+ |
PRKACA | up-regulates
phosphorylation
|
KCNH2 |
0.308 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-70718 |
Ser1137 |
EGPTRRLsLPGQLGA |
Homo sapiens |
|
pmid |
sentence |
10488078 |
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 |
10488078 |
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 |
10488078 |
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 |
10488078 |
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 |
+ |
PRKD1 | down-regulates activity
phosphorylation
|
KCNH2 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-277612 |
Ser284 |
ASVRRASsADDIEAM |
Homo sapiens |
HEK-293 Cell |
pmid |
sentence |
29949809 |
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 |
+ |
KCNH2 | up-regulates activity
binding
|
ITGB1 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-277613 |
|
|
Homo sapiens |
|
pmid |
sentence |
35442831 |
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 |
+ |
ITGB1 | up-regulates activity
binding
|
KCNH2 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-277614 |
|
|
Homo sapiens |
|
pmid |
sentence |
35442831 |
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 |
+ |
Terfenadine | down-regulates activity
chemical inhibition
|
KCNH2 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258673 |
|
|
Homo sapiens |
HEK-293 Cell |
pmid |
sentence |
9395068 |
We have previously shown that terfenadine can inhibit both Kv1.5 and HERG with its effects on HERG being approximately 10‐fold more potent |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-257826 |
|
|
in vitro |
|
pmid |
sentence |
19660947 |
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 |
|
Publications: |
2 |
Organism: |
Homo Sapiens, In Vitro |
+ |
NEDD4L | down-regulates quantity by destabilization
ubiquitination
|
KCNH2 |
0.401 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-278771 |
|
|
Homo sapiens |
|
pmid |
sentence |
21463633 |
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 |
+ |
cisapride | down-regulates activity
chemical inhibition
|
KCNH2 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-258672 |
|
|
Homo sapiens |
HEK-293 Cell |
pmid |
sentence |
9395068 |
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 |
+ |
NEDD4 | down-regulates quantity by destabilization
ubiquitination
|
KCNH2 |
0.269 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-260998 |
|
|
Homo sapiens |
HEK-293T Cell |
pmid |
sentence |
26363003 |
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 |
+ |
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthrenyl]-1-propanol | down-regulates activity
chemical inhibition
|
KCNH2 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-257816 |
|
|
in vitro |
|
pmid |
sentence |
19222165 |
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 |
+ |
MINK1 | up-regulates
binding
|
KCNH2 |
0.286 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-49869 |
|
|
Homo sapiens |
|
pmid |
sentence |
9230439 |
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 |
+ |
PTPN6 | down-regulates
dephosphorylation
|
KCNH2 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-94007 |
|
|
Homo sapiens |
|
pmid |
sentence |
12361947 |
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 |