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Effects of the M1 agonist xanomeline on processing of human beta-amyloid precursor protein (FAD, Swedish mutant) transfected into Chinese hamster ovary-m1 cells.
DeLapp, N; Wu, S; Belagaje, R; Johnstone, E; Little, S; Shannon, H; Bymaster, F; Calligaro, D; Mitch, C; Whitesitt, C; Ward, J; Sheardown, M; Fink-Jensen, A; Jeppesen, L; Thomsen, C; Sauerberg, P.
Afiliación
  • DeLapp N; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA. nwd@lilly.com
Biochem Biophys Res Commun ; 244(1): 156-60, 1998 Mar 06.
Article en En | MEDLINE | ID: mdl-9514902
Complementary DNA (cDNA) encoding human beta-amyloid precursor protein familial Alzheimer's disease (FAD) Swedish mutant (beta APPSM) form was cloned into a mammalian expression vector (PK255) containing the CMV promoter. The vector was transfected into Chinese hamster ovary cells containing human muscarinic m1 receptors (CHO-m1), and clonal cells stably expressing beta APPSM were isolated. The effects of m1-receptor activation by the selective m1 agonist xanomeline and the non-selective muscarinic agonist carbachol on processing of beta APPSM to release soluble APP (APPs) and beta-amyloid peptide (A beta) were compared. Xanomeline stimulated APP release with a potency 1000-fold greater than that observed for carbachol. Concentrations of carbachol and xanomeline producing maximal effects on APPs release reduced the secretion of A beta by 28 and 46%, respectively. These results extend previous studies with xanomeline and suggest that cholinergic replacement therapy for Alzheimer's disease may reduce amyloid deposition.
Asunto(s)
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Tiadiazoles / Transfección / Procesamiento Proteico-Postraduccional / Receptores Muscarínicos / Precursor de Proteína beta-Amiloide / Agonistas Muscarínicos / Mutación Límite: Animals / Humans País/Región como asunto: Europa Idioma: En Revista: Biochem Biophys Res Commun Año: 1998 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Tiadiazoles / Transfección / Procesamiento Proteico-Postraduccional / Receptores Muscarínicos / Precursor de Proteína beta-Amiloide / Agonistas Muscarínicos / Mutación Límite: Animals / Humans País/Región como asunto: Europa Idioma: En Revista: Biochem Biophys Res Commun Año: 1998 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos