English
español
Por favor, use este identificador para citar o enlazar a este item:
http://hdl.handle.net/10261/16146
COMPARTIR / IMPACTO:
Estadísticas |
![]() ![]() ![]() |
|
|
Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL | |||
Título: | Kinetic assay for high-throughput screening of in vitro transthyretin amyloid fibrillogenesis inhibitors |
Autor: | Dolado, Ignacio; Nieto, Joan; Saraiva, Maria João; Arsequell, Gemma; Valencia Parera, Gregorio; Planas, Antoni |
Palabras clave: | Kinetic assay In vitro inhibitors hTTR Amyloid Fibril High-Throughput Screening |
Fecha de publicación: | 10-feb-2005 |
Editor: | American Chemical Society |
Citación: | Journal of Combinatorial Chemistry 7(2): 246-252 (2005) |
Resumen: | Stabilization of tetrameric transthyretin (TTR) by binding of small ligands is a current strategy aimed at inhibiting amyloid fibrillogenesis in transthyretin-associated pathologies, such as senile systemic amyloidosis (SSA) and familial amyloidotic polyneuropathy (FAP). A kinetic assay is developed for rapid evaluation of compounds as potential in vitro inhibitors in a high-throughput screening format. It is based on monitoring the time-dependent increase of absorbance due to turbidity occurring by acid-induced protein aggregation. The method uses the highly amyloidogenic Y78F mutant of human transthyretin (heterogously expressed in Escherichia coli cells). Initial rates of protein aggregation at different inhibitor concentrations follow a monoexponential dose−response curve from which inhibition parameters are calculated. For the assay development, thyroid hormones and nonsteroidal antiinflamatory drugs were chosen among other reference compounds. Some of them are already known to be in vitro inhibitors of TTR amyloidogenesis. Analysis time is optimized to last 1.5 h, and the method is implemented in microtiter plates for screening of libraries of potential fibrillogenesis inhibitors. |
Descripción: | 7 pages, 4 figures, 1 scheme, 2 tables.-- PMID: 15762752 [PubMed].-- Printed version published Mar 2005. |
Versión del editor: | http://dx.doi.org/10.1021/cc049849s |
URI: | http://hdl.handle.net/10261/16146 |
DOI: | 10.1021/cc049849s |
ISSN: | 1520-4766 (Print) 1520-4774 (Online) |
Aparece en las colecciones: | (IQAC) Artículos |
Ficheros en este ítem:
No hay ficheros asociados a este ítem.
Mostrar el registro completo
Artículos relacionados:
NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.