scholarly journals Role of protein kinases in stimulation of human polymorphonuclear leukocyte oxidative metabolism by various agonists. Differential effects of a novel protein kinase inhibitor.

1986 ◽  
Vol 77 (1) ◽  
pp. 61-65 ◽  
Author(s):  
C Gerard ◽  
L C McPhail ◽  
A Marfat ◽  
N P Stimler-Gerard ◽  
D A Bass ◽  
...  
Keyword(s):  
Protein Kinase ◽  
Protein Kinases ◽  
Oxidative Metabolism ◽  
Polymorphonuclear Leukocyte ◽  
Kinase Inhibitor ◽  
Protein Kinase Inhibitor ◽  
Human Polymorphonuclear Leukocyte ◽  
Novel Protein ◽  
Stimulation Of

Role of protein kinase C in T-cell antigen receptor regulation of p21ras: evidence that two p21ras regulatory pathways coexist in T cells

1992 ◽  
Vol 12 (7) ◽  
pp. 3305-3312
Author(s):  
M Izquierdo ◽  
J Downward ◽  
J D Graves ◽  
D A Cantrell
Keyword(s):  
T Cells ◽  
Protein Kinase C ◽  
Protein Kinase ◽  
Kinase Inhibitor ◽  
Antigen Receptor ◽  
Permeabilized Cell ◽  
Regulatory Pathways ◽  
Kinase C ◽  
Stimulation Of

T-lymphocyte activation via the antigen receptor complex (TCR) results in accumulation of p21ras in the active GTP-bound state. Stimulation of protein kinase C (PKC) can also activate p21ras, and it has been proposed that the TCR effect on p21ras occurs as a consequence of TCR regulation of PKC. To test the role of PKC in TCR regulation of p21ras, a permeabilized cell system was used to examine TCR regulation of p21ras under conditions in which TCR activation of PKC was blocked, first by using a PKC pseudosubstrate peptide inhibitor and second by using ionic conditions that prevent phosphatidyl inositol hydrolysis and hence diacylglycerol production and PKC stimulation. The data show that TCR-induced p21ras activation is not mediated exclusively by PKC. Thus, in the absence of PKC stimulation, the TCR was still able to induce accumulation of p21ras-GTP complexes, and this stimulation correlated with an inactivation of p21ras GTPase-activating proteins. The protein tyrosine kinase inhibitor herbimycin could prevent the non-PKC-mediated, TCR-induced stimulation of p21ras. These data indicate that two mechanisms for p21ras regulation coexist in T cells: one PKC mediated and one not. The TCR can apparently couple to p21ras via a non-PKC-controlled route that may involve tyrosine kinases.

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 novel protein kinase inhibitor IMB-YH-8 with anti-tuberculosis activity

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Jian Xu ◽  
Ju-xian Wang ◽  
Jin-ming Zhou ◽  
Chang-liang Xu ◽  
Bin Huang ◽  
...  
Keyword(s):  
Protein Kinase ◽  
Kinase Inhibitor ◽  
Protein Kinase Inhibitor ◽  
Tuberculosis Activity ◽  
Novel Protein
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