IndraLab

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Pyridine inhibits KCNH2. 7 / 7
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"In addition, pyridine-derived compound GSK-690 was reported to inhibit the human ether-a-go-go-related gene (hERG) cardiac ion channel, albeit with good anti-LSD1 potency in biochemical and cellular level41., 42.."
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"The major findings of this study are as follows : 1) hERG1 interacts via its PY motif with the ubiquitin ligase Nedd4-2, 2) this interaction promotes the down-regulation of the functional form of the [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Flow cytometry analysis provided further evidence showing that the PY peptide significantly prevented hERG channel proteins from degradation induced by overexpression of Nedd4-2."
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"Our synthetic PY peptide competitively inhibits the degradation of the Kv11.1 channel, which is over-activated because of higher expression of Nedd4-2 under pathological conditions."
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"We first tested if this synthetic PY peptide attenuated Nedd4-2-dependent degradation of the hERG channel in the HEK293 cell line with stable transfection of the hERG channel (hERG-HEK293)."
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"Our finding provided direct evidence that the synthetic PY peptide prevents hERG channel proteins from Nedd4-2-dependent degradation.Next, we tested the effect of in vivo administration of synthetic PY peptide on cardiac electrical remodeling in pCH guinea pigs."
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"We investigated whether a mutation in the PY motif of hERG1 could abolish the Nedd4-2 effect on I hERG1."
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