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Inhibitors of protein tyrosine kinases
Current Opinion in Biotechnology, 1995The description in the past year of several novel protein tyrosine kinase inhibitors, which exhibit dramatic improvements in potency and specificity over earlier agents, will be considered a major turning point in the field. These compounds appear to have the necessary pharmacological properties to finally allow clarification of whether suppression of ...
David W. Fry, Alexander James Bridges
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Paullones as Inhibitors of Protein Kinases
Current Topics in Medicinal Chemistry, 2011Paullones are a class of molecules structurally based on the 7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one parent scaffold. Many of these structures are inhibitors of certain protein kinases, namely cyclin-dependent kinases and glycogen synthase kinase-3. Being well referenced in the literature on the one hand and commercially available on the other
Conrad Kunick, Nadine Tolle
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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 ...
Stanley B. Kaye, Helen C. Swannie
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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 ...
Stanley B. Kaye, Helen C. Swannie
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An inhibitor protein of nuclear protein kinases
Nature, 1979THE 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.
Francoise Farron-Furstenthal+1 more
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Protein Kinase Inhibitors [PDF]
The article contains sections titled: 1. Introduction 2. Approved Kinase Inhibitors and Their Syntheses 3.
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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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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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Peptide Inhibitors Targeting Protein Kinases [PDF]
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.
Miriam Eisenstein, Hagit Eldar-Finkelman
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Therapeutic Protein Kinase Inhibitors
Cellular and Molecular Life Sciences, 2008Protein 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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6 Protein Tyrosine Kinase Inhibitors
1996Publisher Summary This chapter describes the classification and structure of protein tyrosine kinases (PTKs), their mode of action, their cellular targets, and the processes in which they are involved. A vast amount of research has been carried out to try to identify the role of PTKs in the general functioning and development of normal mammalian ...
Kevin R. H. Solomons+3 more
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Bacterial protein kinase inhibitors
Drug Development Research, 2010AbstractProtein kinases have become the second most important group of drug targets for the pharmaceutical industry next to G‐protein‐coupled receptors. Thus, over the past decade, a significant number of small molecules have been generated for protein kinase drug optimization programs. The vast majority of kinase inhibitors target the ATP binding site
Eeshwaraiah Begari, Michio Kurosu
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