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Glutamine B16 insulin: Reduced insulin-like metabolic activity with moderately preserved mitogenic activity
Authors:Gerald P Schwartz  Diana Wong  G Thompson Burke  Monique A de Vroede  Matthew M Rechler and Panayotis G Katsoyannis
Institution:(1) Department of Biochemistry, Mount Sinai School of Medicine of the City University of New York, New York, New York;(2) Molecular, Cellular and Nutritional Endocrinology Branch, National Institute of Arthritis, Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland
Abstract:An analogue of insulin in which the naturally occurring tyrosine residue in position B16 is replaced by a glutamine residue has been synthesized. Glutamine appears in the corresponding position in the B-domain of the insulin-like growth factors. This analogue displays 9% of the potency of insulin in binding to the insulin receptor from rat liver plasma membranes, 17% in stimulating the conversion of 3-3H] glucose into lipids in rat adipocytes, and 23% in insulin radioimmunoassay, but 40% of the potency of insulin in stimulating DNA synthesis in cultured chick fibroblasts. The analogue is a more potent mitogen than is a hybrid molecule which contains the A-chain of insulin and the entire B-domain sequence of IGF-I.
Keywords:insulin analogue  insulin-like growth factor  metabolic assay  mitogenic assay  synthesis
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