Complete chemical synthesis for lasso polypeptide

A lasso and chemical technology, applied in the field of synthesis of lasso polypeptides and their analogs, can solve the problems of rapid increase in marketization cost and difficulty of popularization, unfavorable drug research and development screening and modification, poor controllability of lasso polypeptide synthesis, etc. Achieve the effect of being conducive to automation and large-scale synthesis, easy to control, and simple steps

Active Publication Date: 2017-05-31
陈铭
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Problems solved by technology

This situation has resulted in poor controllability and unautomation of the synthesis of lasso polypeptides, which is not conducive to the scree

Method used

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  • Complete chemical synthesis for lasso polypeptide
  • Complete chemical synthesis for lasso polypeptide
  • Complete chemical synthesis for lasso polypeptide

Examples

Experimental program
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Embodiment

[0035] The target product is the natural lasso polypeptide BI-32169 with glucagon receptor antagonist, the sequence and the spatial configuration of the computer simulation are as follows figure 2 shown. Wherein, G in the sequence line is glycine, L is leucine, P is proline, W is tryptophan, C is cysteine, S is serine, D is aspartic acid, and I is isoleucine Amino acid, N is asparagine, T is threonine, A is alanine.

[0036] Step 1, the loading of the first amino acid in the ionic liquid. The imidazole ionic liquid 1,3-dimethyl-2-hydroxymethylimidazolium tetraphenylborate is used as the initial support, and the structural formula is: 1.0 equivalent (110.0 μL) of ionic liquid was dissolved in 1.2 mL of dichloromethane, and 2.0 equivalent of fluorenylmethoxycarbonyl-protected cysteine ​​was added. After stirring and dissolving, 4.0 equivalents of condensing agent N,N'-dicyclohexylcarbodiimide and 1.0 equivalents of catalyst 4-dimethylaminopyridine were added. After stirrin...

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Abstract

The invention relates to a complete chemical synthesis method for realizing lasso polypeptide and analogues thereof through the support of multiple anchor points. The support of multiple anchor points is preferably selected from a cryptand-ion liquid compound. The trend of a polypeptide chain is controlled through the limitation and guiding of the connecting point, so as to form a topological lasso structure. The synthesis method provided by the invention is easily automated; the marketing of the lasso polypeptide drugs becomes possible; the complete chemical synthesis of the lasso polypeptide and analogues thereof is firstly realized; the domestic and overseas blank of the chemical synthesis of the lasso polypeptide at present can be filled up; the method has significance in chemically synthesizing the polypeptide and researching and developing the polypeptide drug.

Description

[0001] Technical field: [0002] The invention relates to the technical field of biochemical synthesis, in particular to a synthesis method of lasso polypeptide and its analogues. This synthetic method uses multi-anchor compound support to realize the first chemical total synthesis of lasso polypeptide or lasso polypeptide analogues, which can be used to synthesize lasso cyclic peptides and their analogues that are difficult to synthesize by traditional chemical methods or biological methods, and has great impact on peptide chemistry. development is important. [0003] Background technique: [0004] Lasso peptides are a class of natural peptide molecules with a topological lasso configuration. Named for its lasso-like configuration, it usually contains an N-terminal peptide ring connected by an isopeptide bond, and a C-terminal peptide chain tail is extended from the peptide ring through a peptide bond connection; the peptide chain tail turns from itself through the peptide l...

Claims

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Application Information

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IPC IPC(8): C07K1/00
CPCC07K1/00C07K7/56
Inventor 陈铭
Owner 陈铭
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