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      Inactivation of Two Hyperactive LH-RH Analogues by Rat Hypothalamic Peptidases

      ,

      Hormone Research in Paediatrics

      S. Karger AG

      Hypothalamus, Peptidases, LH-RH, Analogues

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          Abstract

          Hyperactive analogues of luteinizing hormone-releasing hormone (LH-RH) are believed to derive their properties from either increased binding affinity to anterior pituitary receptor sites or through decreased susceptibility to enzymic degradation. To investigate the latter suggestion and to examine the possible sites of action of hypothalamic peptidases inactivating LH-RH, D-Ser(TBU)<sup>6</sup>-EA<sup>10</sup>-LH-RH and D-Leu<sup>6</sup>-EA<sup>10</sup>-LH-RH, which are known to have considerably greater activity than LH-RH, were incubated with a hypothalamic supernatant fraction containing active peptidases degrading LH-RH, and their gonadotrophin-releasing ability after incubation with the enzymes was tested in normal, adult male rats; LH-RH was also tested in the same way. From a comparison of the relative losses of biological activity, both the LH-RH analogues treated proved to be more resistant to the hypothalamic peptidases than LH-RH itself: the D-Leu<sup>6</sup>-EA<sup>10</sup>-LH-RH retained its gonadotrophin-releasing activity longer than the D-Ser(TBU)<sup>6</sup>-EA<sup>10</sup>-LH-RH. These findings indicate that increased activity of the analogues may, in part, be due to increased resistance to enzymic inactivation and suggest initial sites of cleavage at the Gly-Leu and Pro-Gly NH<sub>2 </sub>bonds in the LH-RH decapeptide by the hypothalamic enzymes. Studies on the action of peptidases on LH-RH and its analogues may yield useful information in the design of peptides with increased biological activity.

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          Author and article information

          Journal
          HRE
          Horm Res Paediatr
          10.1159/issn.1663-2818
          Hormone Research in Paediatrics
          S. Karger AG
          1663-2818
          1663-2826
          1979
          1979
          25 November 2008
          : 10
          : 5
          : 233-242
          Affiliations
          Department of Physiology, University of Manchester, Manchester, and Frauenklinik, Universität Marburg, Marburg a.d. Lahn
          Article
          179005 Horm Res 1979;10:233–242
          10.1159/000179005
          378806
          © 1979 S. Karger AG, Basel

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          Pages: 10
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