Chemical Total Synthesis of Lasso Polypeptide

Abstract

A cryptand-ionic liquid supported method for the first totally chemical synthesis of lasso peptide BI-32169 and its analogs is described. Cryptand-ionic liquid supported technique has been proved to be a powerful and controllable synthetic tool for producing or modifying chemically engineered lasso-shaped peptides and studying structure-activity relationships of lasso peptides as well. Thus, it is highly desirable that this synthetic strategy with designable multi-linker support could benefit the expansion of diverse lasso peptide libraries for discovery of novel bioactive peptides.

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. Background technique: [0003] 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 loop. Ge...

AI Technical Summary

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 screening and modification of drug research and development, and the cost of marketization and the difficulty of popularization have increased sharply

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