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Protein kinase C inhibitors

Current Oncology Reports, 2002
Protein kinase C (PKC) is a family of serine-threonine protein kinases that are involved in signal transduction pathways that regulate growth factor response, proliferation, and apoptosis. Its central role in these processes, which are closely involved in tumor initiation, progression, and response to antitumor agents, makes it an attractive ...
Helen C, Swannie, Stanley B, Kaye
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Therapeutic Protein Kinase Inhibitors

Cellular and Molecular Life Sciences, 2008
Protein kinase inhibitors represent an important and still emerging class of targeted therapeutic agents. Drug discovery and development strategies have explored numerous approaches to target the inhibition of protein kinase signaling. This review will highlight some of the strategies that have led to the successful clinical development of therapeutic ...
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JAK Protein Kinase Inhibitors

Drug News & Perspectives, 2005
In humans, the Janus protein tyrosine kinase family (JAKs) contains four members: JAK1, JAK2, JAK3 and TYK2. JAKs phosphorylate signal transducers and activators of transcription (STATs) simultaneously with other phosphorylations required for activation, and there are several cellular mechanisms in place to inhibit JAK/STAT signaling. That one might be
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An inhibitor protein of nuclear protein kinases

Nature, 1979
THE cyclical phosphorylation and dephosphorylation of proteins, catalysed by protein kinases and phosphoprotein phosphatases, respectively, are important ways in which cells regulate many of their metabolic activities. Cells seem to have at least two distinct phosphorylation systems, one in the cytoplasm, the other in the nucleus.
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Peptide Inhibitors Targeting Protein Kinases

Current Pharmaceutical Design, 2009
Phosphorylation by protein kinases is a central theme in biological systems. Aberrant protein kinase activity has been implicated in a variety of human diseases, therefore, modulation of kinase activity represents an attractive therapeutic approach for the treatment of human illnesses.
Hagit, Eldar-Finkelman   +1 more
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Profiling of inhibitors of protein kinase C

Advances in Enzyme Regulation, 1988
A rapid screen assay for protein kinase C was described which allowed the detection of inhibitors and activators of the enzyme at different states of activation. Upon secondary evaluation of the active inhibitors, three classes of compounds were identified.
L P, Wennogle, H E, Wysowskyj, A Y, Jeng
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Ruthenium Complexes as Protein Kinase Inhibitors

Organic Letters, 2004
[reaction: see text] Replacing complex natural products with simple metal complexes could lead to a new class of metallopharmaceuticals in which the metal center plays mainly a structural role. A strategy is introduced for the creation of ruthenium complex-based protein kinase inhibitors 1 (X = CO or CH(2)), morphed out of the class of indolocarbazole ...
Lilu, Zhang   +2 more
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Rottlerin, a Novel Protein Kinase Inhibitor

Biochemical and Biophysical Research Communications, 1994
Rottlerin, a compound from Mallotus philippinensis, is shown to inhibit protein kinases with some specificity for PKC. To some extent, the novel inhibitor is able to differentiate between PKC isoenzymes, with IC50 values for PKC delta of 3-6 microM, PKC alpha,beta,gamma of 30-42 microM and PKC epsilon,eta,zeta of 80-100 microM.
M, Gschwendt   +6 more
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The Protein Kinase C Inhibitor: Ruboxistaurin

2015
The isozyme protein kinase C (PKC) β is involved in several processes that are deregulated in different retinal cell types by hyperglycemia. This family of serine/threonine-specific protein kinases comprises several different members, which differ in their structure, cofactor requirement and substrate specificity.
Heidrun L, Deissler, Gabriele E, Lang
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Protein kinase inhibitors and antibiotic resistance

Pharmacology & Therapeutics, 2002
While antibiotics revolutionized the treatment of infectious disease in the 20th century, bacterial resistance now threatens to render many of them ineffective. Aminoglycosides are a class of clinically important antibiotics used in the treatment of infections caused by Gram-positive and -negative organisms.
David L, Burk, Albert M, Berghuis
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