Development of Selective Covalent Janus Kinase 3 Inhibitors
نویسندگان
چکیده
منابع مشابه
Advances in the Inhibitors of Janus Kinase
In recent years, for the lesion site, studies at the molecular level of drugs targeting protein molecules has been a major research method for exploiting new, high-efficiency drugs with low toxicity [1]. Janus kinases (JAKs) are important signal transducers of many cytokines, growth factors and interferon. In recent years, it has been found in cancer cells and cells transfected with oncogenes t...
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The reports of a unique mutation in the Janus kinase-2 gene (JAK2) in polycythemia vera by several independent groups in 2005 quickly spurred the development of the Janus kinase inhibitors. In one of the great victories of translational research in recent times, the first smallmolecule Janus kinase inhibitor ruxolitinib entered a phase I trial in 2007. With the approval of ruxolitinib by the US...
متن کاملJAK 3 ( janus kinase 3 or just another kinase 3 )
JAK3 is expressed in 12 normal human tissues (bone marrow, spleen, thymus, brain, spinal cord, heart, skeletal muscle, liver, pancreas, prostate, kidney, and lung). JAK3S is more commonly seen in hematopoietic cells, whereas JAK3B and JAK3M are detected in cells of hematopoietic or epithelial origin. Localisation Intracellular, membrane-associated through association with interleukin (IL) recep...
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The human FGF receptors (FGFRs) play critical roles in various human cancers, and several FGFR inhibitors are currently under clinical investigation. Resistance usually results from selection for mutant kinases that are impervious to the action of the drug or from up-regulation of compensatory signaling pathways. Preclinical studies have demonstrated that resistance to FGFR inhibitors can be ac...
متن کاملFeatures of selective kinase inhibitors.
Small-molecule inhibitors of protein and lipid kinases have emerged as indispensable tools for studying signal transduction. Despite the widespread use of these reagents, there is little consensus about the biochemical criteria that define their potency and selectivity in cells. We discuss some of the features that determine the cellular activity of kinase inhibitors and propose a framework for...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2015
ISSN: 0022-2623,1520-4804
DOI: 10.1021/acs.jmedchem.5b00710