Somatostatin

Literature References: Widely occurring cyclic tetradecapeptide that mediates, together with somatoliberin, q.v., the neuroregulation of somatotropin secretion. Inhibits release of growth hormone, insulin and glucagon. Also a potent inhibitor in a number of systems, including central and peripheral neural, gastrointestinal, and vascular smooth muscle. Isoln from ovine hypothalamic extracts: P. Brazeau et al., Science 179, 77 (1973). Structure: Burgus et al., Proc. Natl. Acad. Sci. USA 70, 684 (1973); Ling et al., Biochem. Biophys. Res. Commun. 50, 127 (1973). Synthesis: Rivier et al., C.R. Seances Acad. Sci. Ser. D 276, 2737 (1973); Sarantakis, McKinley, Biochem. Biophys. Res. Commun. 54, 234 (1973); Yamashiro, Li, ibid. 882; Coy et al., ibid. 1267; A. M. Felix et al., Int. J. Pept. Protein Res. 15, 342 (1980); B. Hartrodt et al., Pharmazie 37, 403 (1982). Synthesis and bacterial expression of somatostatin gene: K. Itakura et al., Science 198, 1056 (1977); K. Itakura, A. D. Riggs, BE 871782; K. Itakura, US 4356270; A. D. Riggs, US 4366246 (1979, 1982, 1982 all to Genentech). Isoln of a 28-amino acid somatostatin, termed SRIF-28, from porcine gastrointestinal tract: L. Pradayrol et al., Biochem. Biophys. Res. Commun. 85, 701 (1978). Primary structure: eidem, FEBS Lett. 109, 55 (1980). Synthesis: E. Wunsch, Z. Naturforsch. 35B, 911 (1980). Isoln of a 25-amino acid somatostatin, SRIF-25, and structure: P. Brazeau et al., C.R. Seances Acad. Sci. Ser. D 290, 1369 (1980). Both of these peptides consist of an N-terminal extension of SRIF-14. They are more potent than SRIF-14 in inhibition of insulin release but less potent in inhibition of glucagon release: L. Mandarino et al., Nature 291, 76 (1981). Synthetic linear SRIF-14 exhibits the same bioactivity as the natural cyclic form: P. Brazeau et al., Endocrinology 94, 184 (1974). Activity studies in humans: T. M. Siler et al., J. Clin. Endocrinol. Metab. 37, 632 (1973). Inhibitory effects on the secretion of thyrotropin: Vale et al., Fed. Proc. 32, 211 (1973); of insulin: K. G. Alberti et al., Lancet 2, 1299 (1973); Koeker et al., Science 184, 482 (1974). Role in diabetes: Maugh, ibid. 188, 920 (1975). Clinical trial in controlling acute variceal hemorrhage: S. A. Jenkins et al., Br. Med. J. 290, 275 (1985). Review of distribution, secretion, physiology of gastrointestinal somatostatin: C. H. S. McIntosh, Life Sci. 37, 2043-2058 (1985). Symposium of biosynthesis, bioactivity, and clinical applications: Adv. Exp. Med. Biol. 188, 1-524 (1985). Reviews: Vale et al., Recent Prog. Horm. Res. 31, 365-397 (1975); Guillemin, Gerich, Annu. Rev. Med. 27, 379-388 (1976); R. L. Moss, Annu. Rev. Physiol. 41, 617 (1979); A. Arimura, J. B. Fishback, Neuroendocrinology 33, 246-256 (1981); several authors in Gut Hormones, S. R. Bloom, J. M. Polack, Eds. (Churchill, New York, 2nd ed., 1981) 605 pp; S. M. McCann, Annu. Rev. Pharmacol. Toxicol. 22, 491-515 (1982); N. Bethge et al., J. Clin. Chem. Clin. Biochem. 20, 603-613 (1982). Book: Somatostatin Vol. 2, M. T. McQuillan, Ed. (Eden Press, Quebec, 1980) 238 pp.