Establishment of a novel cell model targeted on FGF-21 receptor for screening anti-diabetic drug candidates / 药学学报
Acta Pharmaceutica Sinica
; (12): 904-909, 2011.
Article
en Zh
| WPRIM
| ID: wpr-233078
Biblioteca responsable:
WPRO
ABSTRACT
The aim of this project is to establish a fibroblast growth factor-21 (FGF-21) signaling pathway targeted cell model, for screening a class of FGF-21 receptor agonists as anti-diabetic candidates. FGF-21 requires beta klotho transmembrane proteins as co-receptor for the activation of tyrosine kinase FGF receptor (FGFR) signaling, thereby activating a series of intracellular signaling pathways and regulating gene transcription for glucose metabolism. Firstly a recombinant plasmid expressing co-receptor beta klotho and EGFP reporter genes was constructed. After introducing the recombinant plasmid into package cells, the cell culture supernatant was used to infect 3T3-L1 cells, which were then screened for stably expressing beta klotho gene. Administration of FGF-21 increased the expression of GLUT1 and stimulated GLUT1-mediated glucose uptake. This novel cell model can be conveniently used in high-throughput drug screening of FGF-21 or FGF-21 analogues.
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1
Índice:
WPRIM
Asunto principal:
Farmacología
/
Plásmidos
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Retroviridae
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Proteínas Recombinantes
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ARN Mensajero
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Transfección
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Transducción de Señal
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Receptores de Factores de Crecimiento de Fibroblastos
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Células 3T3 NIH
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Células 3T3-L1
Tipo de estudio:
Diagnostic_studies
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Prognostic_studies
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Screening_studies
Límite:
Animals
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Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2011
Tipo del documento:
Article