Physicochemical Features of the hERG Channel Drug Binding Site

Blockade of hERG K+ channels in the heart is an unintentional side effect of many drugs and can induce cardiac arrhythmia and sudden death. It has become common practice in the past few years to screen compounds for hERG channel activity early during the drug discovery process. Understanding the mol...

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Veröffentlicht in:	The Journal of biological chemistry 2004-03, Vol.279 (11), p.10120-10127
Hauptverfasser:	Fernandez, David, Ghanta, Azad, Kauffman, Gregory W., Sanguinetti, Michael C.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Motifs Amino Acid Sequence Animals Benzopyrans - pharmacology Binding Sites Biophysical Phenomena Biophysics Cation Transport Proteins - chemistry Cation Transport Proteins - genetics Cation Transport Proteins - metabolism Cisapride - pharmacology Ether-A-Go-Go Potassium Channels Histamine H1 Antagonists - pharmacology Inhibitory Concentration 50 Kinetics Models, Molecular Molecular Sequence Data Mutation Oocytes - metabolism Phenylalanine - chemistry Piperidines - pharmacology Point Mutation Potassium Channels - chemistry Potassium Channels - genetics Potassium Channels - metabolism Potassium Channels, Voltage-Gated Protein Binding Protein Structure, Tertiary RNA, Complementary - metabolism Sequence Homology, Amino Acid Serotonin Receptor Agonists - pharmacology Temperature Terfenadine - chemistry Terfenadine - pharmacology Tyrosine - chemistry Xenopus
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