Identification of a New Class of Inhibitors of the Voltage-Gated Potassium Channel, Kv1.3, with Immunosuppressant Properties

The voltage-gated potassium channel, Kv1.3, is a novel target for development of immunosuppressants. Using a functional 86Rb+ efflux assay, a new class of high-affinity Kv1.3 inhibitors has been identified. The initial active in this series, 4-phenyl-4-[3-(2-methoxyphenyl)-3-oxo-2-azaprop-1-yl]cyclo...

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Veröffentlicht in:	Biochemistry (Easton) 2002-06, Vol.41 (24), p.7781-7794
Hauptverfasser:	Schmalhofer, William A, Bao, Jianming, McManus, Owen B, Green, Brian, Matyskiela, Mary, Wunderler, Denise, Bugianesi, Randal M, Felix, John P, Hanner, Markus, Linde-Arias, Ana-Rosa, Ponte, Cristiano G, Velasco, Lucia, Koo, Gloria, Staruch, Mary Jo, Miao, Shouwu, Parsons, William H, Rupprecht, Kathleen, Slaughter, Robert S, Kaczorowski, Gregory J, Garcia, Maria L
Format:	Artikel
Sprache:	eng
Schlagworte:	Alanine - genetics Animals Binding Sites Cell Line CHO Cells Cricetinae Cyclohexanones - chemical synthesis Cyclohexanones - metabolism Cyclohexanones - pharmacology Guinea Pigs Humans Immunosuppressive Agents - chemical synthesis Immunosuppressive Agents - metabolism Immunosuppressive Agents - pharmacology Intracellular Fluid - metabolism Kv1.3 Potassium Channel Lymphocyte Activation - drug effects Monoiodotyrosine - metabolism Patch-Clamp Techniques Phenylalanine - genetics Potassium Channel Blockers Potassium Channels - genetics Potassium Channels - metabolism Potassium Channels, Voltage-Gated - antagonists & inhibitors Potassium Channels, Voltage-Gated - metabolism Rats Scorpion Venoms - metabolism T-Lymphocytes - drug effects T-Lymphocytes - immunology T-Lymphocytes - metabolism Transfection Triterpenes - metabolism Tyrosine - genetics
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