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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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Emerging protein kinase inhibitors for non-small cell lung cancer

Expert Opinion on Emerging Drugs, 2013
Introduction: In the current paradigm of precision medicine in non-small cell lung cancer (NSCLC), the therapeutic strategy is determined by the molecular characteristics.
Stephen V. Liu   +4 more
semanticscholar   +1 more source

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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Peptide Inhibitors Targeting Protein Kinases [PDF]

open access: possibleCurrent 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.
Miriam Eisenstein, Hagit Eldar-Finkelman
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6 Protein Tyrosine Kinase Inhibitors

1996
Publisher 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, 2010
AbstractProtein 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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Chemical Inhibitors of Protein Kinases

Chemical Reviews, 2001
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
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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.
Friedrich Marks   +6 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.
Halyna E. Wysowskyj   +2 more
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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 ...
Patrick J. Carroll   +2 more
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