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Site-directed mutagenesis of the rat beta1-adrenoceptor. Involvement of Tyr356 (7.43) in (+/-)cyanopindolol but not (+/-)[125Iodo]cyanopindolol binding

Rezmann-Vitti, Linda A ; Louis, Simon N S ; Nero, Tracy L ; Jackman, Graham P ; Machida, Curtis A ; Louis, William J

European journal of medicinal chemistry, 2004-07, Vol.39 (7), p.625 [Periódico revisado por pares]

France

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Título:
Site-directed mutagenesis of the rat beta1-adrenoceptor. Involvement of Tyr356 (7.43) in (+/-)cyanopindolol but not (+/-)[125Iodo]cyanopindolol binding
Autor: Rezmann-Vitti, Linda A ; Louis, Simon N S ; Nero, Tracy L ; Jackman, Graham P ; Machida, Curtis A ; Louis, William J
Assuntos: Adrenergic beta-Antagonists - chemistry ; Adrenergic beta-Antagonists - metabolism ; Adrenergic beta-Antagonists - pharmacology ; Animals ; Iodine Radioisotopes ; Models, Molecular ; Mutagenesis, Site-Directed ; Pindolol - analogs & derivatives ; Pindolol - chemistry ; Pindolol - metabolism ; Pindolol - pharmacology ; Protein Binding ; Protein Conformation ; Radioligand Assay ; Rats ; Receptors, Adrenergic, beta-1 - genetics ; Receptors, Adrenergic, beta-1 - metabolism ; Tyrosine - chemistry ; Tyrosine - genetics ; Tyrosine - metabolism
É parte de: European journal of medicinal chemistry, 2004-07, Vol.39 (7), p.625
Descrição: To determine the role played by Tyr(356 (7.43)) in the rat beta(1)-adrenoceptor in binding the antagonists (+/-)cyanopindolol (4-[3-(t-butylamino]-3-(2'-cyano-indoloxy)-2-propanolol) and its iodinated analogue (+/-)[(125)Iodo]cyanopindolol (1-(t-butylamino]-3-(2'-cyano-3'-iodo-indoloxy)-2-propanolol), Tyr(356 (7.43)) was mutated to either Phe or Ala and binding affinities determined for wild type and mutant rat beta(1)-adrenoceptors. Our results indicate that Tyr(356 (7.43)) is important for (+/-)cyanopindolol, but not (+/-)[(125)Iodo]cyanopindolol, binding and that (+/-)cyanopindolol adopts a "reverse" binding orientation whereas (+/-)[(125)Iodo]cyanopindolol cannot be accommodated in this binding mode. We define a "reverse" antagonist binding mode as one where the aryloxy moiety interacts with residues on transmembrane helices 1, 2, 3 and 7. The beta(1)-adrenoceptor site-directed mutagenesis results are the first to support a "reverse" antagonist binding orientation and the involvement of Tyr(356 (7.43)) in this binding mode.
Editor: France
Idioma: Inglês

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Site-directed mutagenesis of the rat beta1-adrenoceptor. Involvement of Tyr356 (7.43) in (+/-)cyanopindolol but not (+/-)[125Iodo]cyanopindolol binding

Rezmann-Vitti, Linda A ; Louis, Simon N S ; Nero, Tracy L ; Jackman, Graham P ; Machida, Curtis A ; Louis, William J

France

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