多肽酰肼法合成Nesiritide

Synthesis of Nesiritide via Ligation of Peptide Hydrazide

Nesiritide是一类重要的多肽类血管扩张药物,在维持心血管和肾脏的体内平衡方面发挥着重要的作用.目前,Nesiritide的合成主要是通过基因重组表达法获得,该方法操作较为复杂且存在一定的限制.本研究运用多肽固相合成及酰肼连接策略,通过3片段连接高效合成了Nesiritide,为大批量工业化生产该类多肽药物打下基础.

Nesiritide is an important class of peptide vasodilator. It plays a significant role in the maintenance homeostasis of cardiovascular and kidney. Nowadays, nesiritide is mainly obtained by biological methods including gene recombinant ex- pression, which is relative time-consuming. In present work, the chemical synthesis of nesiritide was reported by using （solid-phase peptide synthesis） （SPPS） strategy combining with the ligation ofpeptide hydrazides with high yield and purity. Therefore, it was considered that the method presented here provided a convinced alternative for acquiring pharmaceutical peptide in a large scale.