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在肽类药物的研究中,合成具有特殊结构的天然肽类似物,是探索肽结构与功能关系的重要方法,也是寻找高效低毒肽类药物的重要途径。这种工作大致可从几个方面进行:1.改变肽的主链结构。在肽链中引入其他化学键,如将酰胺键的羰基变为硫羰基等。2.改变氨基酸残基的侧链结构。如引入非天然氨基酸或对天然氨基酸侧链进行化学修饰等。3.肽链中引入D型氨基酸能有效地抑制体内蛋白酶对肽链的水解,也能改变肽的构象。
In the study of peptide drugs, the synthesis of natural peptide analogues with special structure is an important method to explore the relationship between structure and function of peptides, and also an important way to find efficient and low toxicity peptide drugs. This work can generally be carried out from several aspects: 1. Change the peptide backbone structure. In the peptide chain into other chemical bonds, such as the amide bond carbonyl to thiocarbonyl and so on. 2. Change the side chain structure of amino acid residues. Such as the introduction of unnatural amino acids or chemical modification of the side chains of natural amino acids. 3. Introduction of D-type amino acids in the peptide chain can effectively inhibit the hydrolysis of peptide chains in the body protease, but also change the peptide conformation.