Yihong Zhang

TL;DR: Ivabradine prolongs ventricular repolarization and alters electrical restitution properties at concentrations relevant to the upper therapeutic range, and may have important implications both clinically and for future bradycardic drug design.

TL;DR: It is concluded that flecainide accesses the hERG channel from the cell interior on channel gating, binding low in the inner cavity, with the S6 F656 residue acting as a principal binding determinant.

TL;DR: Docking simulations indicated that the larger size of ranolazine gives it potential for a greater range of interactions with hERG pore side chains compared to lidocaine, in particular enabling interaction of its two aromatic groups with side chains of both Y652 and F656.

TL;DR: An update of recent research is described that addresses the nature of the particular gated state of hERG captured in the new structure, and the insight afforded by the structure into the molecular basis for high affinity drug block of h ERG, the binding ofhERG activators and the Molecular basis of hERG's peculiar gating properties are addressed.

TL;DR: HERG channel inhibition by a minimally structured high-affinity hERG inhibitor, Cavalli-2, composed of three phenyl groups linked by polymethylene spacers around a central amino group, chosen to probe the spatial arrangement of side chain groups in the high-Affinity drug-binding site of the hERG pore is characterized.