing 20-300 bases, and double-stranded DNA refers to a double-stranded deoxyribonucleic acid containing 20-300 base pairs. Generally speaking, during the reaction process, the reaction equivalent is 1 equivalent of biological macromolecule, 5-1000 ...

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Abstract

The invention relates to a preparation method of a labeled biomacromolecule for constructing a DEL database, and the method comprises the following steps: dissolving compounds shown in a formula A and a formula B in a solution, generating a formula C in a buffer solution with the pH value of 4-11 under the action of a catalyst, and then reacting with D or E in the same system to directly generate a compound shown in a formula 1 or 2, wherein R1 is a biological macromolecule, and R2, R3 and R4 are chemical micromolecules. According to the invention, on the basis of a bio-orthogonal connection technology based on the core linker iminosutur oxydifluoride, two fluorine groups of difluoride can be selectively combined with different amino groups and phenolic hydroxyl groups in DNA, and meanwhile, the compatibility of functional groups is good, so that the reaction types of a DNA coding compound library can be greatly expanded, and even, different small molecules can be connected in the three-dimensional space direction at the same high-valence sulfur center at the same time. The brand-new DNA coding compound library developed by the technology improves the possibility of finding a new drug lead compound with a brand-new structure.

Description

technical field [0001] The invention relates to the technical field of chemistry and biology, in particular to a method for preparing a labeled biomacromolecule that can be used to construct a DEL database. Background technique [0002] In the process of long and huge investment in new drug research and development, the most fundamental thing is the discovery and optimization of lead compounds. Moreover, the main challenge in the drug discovery process is how to quickly and high-quality find as many active compounds that can bind to target proteins as possible within a controllable cost range, which is a pain point and difficulty for the entire new drug development industry. . Traditional screening technologies face the disadvantages of slow screening speed, low spatial coverage of screening compounds, and inability to effectively screen some targets. In order to solve this problem, new drug companies are constantly improving and innovating screening methods. For example,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G16B20/00G16B45/00G16C10/00G16C20/50G16C20/62G16C20/80
CPCG16B20/00G16B45/00G16C10/00G16C20/50G16C20/62G16C20/80
Inventor 刘烽李雯刘子薰
Owner 苏州昆堃生物医药科技有限公司