Structure activity studies on somatostatin.

作者: D. SARANTAKIS , W. A. McKINLEY , I. JAUNAKAIS , D. CLARK , N. H. GRANT

DOI: 10.1111/J.1365-2265.1976.TB03835.X

关键词: EndocrinologyPlasma glucagonInsulinPlasma growth hormoneGrowth hormone secretionInternal medicineSomatostatinBiology

摘要: SUMMARY Seven synthetic analogues of somatostatin helped clarify structural requirements for suppression growth hormone secretion in rats. Size the ring is not critical; deletions serine-13, lysine-4 or asparagine-5 result peptides which retain an appreciable fraction activity. The analogue des-Ala1, Gly2, Asn5-somatostatin lowers plasma and insulin levels without affecting glucagon significantly.

参考文章(11)
D. Sarantakis, W.A. McKinley, Total synthesis of hypothalamic “somatostatin” Biochemical and Biophysical Research Communications. ,vol. 54, pp. 234- 238 ,(1973) , 10.1016/0006-291X(73)90913-3
R Dobbs, H Sakurai, H Sasaki, G Faloona, I Valverde, D Baetens, L Orci, R Unger, Glucagon: role in the hyperglycemia of diabetes mellitus. Science. ,vol. 187, pp. 544- 547 ,(1975) , 10.1126/SCIENCE.1089999
P. Brazeau, W. Vale, R. Burgus, N. Ling, M. Butcher, J. Rivier, R. Guillemin, Hypothalamic Polypeptide That Inhibits the Secretion of Immunoreactive Pituitary Growth Hormone Science. ,vol. 179, pp. 77- 79 ,(1973) , 10.1126/SCIENCE.179.4068.77
G.W. DeVane, T.M. Siler, S.S.C. Yen, Acute suppression of insulin and glucose levels by synthetic somatostatin in normal human subjects. The Journal of Clinical Endocrinology and Metabolism. ,vol. 38, pp. 913- 915 ,(1974) , 10.1210/JCEM-38-5-913
F.P. Alford, S.R. Bloom, J.D.N. Nabarro, R. Hall, G.M. Besser, D.H. Coy, A.J. Kastin, A.V. Schally, GLUCAGON CONTROL OF FASTING GLUCOSE IN MAN The Lancet. ,vol. 304, pp. 974- 977 ,(1974) , 10.1016/S0140-6736(74)92071-6
K.G.M.M. Alberti, N. Juel Christensen, S. Engkjær Christensen, AA. Prange Hansen, J. Iversen, K. Lundbæk, K. Seyer-Hansen, H. Ørskov, INHIBITION OF INSULIN SECRETION BY SOMATOSTATIN The Lancet. ,vol. 302, pp. 1299- 1301 ,(1973) , 10.1016/S0140-6736(73)92873-0
S.R Bloom, C.H Mortimer, M.O Thorner, G.M Besser, R Hall, A Gomez-Pan, V.M Roy, R.C.G Russell, D.H Coy, A.T Kastin, A.V Schally, INHIBITION OF GASTRIN AND GASTRIC-ACID SECRETION BY GROWTH-HORMONE RELEASE-INHIBITING HORMONE The Lancet. ,vol. 304, pp. 1106- 1109 ,(1974) , 10.1016/S0140-6736(74)90869-1
R. B. Merrifield, Solid phase peptide synthesis. I. the synthesis of a tetrapeptide Journal of the American Chemical Society. ,vol. 85, pp. 2149- 2154 ,(1963) , 10.1021/JA00897A025