BIOACTIVE CONFORMATION OF LUTEINIZING-HORMONE-RELEASING HORMONE - EVIDENCE FROM A CONFORMATIONALLY CONSTRAINED ANALOG
BIOACTIVE CONFORMATION OF LUTEINIZING-HORMONE-RELEASING HORMONE - EVIDENCE FROM A CONFORMATIONALLY CONSTRAINED ANALOG
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DOI：
10.1126/science.7001627
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发表时间：
1980-01-01
期刊：
影响因子：
56.9
通讯作者：
SAPERSTEIN, R
中科院分区：
文献类型：
--
作者：
FREIDINGER, RM;VEBER, DF;SAPERSTEIN, R
使用甲硫氨酸锍盐的新型环化制备含有γ-内酰胺作为构象约束的黄体生成素释放激素[luliberin]的类似物。作为黄体生成素释放激素激动剂，该类似物比母体激素[用雌二醇和黄体酮引发的切除卵巢的大鼠中促黄体生成素的释放]更活跃，并且为含有β-转角的生物活性构象提供了证据。
An analog of luteinizing hormone-releasing hormone [luliberin] containing a .gamma.-lactam as a conformational constraint was prepared with the use of a novel cyclization of a methionine sulfonium salt. The analog is more active as a luteinizing hormone-releasing hormone agonist than the parent hormone [lutropin release in ovariectomized rats primed with estradiol and progesterone], and provides evidence for a bioactive conformation containing a .beta.-turn.