About: Pharmacological inhibitors of JNK and ERK kinases SP600125 and U0126 are not appropriate tools for studies of drug metabolism because they activate aryl hydrocarbon receptor     Goto   Sponge   NotDistinct   Permalink

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  • Mitogen-activated protein kinases (MAPKs) are important regulators of aryl hydrocarbon receptor (AhR). An immense progress in MAPKs' biochemistry was attained with the discovery of their specific pharmacological inhibitors. Unfortunately, the inhibitors of JNK and ERK MAPKs, i.e. SP600125 and U0126, respectively, affect AhR-CYPIA signaling pathway because they are partial agonists of AhR and induce CYP1A genes. This implies that SP600125 and U0126 are inappropriate tools for studies of the role of MAPKs in AhR regulation. The results from studies using SP600125 or U 126, past or future, should be interpreted with prudence regarding their stimulatory effects on AhR-CYP1A pathway.
  • Mitogen-activated protein kinases (MAPKs) are important regulators of aryl hydrocarbon receptor (AhR). An immense progress in MAPKs' biochemistry was attained with the discovery of their specific pharmacological inhibitors. Unfortunately, the inhibitors of JNK and ERK MAPKs, i.e. SP600125 and U0126, respectively, affect AhR-CYPIA signaling pathway because they are partial agonists of AhR and induce CYP1A genes. This implies that SP600125 and U0126 are inappropriate tools for studies of the role of MAPKs in AhR regulation. The results from studies using SP600125 or U 126, past or future, should be interpreted with prudence regarding their stimulatory effects on AhR-CYP1A pathway. (en)
Title
  • Pharmacological inhibitors of JNK and ERK kinases SP600125 and U0126 are not appropriate tools for studies of drug metabolism because they activate aryl hydrocarbon receptor
  • Pharmacological inhibitors of JNK and ERK kinases SP600125 and U0126 are not appropriate tools for studies of drug metabolism because they activate aryl hydrocarbon receptor (en)
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  • Pharmacological inhibitors of JNK and ERK kinases SP600125 and U0126 are not appropriate tools for studies of drug metabolism because they activate aryl hydrocarbon receptor
  • Pharmacological inhibitors of JNK and ERK kinases SP600125 and U0126 are not appropriate tools for studies of drug metabolism because they activate aryl hydrocarbon receptor (en)
skos:notation
  • RIV/61989592:15310/08:00005339!RIV10-MSM-15310___
http://linked.open...avai/riv/aktivita
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  • P(GA303/07/0128), Z(MSM6198959216)
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  • 2
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  • 386456
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  • RIV/61989592:15310/08:00005339
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  • Aryl hydrocarbon receptor; MAPK; JNK; ERK; SP600125; U0126 (en)
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  • SK - Slovenská republika
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  • [0D6F2F2BBE91]
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  • General Physiology and Biophysics
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  • 27
http://linked.open...iv/tvurceVysledku
  • Dvořák, Zdeněk
  • Bachleda, Petr
http://linked.open...n/vavai/riv/zamer
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  • 0231-5882
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  • 15310
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