Bioactive conformation of luteinizing hormone-releasing hormone: evidence from a conformationally constrained analog

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Science  07 Nov 1980:
Vol. 210, Issue 4470, pp. 656-658
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.