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Endothelin-receptor interactions. Role of a putative sulfhydryl on the endothelin receptor.
Spinella, M J; Kottke, R; Magazine, H I; Healy, M S; Catena, J A; Wilken, P; Andersen, T T.
Afiliação
  • Spinella MJ; Department of Biochemistry and Molecular Biology, Albany Medical College, NY 12208.
FEBS Lett ; 328(1-2): 82-8, 1993 Aug 09.
Article em En | MEDLINE | ID: mdl-8344436
The mechanism of action of endothelin-receptor interactions was studied, using radioligand binding assays and SDS-PAGE, to investigate the possibility of disulfide interchange. Electrophoretic analysis suggested involvement of disulfide bond(s) in the receptor-ligand complex. Treatment of Et receptors with sulfhydryl-specific alkylating reagents (NEM or others) resulted in decreased ability to bind [125I]Et-1. [Dpr1-Asp15]Et-1, an antagonist homologous to Et but with an amide link replacing one of the disulfides, bound to Et receptors reversibly, but binding of Et-1 was less reversible. Preincubation of receptors with Et-1, but not with [Dpr1-Asp15]Et-1, protected receptors from alkylation with [14C]NEM. The data suggest that the Et receptor has a sulfhydryl group at or near the Et binding site. A model is proposed in which the role of the putative sulfhydryl group is discussed.
Assuntos
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Sulfidrila / Endotelinas / Receptores de Endotelina Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: FEBS Lett Ano de publicação: 1993 Tipo de documento: Article País de publicação: Reino Unido
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Sulfidrila / Endotelinas / Receptores de Endotelina Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: FEBS Lett Ano de publicação: 1993 Tipo de documento: Article País de publicação: Reino Unido