Analogs of MK-499 are differentially affected by a mutation in the S6 domain of the hERG K+ channel

Biochemical Pharmacology

Volumn 77, Issue 10, 2009, Pages 1602-1611

  Karczewski, Jerzy ^a   Wang, Jixin ^a   Kane, Stefanie A ^a   Kiss, Laszlo ^a   Koblan, Kenneth S ^a   Culberson, J Christopher ^a   Spencer, Robert H ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

hERG potassium channel; Ion channel pharmacology; MK 499; Molecular modeling; Site directed mutagenesis

Indexed keywords

1' (6 CYANO 1,2,3,4 TETRAHYDRO 2 NAPHTHYL) 3,4 DIHYDRO 6 METHANESULFONAMIDOSPIRO[2H 1 BENZOPYRAN 2,4' PIPERIDIN] 4 OL; AMINE; BENZOPYRAN DERIVATIVE; CISAPRIDE; HYDROXYL GROUP; KETONE; POTASSIUM CHANNEL HERG; S6 KINASE; TERFENADINE;

ANIMAL CELL; ARTICLE; ATOMIC ABSORPTION SPECTROMETRY; DRUG POTENCY; DRUG RECEPTOR BINDING; HEART ELECTROPHYSIOLOGY; HIGH THROUGHPUT SCREENING; HYDROGEN BOND; IC 50; MOLECULAR DOCKING; MOLECULAR MODEL; NONHUMAN; PATCH CLAMP; PHARMACOPHORE; PRIORITY JOURNAL; RECEPTOR AFFINITY; SITE DIRECTED MUTAGENESIS; STRUCTURAL HOMOLOGY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; VOLTAGE CLAMP;

ANIMALS; BENZOPYRANS; CELL CULTURE TECHNIQUES; CHLORIDES; CHO CELLS; CRICETINAE; CRICETULUS; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; ION CHANNEL GATING; LONG QT SYNDROME; MODELS, MOLECULAR; MUTATION; PATCH-CLAMP TECHNIQUES; PIPERIDINES; POTASSIUM CHANNEL BLOCKERS; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; RUBIDIUM; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSFECTION;

EID: 64049110808     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2009.02.011     Document Type: Article

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