Microinjection of synthetic protein kinase inhibitor into single barnacle muscle fibers before and after cyclic AMP

1987 ◽  
Vol 43 (9) ◽  
pp. 1008-1009 ◽  
Author(s):  
E. E. Bittar ◽  
J. Nwoga
Keyword(s):  
Protein Kinase ◽  
Cyclic Amp ◽  
Kinase Inhibitor ◽  
Muscle Fibers ◽  
Protein Kinase Inhibitor ◽  
Barnacle Muscle ◽  
Synthetic Protein ◽  
Before And After ◽  
Barnacle Muscle Fibers

Effect of H-7, A Protein Kinase Inhibitor, on Cyclic AMP-Dependent Inhibition of Monoamine Transport in PC12 Cells

Pteridines ◽  
1995 ◽  
Vol 6 (3) ◽  
pp. 126-128
Author(s):  
Nobuo Nakanishi ◽  
Reiko Matsumoto ◽  
Kinji Kurihara ◽  
Takao Ueha ◽  
Hiroyuki Hasegawa
Keyword(s):  
Protein Kinase ◽  
Cyclic Amp ◽  
Pc12 Cells ◽  
Kinase Inhibitor ◽  
Protein Kinase Inhibitor ◽  
Monoamine Transport ◽  
Dependent Inhibition

scholarly journals Protein kinase activities in rat pancreatic islets of Langerhans

1979 ◽  
Vol 180 (1) ◽  
pp. 219-229 ◽  
Author(s):  
M C Sugden ◽  
S J Ashcroft ◽  
P H Sugden
Keyword(s):  
Protein Kinase ◽  
Cyclic Amp ◽  
Islets Of Langerhans ◽  
Kinase Inhibitor ◽  
Protein Kinase Inhibitor ◽  
Dependent Protein Kinase ◽  
Rat Islets ◽  
Dependent Protein ◽  
Rat Islets Of Langerhans ◽  
Independent Protein

1. Protein kinase activities in homogenates of rat islets of Langerhans were studied. 2. On incubation of homogenates with [gamma-32P]ATP, incorporation of 32P into protein occurred: this phosphorylation was neither increased by cyclic AMP nor decreased by the cyclic AMP-dependent protein kinase inhibitor described by Ashby & Walsh [(1972) J. Biol. Chem. 247, 6637–6642]. 3. On incubation of homogenates with [gamma-32P]ATP and histone as exogenous substrate for phosphorylation, incorporation of 32P into protein was stimulated by cyclic AMP (approx. 2.5-fold) and was inhibited by the cyclic AMP-dependent protein kinase inhibitor. In contrast, when casein was used as exogenous substrate, incorporation of 32P into protein was not stimulated by cyclic AMP, nor was it inhibited by the cyclic AMP-dependent protein kinase inhibitor. 4. DEAE-cellulose ion-exchange chromatography resolved four peaks of protein kinase activity. One species was the free catalytic subunit of cyclic AMP-dependent protein kinase, two species corresponded to ‘Type I’ and ‘Type II’ cyclic AMP-dependent protein kinase holoenzymes [see Corbin, Keely & Park (1975) J. Biol. Chem. 250, 218–225], and the fourth species was a cyclic AMP-independent protein kinase. 5. Determination of physical and kinetic properties of the protein kinases showed that the properties of the cyclic AMP-dependent activities were similar to those described in other tissues and were clearly distinct from those of the cyclic AMP-independent protein kinase. 6. The cyclic AMP-independent protein kinase had an s20.w of 5.2S, phosphorylated a serine residue(s) in casein and was not inhibited by the cyclic AMP-dependent protein kinase inhibitor. 7. These studies demonstrate the existence in rat islets of Langerhans of multiple forms of cyclic AMP-dependent protein kinase and also the presence of a cyclic AMP-independent protein kinase distinct from the free catalytic subunit of cyclic AMP-dependent protein kinase. The presence of the cyclic AMP-independent protein kinase may account for the observed characteristics of 32P incorporation into endogenous protein in homogenates of rat islets.

Structural origins of AGC protein kinase inhibitor selectivities: PKA as a drug discovery tool

2012 ◽  
Vol 393 (10) ◽  
pp. 1121-1129 ◽  
Author(s):  
Espen Åberg ◽  
Bjarte Lund ◽  
Alexander Pflug ◽  
Osman A.B.S.M. Gani ◽  
Ulli Rothweiler ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Protein Kinase ◽  
Cyclic Amp ◽  
Protein Kinases ◽  
Kinase Inhibitor ◽  
Protein Kinase Inhibitor ◽  
Constitutive Activity ◽  
Inhibitor Selectivity ◽  
Kinase A

Abstract The era of structure-based protein kinase inhibitor design began in the early 1990s with the determination of crystal structures of protein kinase A (PKA, or cyclic AMP-dependent kinase). Although many other protein kinases have since been extensively characterized, PKA remains a prototype for studies of protein kinase active conformations. It serves well as a model for the structural properties of AGC subfamily protein kinases, clarifying inhibitor selectivity profiles. Its reliable expression, constitutive activity, simple domain structure, and reproducible crystallizability have also made it a useful surrogate for the discovery of inhibitors of both established and emerging AGC kinase targets.

scholarly journals A protein kinase inhibitor in brown adipose tissue of developing rats

1974 ◽  
Vol 138 (2) ◽  
pp. 195-199 ◽  
Author(s):  
Josef P. Skala ◽  
George I. Drummond ◽  
Peter Hahn
Keyword(s):  
Adipose Tissue ◽  
Protein Kinase ◽  
Cyclic Amp ◽  
Brown Adipose Tissue ◽  
Inhibitory Activity ◽  
Kinase Inhibitor ◽  
Protein Kinase Inhibitor ◽  
Supernatant Fraction ◽  
Brown Adipose ◽  
Tissue Homogenates

A heat-stable protein was extracted from brown adipose tissue of infant rats that inhibited both purified bovine heart protein kinase and a crude preparation of protein kinase from brown fat. It did not act as an adenosine triphosphatase nor did it exert its effect by proteolytic action. Inhibition of protein kinase was affected in both the presence and the absence of cyclic AMP. Most of the inhibitory activity was present in the 100000g supernatant fraction of tissue homogenates. Inhibitory activity was highest perinatally and it declined 10 days after birth. It is suggested that the protein kinase inhibitor may play a role in regulating cyclic AMP actions.

Synthesis and biodistribution of [11C]H8, a cyclic AMP dependent protein kinase inhibitor

2001 ◽  
Vol 44 (S1) ◽  
pp. S368-S369
Author(s):  
K. Takahashi ◽  
S. Miura ◽  
M. Ibaraki ◽  
J. Hatazawa ◽  
K. Okane ◽  
...  
Keyword(s):  
Protein Kinase ◽  
Cyclic Amp ◽  
Kinase Inhibitor ◽  
Protein Kinase Inhibitor ◽  
Dependent Protein Kinase ◽  
Dependent Protein
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