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Article: Reports outline pharmacology study findings from J. Karczewski and colleagues.
- Article from:
- Biotech Week
- Article date:
- July 1, 2009
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According to a study from the United States, "Drug-induced long QT syndrome has been principally ascribed to block of the cardiac hERG K+ channel. Methanesulfonanilides, such as MK-499, E-4031 and dofetilide, are potent hERG antagonists that likely bind along the S6 helix within the inner vestibule of the pore."
"To further investigate these interactions, we broadly explored the structure-activity relationships of closely related analogs of MK-499 using a high-throughput ion flux assay, and evaluated in greater detail using patch-clamp electrophysiology. We observed that substitutions at the 4-position on the benzopyran ring significantly affected the potency of ...