Relation Results

Summary

Name KCNH2
Full Name Potassium voltage-gated channel subfamily H member 2
Synonyms Eag homolog, Ether-a-go-go-related gene potassium channel 1, ERG-1, Eag-related protein 1, Ether-a-go-go-related protein 1, H-ERG, hERG-1, hERG1, Voltage-gated potassium channel subunit Kv11.1 | ERG, ERG1, HERG
Primary ID Q12809
Links - -
Type protein
Relations 15
Inhibitors Terfenadine; cisapride; 3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthrenyl]-1-propanol
Function Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Me ...
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Type: Score: Layout: SPV 
0.3070.20.2850.80.80.2690.20.20.80.20.4PRKACAKCNH2PRKD1MINK1TerfenadinecisaprideNEDD4ITGB13-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthrenyl]-1-propanolPTPN6NEDD4L

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▶Modifications Tables

Relations
Regulator
Mechanism
target
score ℹ
+ PRKACAup-regulates img/direct-activation.png phosphorylation KCNH2 0.307
Identifier Residue Sequence Organism Cell Line
SIGNOR-70718 Ser1137 EGPTRRLsLPGQLGA Homo sapiens
pmid sentence
Deletion of protein kinase a phosphorylation sites in the herg potassium channel inhibits activation shift by protein kinase afour consensus pka phosphorylation sites (s283a, s890a, t895a, s1137a)
Identifier Residue Sequence Organism Cell Line
SIGNOR-70722 Ser283 CASVRRAsSADDIEA Homo sapiens
pmid sentence
Deletion of protein kinase a phosphorylation sites in the herg potassium channel inhibits activation shift by protein kinase afour consensus pka phosphorylation sites (s283a, s890a, t895a, s1137a)
Identifier Residue Sequence Organism Cell Line
SIGNOR-70726 Ser890 RQRKRKLsFRRRTDK Homo sapiens
pmid sentence
Deletion of protein kinase a phosphorylation sites in the herg potassium channel inhibits activation shift by protein kinase afour consensus pka phosphorylation sites (s283a, s890a, t895a, s1137a)
Identifier Residue Sequence Organism Cell Line
SIGNOR-70730 Thr895 KLSFRRRtDKDTEQP Homo sapiens
pmid sentence
Deletion of protein kinase a phosphorylation sites in the herg potassium channel inhibits activation shift by protein kinase afour consensus pka phosphorylation sites (s283a, s890a, t895a, s1137a)
Publications: 4 Organism: Homo Sapiens
+ PRKD1down-regulates activity img/direct_inhibition.png phosphorylation KCNH2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-277612 Ser284 ASVRRASsADDIEAM Homo sapiens HEK-293 Cell
pmid sentence
Based on LC-MS results from in vivo and HEK293 cell experiments we chose four KV11.1 mutant candidates for further functional analysis. Ablation of the putative PKD phosphorylation site in the mutant S284A increased the maximal current indicating S284 as a main PKD target in KV11.1.
Publications: 1 Organism: Homo Sapiens
+ MINK1up-regulates img/direct-activation.png binding KCNH2 0.285
Identifier Residue Sequence Organism Cell Line
SIGNOR-49869 Homo sapiens
pmid sentence
Herg, a human homologue of the ether-a-go-go gene of the fruitfly drosophila melanogaster, encodes aproteinthat produces the rapidly activating cardiac delayed rectifier (i[kr]). / our results show that mink physically associates with herg and that the interaction leads to increased ikr current density.
Publications: 1 Organism: Homo Sapiens
+ Terfenadinedown-regulates activity img/direct_inhibition.png chemical inhibition KCNH2 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-257826 in vitro
pmid sentence
 hERG activity was initially determined in a high throughput patch clamp screening assay (Ionworks)5 while a human H1 binding assay was used to determine H1 binding affinity.6 Selected results were confirmed in vitro using an IonWorks Quattro patch clamp assay and in vivo in the guinea pig.7, 8 Histamine H1activity was confirmed in vivo in the guinea pig.7
Identifier Residue Sequence Organism Cell Line
SIGNOR-258673 Homo sapiens HEK-293 Cell
pmid sentence
We have previously shown that terfenadine can inhibit both Kv1.5 and HERG with its effects on HERG being approximately 10‐fold more potent
Publications: 2 Organism: In Vitro, Homo Sapiens
+ cisapridedown-regulates activity img/direct_inhibition.png chemical inhibition KCNH2 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258672 Homo sapiens HEK-293 Cell
pmid sentence
A mechanism for the proarrhythmic effects of cisapride (Propulsid): high affinity blockade of the human cardiac potassium channel HERG. cisapride displays specific, high affinity block of the human cardiac K+ channel HERG. It is likely that this interaction underlies the proarrhythmic effects of the drug observed under certain clinical settings.
Publications: 1 Organism: Homo Sapiens
+ NEDD4down-regulates quantity by destabilization img/direct_inhibition.png ubiquitination KCNH2 0.269
Identifier Residue Sequence Organism Cell Line
SIGNOR-260998 Homo sapiens HEK-293T Cell
pmid sentence
We have previously shown that the E3 ubiquitin (Ub) ligase Nedd4-2 (neural precursor cell expressed developmentally down-regulated protein 4-2) targets the PY motif of hERG channels to initiate channel degradation. Although both immature and mature hERG channels contain the PY motif, Nedd4-2 selectively mediates the degradation of mature hERG channels.
Publications: 1 Organism: Homo Sapiens
+ KCNH2up-regulates activity img/direct-activation.png binding ITGB1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-277613 Homo sapiens
pmid sentence
One such mechanism is operant in colorectal cancer (CRC) cells. On integrin-dependent CRC cell adhesion, the Kv11.1/β1 integrin complex recruits the PI3K p85 subunit, which stimulates AKT phosphorylation and thus regulates autophagy
Publications: 1 Organism: Homo Sapiens
+ ITGB1up-regulates activity img/direct-activation.png binding KCNH2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-277614 Homo sapiens
pmid sentence
One such mechanism is operant in colorectal cancer (CRC) cells. On integrin-dependent CRC cell adhesion, the Kv11.1/β1 integrin complex recruits the PI3K p85 subunit, which stimulates AKT phosphorylation and thus regulates autophagy
Publications: 1 Organism: Homo Sapiens
+ 3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthrenyl]-1-propanoldown-regulates activity img/direct_inhibition.png chemical inhibition KCNH2 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-257816 in vitro
pmid sentence
4 inhibited cloned hERG potassium ion channel repolarization with an IC50 comparable to other antimalarial agents in this class (Table 6).
Publications: 1 Organism: In Vitro
+ PTPN6down-regulates img/direct_inhibition.png dephosphorylation KCNH2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-94007 Homo sapiens
pmid sentence
Our results show that erg-1 is a shp-1 substrate constituting the first report that an ion current is regulated by shp-1.
Publications: 1 Organism: Homo Sapiens
+ NEDD4Ldown-regulates quantity by destabilization img/direct_inhibition.png ubiquitination KCNH2 0.4
Identifier Residue Sequence Organism Cell Line
SIGNOR-278771 Homo sapiens
pmid sentence
As quantified in Fig. 5 B, only Nedd4-2 significantly increased the basal ubiquitylation of hERG1, while Nedd4-2-C801S and the other ubiquitin ligases had no effect.|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 channel at the plasma membrane through Nedd4-2 ubiquitylation of the channel, and 3) I hERG1 is strongly decreased by Nedd4-2 catalytic dependent activity.The hERG1 PY motif is a highly conserved sequence across animal species lines, highlighting its crucial role in the regulation of the hERG1 channel at the cell surface.
Publications: 1 Organism: Homo Sapiens
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