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Molecular elements in FGF19 and FGF21 defining KLB/FGFR activity and specificity.

Mol Metab. 2018-07; 
AgrawalArchita,ParleeSebastian,Perez-TilveDiego,LiPengyun,PanJia,MrozPiotr A,Kruse HansenAnn Maria,AndersenBirgitte,FinanBrian,KharitonenkovAlexei,DiMarchiRicha
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Proteins, Expression, Isolation and Analysis … ProtParam). FGF21, FGF19, FGF21-19A protein preparations used for in vivo studies were purified from endotoxin by ToxinEraser Endotoxin removal kit (GenScript) to ensure 0.5 EU/mg or less endotoxin. 2.4. Cell lines. For generating … Get A Quote

摘要

To signal, FGF19 and FGF21 require co-receptor βKlotho (KLB) to act in concert with FGF receptors, and yet there is appreciable variance in the C-terminal sequences of these two novel metabolic hormones where binding is believed to be primary. We seek to determine the functional consequences for these amino acid differences and determine whether such information can be used to design high potency antagonists and agonists.

关键词

Alanine-scan,FGF antagonism,FGF19,FGF21,FGFR isoforms,KLB,Structure-activity-relation