Design of a selective insulin receptor tyrosine kinase inhibitor and its effect on glucose uptake and metabolism in intact cells

An inhibitor of the insulin receptor tyrosine kinase (IRTK), (hydroxy-2-naphthalenyl-methyl) phosphonic acid, was designed and synthesized and was shown to be an inhibitor of the biological effects of insulin in vitro. With a wheat germ purified human placental insulin receptor preparation, this com...

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Veröffentlicht in:	Biochemistry (Easton) 1989-06, Vol.28 (13), p.5694-5701
Hauptverfasser:	Saperstein, Richard, Vicario, Pasquale P, Strout, H. Vincent, Brady, Edward, Slater, Eve E, Greenlee, William J, Ondeyka, Debra L, Patchett, Arthur A, Hangauer, David G
Format:	Artikel
Sprache:	eng
Schlagworte:	550601 - Medicine- Unsealed Radionuclides in Diagnostics Adipose Tissue - metabolism ALDEHYDES Amino Acid Sequence AMINO ACIDS Analytical, structural and metabolic biochemistry ANIMAL CELLS ANIMALS BETA DECAY RADIOISOTOPES Biological and medical sciences Biological Transport, Active - drug effects BIOSYNTHESIS CARBOHYDRATES CARBON 14 COMPOUNDS CARBOXYLIC ACIDS Cell Line CHO CELLS CONNECTIVE TISSUE CELLS DAYS LIVING RADIOISOTOPES Deoxy Sugars - metabolism Deoxyglucose - metabolism Drug Design ELECTRON CAPTURE RADIOISOTOPES ENZYME ACTIVITY ENZYME INHIBITORS ENZYMES Enzymes and enzyme inhibitors FAT CELLS Female Fundamental and applied biological sciences. Psychology GLUCOSE HEXOSES HORMONES Humans HYDROXY ACIDS INSULIN Insulin - pharmacology INTERMEDIATE MASS NUCLEI IODINE 125 IODINE ISOTOPES ISOTOPE APPLICATIONS ISOTOPES Kinetics LABELLED COMPOUNDS Macromolecular Substances Male MAMMALS MAN MEMBRANE PROTEINS Molecular Sequence Data MONOSACCHARIDES Naphthalenes - chemical synthesis Naphthalenes - pharmacology NUCLEI ODD-EVEN NUCLEI ORGANIC ACIDS ORGANIC COMPOUNDS Organophosphonates Organophosphorus Compounds - chemical synthesis Organophosphorus Compounds - pharmacology PEPTIDE HORMONES PHOSPHORUS-GROUP TRANSFERASES Phosphorylation PHOSPHOTRANSFERASES placenta Placenta - metabolism Pregnancy PRIMATES Prodrugs - pharmacology protein kinase Protein-Tyrosine Kinases - antagonists & inhibitors PROTEINS Rabbits RADIOISOTOPES RADIOLOGY AND NUCLEAR MEDICINE RADIORECEPTOR ASSAY RATS Rats, Inbred Strains Receptor, Insulin - metabolism RECEPTORS RODENTS SACCHARIDES SOMATIC CELLS SYNTHESIS TRACER TECHNIQUES TRANSFERASES TYROSINE UPTAKE VERTEBRATES
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