Freidinger R M, Veber D F, Perlow D S, Brooks J R, Saperstein R
Science. 1980 Nov 7;210(4470):656-8. doi: 10.1126/science.7001627.
An analog of luteinizing hormone-releasing hormone containing a gamma-lactam as a conformational constraint has been 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 that the parent hormone, and provides evidence for a bioactive conformation containing a beta-turn.
一种含有γ-内酰胺作为构象限制的促黄体生成激素释放激素类似物,已通过甲硫氨酸锍盐的新型环化反应制备而成。该类似物作为促黄体生成激素释放激素激动剂比母体激素更具活性,并为含有β-转角的生物活性构象提供了证据。