摘要
As a 37-amino acid vasoactive neuropeptide, calcitonin gene-related peptide （CGRP） is widely distributed in nervous systems. The studies and clinical applications of CGRP are limited by its peptide nature and short half-life. A series of peptide analogues of the α-form of CGRP were synthesized. Afterwards, by using in vitro metabolic and activity studies, we prepared two high affinity analogues with significantly improved plasma stability.
降钙素基因相关肽(CGRP)是一种广泛分布于神经系统的神经肽,由37个氨基酸组成。CGRP较短的半衰期阻碍了其研究和应用。本文利用固相多肽合成技术和无铜点击化学合成了多个脂肪酸修饰的CGRP衍生物,并对其进行了体外稳定性和活性的评价,筛选得到两种稳定性得到显著提高且具有高亲和力的衍生物。
