scholarly journals In vitro and in vivo activation of the insulin receptor kinase in control and denervated skeletal muscle.

1986 ◽  
Vol 261 (19) ◽  
pp. 8985-8993
Author(s):  
C F Burant ◽  
M K Treutelaar ◽  
M G Buse
Keyword(s):  
Skeletal Muscle ◽  
Insulin Receptor ◽  
Receptor Kinase ◽  
Insulin Receptor Kinase

Delayed onset of insulin activation of the insulin receptor kinase in vivo in human skeletal muscle

Diabetes ◽  
1994 ◽  
Vol 43 (1) ◽  
pp. 118-126 ◽  
Author(s):  
G. R. Freidenberg ◽  
S. Suter ◽  
R. R. Henry ◽  
J. Nolan ◽  
D. Reichart ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Insulin Receptor ◽  
Human Skeletal Muscle ◽  
Receptor Kinase ◽  
Delayed Onset ◽  
Insulin Receptor Kinase

In vivo insulin mimetic effects of pV compounds: role for tissue targeting in determining potency

1995 ◽  
Vol 268 (1) ◽  
pp. E60-E66 ◽  
Author(s):  
A. P. Bevan ◽  
J. W. Burgess ◽  
J. F. Yale ◽  
P. G. Drake ◽  
D. Lachance ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Insulin Receptor ◽  
Glycogen Synthesis ◽  
Insulin Receptors ◽  
Receptor Kinase ◽  
Rat Diaphragm ◽  
Insulin Mimetic ◽  
Integrated Response ◽  
Insulin Receptor Kinase

Peroxovanadium (pV) compounds activate the insulin receptor kinase in hepatocytes and inhibit the dephosphorylation of insulin receptors in hepatic endosomes with highly correlated potencies (Posner, B. I., R. Faure, J. W. Burgess, A. P. Bevan, D. Lachance, G. Zhang-Sun, J. B. Ng, D. A. Hall, B. S. Lum, and A. Shaver J. Biol. Chem. 269: 4596–4604, 1994). After intravenous administration, K2[VO(O2)2(picolinato)].2H2O [bpV(pic)], VO(O2) (picolinato) (H2O)2 [mpV(pic)], K[VO(O2)2(picolinato)].3H2O [bpV(phen)], and K[VO(O2)2(4,7-dimethyl-1,10-phenanthroline)].1/2H2O [bpV(Me2phen)] produced 50% of their maximal hypoglycemic effect at doses of 0.04, 0.04, 0.32, and 0.65 mumol/100 g body wt, respectively. In contrast, their potencies as inhibitors of dephosphorylation were bpV(pic) = bpV(phen) > mpV(pic) = bpV(Me2phen). bpV(pic) stimulated [14C]glucose incorporation into rat diaphragm glycogen in vivo, and its effect was dose dependent, synergistic with insulin, and evident in other skeletal muscles. In contrast, bpV(phen) displayed no effect on glycogen synthesis in skeletal muscle. mpV(pic) stimulated and bpV(Me2phen) had no effect on glycogen synthesis in the diaphragm. bpV(pic) augmented rat diaphragm insulin receptor kinase 2.2-fold with a time-integrated response 70% that of insulin. In contrast, the effect of bpV(phen) was delayed and much reduced. Thus, the in vivo potencies of pV compounds reflect differing capacities to act on skeletal muscle. The ancillary ligand within the pV complex may target one tissue in preference to another.

Tissue Specific Differences in the Insulin Receptor Kinase Activated in Vitro and in Vivo*

Endocrinology ◽  
1988 ◽  
Vol 122 (2) ◽  
pp. 427-437 ◽  
Author(s):  
CHARLES F. BURANT ◽  
MARY K. TREUTELAAR ◽  
MARIA G. BUSE
Keyword(s):  
Insulin Receptor ◽  
Receptor Kinase ◽  
Tissue Specific ◽  
Insulin Receptor Kinase

Delayed Onset of Insulin Activation of the Insulin Receptor Kinase In Vivo in Human Skeletal Muscle

Diabetes ◽  
1994 ◽  
Vol 43 (1) ◽  
pp. 118-126 ◽  
Author(s):  
G. R. Freidenberg ◽  
S. Suter ◽  
R. R. Henry ◽  
J. Nolan ◽  
D. Reichart ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Insulin Receptor ◽  
Human Skeletal Muscle ◽  
Receptor Kinase ◽  
Delayed Onset ◽  
Insulin Receptor Kinase

scholarly journals Internalization and Activation of the Rat Liver Insulin Receptor Kinase in vivo

1989 ◽  
Vol 264 (22) ◽  
pp. 12931-12940 ◽  
Author(s):  
M N Khan ◽  
G Baquiran ◽  
C Brule ◽  
J Burgess ◽  
B Foster ◽  
...  
Keyword(s):  
Insulin Receptor ◽  
Rat Liver ◽  
Receptor Kinase ◽  
Insulin Receptor Kinase

Impaired insulin action but normal insulin receptor activity in diabetic rat liver: effect of vanadate

1990 ◽  
Vol 258 (3) ◽  
pp. E459-E467 ◽  
Author(s):  
O. Blondel ◽  
J. Simon ◽  
B. Chevalier ◽  
B. Portha
Keyword(s):  
Insulin Receptor ◽  
Insulin Action ◽  
Diabetic Rats ◽  
Receptor Kinase ◽  
Peripheral Tissues ◽  
Impaired Insulin ◽  
Insulin Dependent ◽  
Insulin Receptor Kinase ◽  
Impaired Insulin Action

In vivo insulin resistance is a characteristic of the liver and peripheral tissues in 10-wk-old female rats with non-insulin-dependent diabetes induced by streptozotocin given on day 5 after birth. Oral administration of vanadate (0.2 mg/ml) for 20 days in the diabetic rats lowered their plasma glucose levels to normal values without affecting their basal plasma insulin levels. In the basal state as well as after submaximal or maximal hyperinsulinemia (euglycemic clamp studies), peripheral glucose utilization and hepatic glucose production in vivo were normalized in the diabetic rats after the vanadate treatment. In wheat germ agglutinin purified receptors, 125I-labeled porcine insulin binding, basal and insulin-stimulated insulin receptor kinase activities for both the autophosphorylation of the beta-subunit and the phosphorylation of the artificial substrate poly (Glu-Tyr) 4:1, were found identical in diabetic and control rats, treated or not with vanadate. Liver phosphoenolpyruvate carboxykinase activity was significantly enhanced in untreated diabetic rats (P less than 0.01) as compared with control rats and returned to normal values after the 20-day vanadate treatment. Thus, in that model of non-insulin-dependent diabetes, 1) oral vanadate exerts a corrective insulin-like effect on impaired insulin action both at the level of liver and peripheral tissues, 2) impaired insulin action with no alteration of the insulin receptor tyrosine kinase is observed in the liver of untreated rats, and 3) corrective effect of vanadate on liver glucose metabolism is probably distal to the insulin receptor kinase activity.

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