Progress toward JAK1-selective inhibitors
The discovery of the JAK-STAT pathway was a landmark in cell biology. The identification of these pathways has changed the landscape of treatment of rheumatoid arthritis and other autoimmune diseases. The two first (unselective) JAK inhibitors have recently been approved by the US FDA for the treatm...
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| Veröffentlicht in: | Future medicinal chemistry 2015-01, Vol.7 (2), p.203-235 |
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| container_title | Future medicinal chemistry |
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| creator | Menet, Christel J Mammoliti, Oscar López-Ramos, Miriam |
| description | The discovery of the JAK-STAT pathway was a landmark in cell biology. The identification of these pathways has changed the landscape of treatment of rheumatoid arthritis and other autoimmune diseases. The two first (unselective) JAK inhibitors have recently been approved by the US FDA for the treatment of myelofibrosis and rheumatoid arthritis and many other JAK inhibitors are currently in clinical development or at the discovery stage. Research groups have demonstrated the different roles of JAK member and the therapeutic potential of targeting them selectively. JAK1 plays a critical and potentially dominant role in the transduction of γc cytokine (γc = common γ chain) and in IL-6 signaling. In this review, we will discuss the state-of-the-art research that evokes JAK1 selective inhibition. |
| doi_str_mv | 10.4155/FMC.14.149 |
| format | Article |
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| source | MEDLINE; PubMed Central |
| subjects | Animals Humans Janus Kinase 1 - antagonists & inhibitors Janus Kinase 1 - metabolism Molecular Structure Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Structure-Activity Relationship |
| title | Progress toward JAK1-selective inhibitors |
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