Towards Selective Inhibitors of Janus Kinase 3: Identification of a Novel Structural Variation between Janus Kinases 2 and 3
نویسندگان
چکیده
منابع مشابه
JAK 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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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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Janus kinase 3 (Jak3) is a nonreceptor tyrosine kinase essential for signaling via cytokine receptors that comprise the common gamma-chain (gammac), i.e., the receptors for IL-2, IL-4, IL-7, IL-9, IL-15, and IL-21. Jak3 is preferentially expressed in hemopoietic cells and is up-regulated upon cell differentiation and activation. Despite the importance of Jak3 in lymphoid development and immune ...
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JAK2, a member of the Janus kinase (JAK) family of protein tyrosine kinases (PTKs), is an important intracellular mediator of cytokine signaling. Mutations of the JAK2 gene are associated with hematologic cancers, and aberrant JAK activity is also associated with a number of immune diseases, including rheumatoid arthritis. Accordingly, the development of JAK2-specific inhibitors has tremendous ...
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A novel homology model of the kinase domain of Janus kinase (JAK) 3 was used for the structure-based design of dimethoxyquinazoline compounds with potent and specific inhibitory activity against JAK3. The active site of JAK3 in this homology model measures roughly 8 A x 11 A x 20 A, with a volume of approximately 530 A3 available for inhibitor binding. Modeling studies indicated that 4-(phenyl)...
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ژورنال
عنوان ژورنال: Bulletin of the Korean Chemical Society
سال: 2012
ISSN: 0253-2964
DOI: 10.5012/bkcs.2012.33.12.4207