IndraLab

Statements

KCNH2 binds RPS6. 7 / 7
| 7
sparser
"Another experimental mutagenesis study by Kamiya et al . have highlighted possible dofetilide interactions with hERG S6 residues G648, Y652, F656, and V659 as well as its pore helix residues T623, S624, and V625 ( xref ) in general agreement with our study."
38352360
sparser
"Thus, it seems reasonable to propose that lidocaine is also likely to interact with S6 aromatic residues of hERG and our docking data ( xref and S5) support such a conclusion."
24877995
sparser
"The direct block was mediated by drug binding to S6 domain of the hERG subunit, while trafficking deficiency was mediated by binding to a different site or a related protein. xref In this study, we used site-directed mutagenesis to test whether Y652A or F656V mutation alter the BBR sensitivity of hERG after long-term treatment."
26543354
sparser
"Altogether, these observations confirmed that the paradoxical activation effect initially observed when S4-S5 L (0) peptide was co-transfected with WT hERG channel was not due to an interaction of this peptide with the S6 T region of hERG."
28273916
sparser
"The drug-binding site is within the cavity formed by four S6 helices of the hERG tetramer ( Fig. 2 )."
22056716
sparser
"Interestingly, one d-sotalol (0) or l-sotalol(+) molecule was observed to bind deep into the hERG pore, just below the SF region and interact with the canonical drug binding F656 and Y652 hERG residues [ xref – xref ] in the pore lining S6 helices (drug molecule M2 in xref and xref ) for most of 8 μs long MD runs, while another drug molecule was observed to transiently bind below, interacting with F656 and/or Y652 from another domain as well as S660 and other residues at the bottom of S6 helices (M1 in xref and xref )."
34062207
sparser
"Interestingly, for l-sotalol(0) and d-sotalol(+) systems, we observed only transient binding of one or two drug molecules at the bottom of hERG channel pore interacting with S660 and other S6 helix residues there ( xref and xref and xref and xref ) Hence up to two sotalol molecules were able to bind to the hERG pore, in agreement with our electrophysiological data (as described below)."
34062207