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Endocrinology, Vol 108, 2409-2411, Copyright © 1981 by Endocrine Society

ARTICLES

Insulin receptor down-regulation, prevention at a post-receptor site

S Filetti, NA Takai and B Rapoport

Nicotinamide (50mM) prevented insulin-mediated down-regulation of insulin receptors in IM-9 lymphoblastoid cells. Half-maximum effectiveness was between 10 and 33mM. Nicotinamide did not influence insulin binding to the cells, cell viability, insulin degradation or protein synthesis. A variety of inhibitors of ADP-ribosylation reactions besides nicotinamide, most of them pyridine analogues, similarly prevented insulin-induced receptor loss. Spermine decreased the number of insulin receptors in IM-9 cells, but this effect was not inhibited by nicotinamide.


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M Kasuga, F. Karlsson, and C. Kahn
Insulin stimulates the phosphorylation of the 95,000-dalton subunit of its own receptor
Science, January 8, 1982; 215(4529): 185 - 187.
[Abstract] [PDF]


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