IndraLab

Statements

Tofacitinib inhibits TYK2. 16 / 33
16 1 | 16
reach
"Tofacitinib inhibits JAK1 and JAK2 to a greater degree than was initially thought and also inhibits Tyk2 marginally.139, 140, 141, 142, 143, 144Tofacitinib is the most potent (inhibitory potency of 1 nM) and selective JAK3 inhibitor developed to date."
| PMC
reach
"Tofacitinib inhibits JAK1, JAK2, JAK3 and to a lesser extent TYK2."
32561292
reach
"Tofacitinib blocks the JAK-1 and JAK-3, and, at high concentrations, tyrosine kinase 2 (TYK2) and JAK-2 pathways as well."
31205486
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"Tofacitinib potently inhibits JAK1, JAK2, and JAK3 and, to a lesser extent, TYK2 in biochemical assay (IC50 = 3.2, 4.1, 1.6, and 34 nM respectively)."
32326669
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"Reports have shown that upadacitinib and tofacitinib significantly inhibit JAK1/TYK2 in IFNα/pSTAT5 compared to filgotinib ."
40352699
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"Tofacitinib inhibits JAK1/JAK3 and, to a lesser extent, JAK2/TYK2."
38576610
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"Tofacitinib inhibits the activity of Janus kinases JAK1 and JAK3 and, to a lesser degree, JAK2 and TYK2."
30237624
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"Tofacitinib preferentially blocks JAK1/3 and, to some degree, JAK2 and TYK2 [6]."
36534552
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"Deucravacitinib was approximately 56- to 120-fold more potent than tofacitinib, upadacitinib, and baricitinib at inhibiting TYK2-dependent IL-12–induced IFN-γ production in human whole blood."
34471993
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"Thus, tofacitinib that inhibits JAK1, JAK2, JAK3 and, to a lesser extent, TYK2 is used in the clinic for treating RA patients in many countries."
28456914
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"Finally, we found that TYK2/JAK2-dependent IL-12-STAT4 signaling in human PBMC-derived T-blasts was inhibited by both BMS-986165 and tofacitinib, but not VVD-118313 (Fig. 4e)."
36097295
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"With an EC50 of 5 nM, tofacitinib inhibits JAK3 and TYK2, reducing inflammatory cytokines associated with RA such as IL-2, IL-4, IL-6, and IL-7."
35444538
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"Notably, as demonstrated in the current analysis, lack of inhibition of TYK2 by tofacitinib, upadacitinib, and baricitinib at therapeutic concentrations suggests that the above adverse effects associated with these JAK 1/2/3 inhibitors are unlikely to be related to TYK2 inhibition.The results from the current analyses confirm that deucravacitinib is a highly selective TYK2 inhibitor with minimal or no activity against JAK 1/2/3 at clinically relevant doses and concentrations."
34471993
reach
"Initially thought as a JAK3 specific inhibitor, tofacitinib also suppresses JAK1, JAK2, and TYK2 in vitro, although with lesser affinity and with functional selectivity for JAK1 and JAK3 in cellular assays [59,60]."
27177233
reach
"Tofacitinib inhibits JAK1/2/3 and, to a lesser extent, TYK2 (Hodge et al., 2016)."
38426013
reach
"Tofacitinib has been shown to inhibit the activity of JAK1, JAK2, and JAK3, and to a lesser extent tyrosine-protein 2 kinases (TyK2)."
| PMC