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  • 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.

Science (New York, N.Y.) (1980-11-07)
R M Freidinger, D F Veber, D S Perlow, J R Brooks, R Saperstein
PMID7001627
ABSTRACT

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.