Novel long-lasting kisspeptin derivatives stimulate luteinizing hormone secretion in bovine

Kisspeptin是一种肽激素，通过刺激垂体促黄体生成素（LH）作为生殖轴的主要正调节因子。为了开发新药，本研究考察了牛kisspeptin c端残基的各种修饰是否能增强其刺激lh的能力，并具有持久的药理作用。与未修饰的kisspeptin相比，部分修饰对培养牛垂体细胞LH分泌的诱导程度更大，持续时间更长。接下来，我们尝试将最佳候选新药注射到小母牛和产后奶牛体内。虽然对产后奶牛的黄体生成素分泌没有显著影响，但对母牛的黄体生成素分泌有刺激作用。因此，我们开发了新的长效kisspeptin衍生物，刺激牛黄体生成素的分泌。

Kisspeptin is a peptide hormone that acts as the principal positive regulator of the reproductive axis by stimulating luteinizing hormone (LH) from pituitary. In order to develop new medicine, this study investigated whether various modification of the C-terminal residue of bovine kisspeptin can potentiate the LH-stimulating ability, and have long-lasting pharmacological effects. Some of modification induced the secretion of LH from cultured bovine pituitary cells to a greater degree and longer-lasting than unmodified kisspeptin. In next, we tried to inject the best candidate of new drugs into heifers and postpartum dairy cows. The best candidate stimulated LH secretion in heifers, although it had no significant effect on LH secretion in postpartum dairy cows. Therefore, we developed novel long-lasting kisspeptin derivatives stimulate luteinizing hormone secretion in bovine.