IndraLab

Statements

reach
"The kinase inhibitor Tofacitinib (Tofa), a small molecule that preferentially blocks JAK1 activity, was administered in a clinically relevant regimen to mimic the human exposure, at doses that largely block phospho-Stat1 activation by IFN, alone or prior to a 2-hr parenteral IFN challenge."
26824662
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"Tofacitinib (TOFA), which inhibits JAK1 and JAK3, upadacitinib (UPA) and filgotinib (FIL) which inhibit JAK1 and to a lesser extent other JAK molecules."
39974590
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"TOFA is a selective inhibitor of JAK1 and JAK3, and its inhibitory effect on JAK2 and tyrosine kinase (TYK) 2 is limited.6 BARI is a selective inhibitor of JAK1 and JAK2 and exhibits a moderate inhibitory activity against TYK2, while its inhibitory activity against JAK3 is limited.7 Randomised controlled trials have shown that TOFA and BARI monotherapies are effective in patients with RA who are methotrexate (MTX) naïve8 9 or have MTX-inadequate response (IR),10 11 tumour necrosis factor inhibitor-IR12 13 and bDMARDs-IR."
33827788
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"To evaluate the influence of the active principles on the phase identity, TOFA (a hydrophilic inhibitor of the JAK1 and 3) and TAC (a hydrophobic immunosuppressive drug) loaded-mesophases were independently prepared and analysed with SAXS."
37311749
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"TOFA preferentially inhibits JAK1 and JAK3 [13], with consequent inhibition of the activity of several pro-inflammatory cytokines that are produced by CD4+ T cells and synovial fibroblasts, including IL-6, and it has been shown to be effective in several models of experimental arthritis [14,15]."
37629770
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"Tofa has also been shown to suppress the activities of all JAKs, particularly JAK1 and JAK3 in mammalian inflammatory bowel disease (19,20)."
34504562
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"These include tofacitinib (TOFA), which mainly inhibits JAK1 and JAK2 and to a lesser extent JAK2; baricitinib (BARI), which primarily inhibits JAK 1 and JAK2; and upadacitinib (UPA) and filgotinib (FILGO), both selective for JAK1 [6]."
38999494
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"TOFA preferentially inhibits JAK1 and JAK3 [ xref ], with consequent inhibition of the activity of several pro-inflammatory cytokines that are produced by CD4+ T cells and synovial fibroblasts, including IL-6, and it has been shown to be effective in several models of experimental arthritis [ xref , xref ]."
37629770
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"Next, we discovered that pretreatment with T-96 inhibited the phosphorylation of JAK2 in IFN-γ treated keratinocytes at 15 min by flow cytometry (Fig.  xref F and Additional file xref : Fig. S5C) and western blot (Additional file xref : Fig. S5D), and Tofa inhibited both JAK1 and JAK2 (Additional file xref : Fig. S5C-F)."
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"TOFA inhibits JAK1, JAK3, and to a lesser extent JAK2, and BARI inhibits JAK1 and JAK2, thereby blocking the proinflammatory cytokine expression at sites of inflammation. xref "
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