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PMID: 4331561 Published · ppublish English Journal Article

Insulin receptors in the liver: specific binding of ( 125 I)insulin to the plasma membrane and its relation to insulin bioactivity.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 68 ·No. 8 ·1971-08-00 ·Pages 1833-7

Freychet P, Roth J, Neville DM

Abstract

With [(125)I]insulin at 7 x 10(-10) M, 25% of the radioactivity was bound to plasma membranes purified from rat liver. 20% of the [(125)I]insulin binding was inhibited by unlabeled insulin at 10(-9) M (6 ng/ml), equivalent to insulin concentrations in hepatic portal blood; inhibition of [(125)I]insulin binding was 80% at 10(-7) M and 90% at 10(-5) M. Eight insulins and derivatives with biological potencies that differed over a 100-fold range inhibited the binding of [(125)I]insulin to liver membranes in direct proportion to their ability to stimulate glucose oxidation in isolated fat cells. Inactive insulin chains, as well as glucagon, ACTH, and human growth harmone were without effect. The binding of [(125)I]insulin increased 55-fold as plasma membrane was purified from crude homogenate. Binding was time- and temperature-dependent, and addition of excess insulin produced rapid dissociation of [(125)I]insulin. This study demonstrates directly the binding of insulin to its biologically important receptors.

MeSH Terms
Adipose Tissue/cytology,metabolism Adrenocorticotropic Hormone/pharmacology Animals Binding Sites Cattle Cell Membrane/analysis,metabolism Fishes Glucagon/pharmacology Glucose/metabolism Growth Hormone/pharmacology Guinea Pigs Humans Insulin/analysis,metabolism,pharmacology Iodine Isotopes Liver/cytology,metabolism Proinsulin/pharmacology Proteins/isolation & purification Radioimmunoassay Rats Receptors, Drug/drug effects Swine Temperature Time Factors
Chemicals
Insulin Iodine Isotopes Proteins Receptors, Drug Adrenocorticotropic Hormone Growth Hormone Glucagon Proinsulin Glucose
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Freychet P
Roth J
Neville D M
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32 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
DOI
10.1073/pnas.68.8.1833
Published
1971-08-00
Pages
1833-7
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC389303
Subset
IM
External Links
PubMed source DOI: 10.1073/pnas.68.8.1833 PMC Full Text View journal details
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