title: [Establishment of a novel cell model targeted on FGF-21 receptor for screening anti-diabetic drug candidates].
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.
authors: College of Life Science of Northeast Agricultural University. Harbin 150030, China.
authors: Hong-Mei
authors: HM
authors: Gao
authors: Wen-Fei
authors: WF
authors: Wang
authors: Qiao
authors: Q
authors: Zhang
authors: Yang
authors: Y
authors: Han
authors: Qi
authors: Q
authors: Wang
authors: Gui-Ping
authors: GP
authors: Ren
authors: Yun-Wei
authors: YW
authors: Fu
authors: De-Shan
authors: DS
authors: Li
mesh_terms: D041721:3T3-L1 Cells; D000818:Animals; D004353:Drug Evaluation, Preclinical; D005346:Fibroblast Growth Factors / Q000378:metabolism / Q000494:pharmacology*; D005947:Glucose / Q000378:metabolism; D051272:Glucose Transporter Type 1 / Q000235:genetics / Q000378:metabolism; D051275:Glucose Transporter Type 4 / Q000235:genetics / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000378:metabolism*; D000090265:Klotho Proteins; D008565:Membrane Proteins / Q000235:genetics* / Q000378:metabolism; D051379:Mice; D041681:NIH 3T3 Cells; D010957:Plasmids; D012333:RNA, Messenger / Q000378:metabolism; D017468:Receptors, Fibroblast Growth Factor / Q000819:agonists*; D011994:Recombinant Proteins / Q000235:genetics / Q000378:metabolism; D012190:Retroviridae / Q000235:genetics; D015398:Signal Transduction; D014162:Transfection
chemical_list: D051272:Glucose Transporter Type 1; D051275:Glucose Transporter Type 4; D007004:Hypoglycemic Agents; C538995:KLB protein, human; D008565:Membrane Proteins; D012333:RNA, Messenger; D017468:Receptors, Fibroblast Growth Factor; D011994:Recombinant Proteins; C414620:fibroblast growth factor 21; C526616:fibroblast growth factor-21 receptor, mouse; D005346:Fibroblast Growth Factors; D000090265:Klotho Proteins; D005947:Glucose