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Synthesis and biological activity of glycosylated analogs of somatostatin
Authors:S Lavielle  N Ling  P Brazeau  R Benoit  T Wasada  D Harris  R Unger  R Guillemin
Affiliation:1. Laboratories for Neuroendocrinology Salk Institute for Biological Studies La Jolla, California 92037 USA;2. Southwestern Medical School University of Texas Dallas, Texas 75235 USA
Abstract:The synthesis by solid-phase methodology of two glycosylated analogs of somatostatin [Glc-Asn5]-SS and [NAcGlc-Asn5]-SS is described. These two analogs have been biologically tested on the secretion of pituitary growth hormone, pancreatic glucagon and insulin. The results show that glycosylation of somatostatin on the Asn5 residue decreases by a hundred fold the inhibition activity on GH release when tested invitro. Invivo, since the activity is similar to somatostatin the carbohydrates are probably removed by some enzymatic reaction and thus liberate the full activity of somatostatin.
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