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FGF21 inhibits apolipoprotein(a) expression in HepG2 cells via the FGFR1-ERK1/2-Elk-1 pathway

Xiaolong Lin1, Guohua Li, Xinglan He

  • 1Key Laboratory for Arteriosclerology of Hunan Province, Institute of Cardiovascular Disease, University of South China, Hengyang, 421001, China, 493814078@qq.com.

Molecular and Cellular Biochemistry
|April 5, 2014
PubMed

Insights

Fibroblast growth factor-21 (FGF21) effectively reduces apolipoprotein(a) [apo(a)] production and secretion. This occurs through the FGF21 receptor (FGFR1), impacting the ERK1/2-Elk-1 signaling pathway, offering potential therapeutic strategies for high lipoprotein(a) levels.

Area of Science:

  • Cardiovascular Biology
  • Molecular Endocrinology
  • Lipid Metabolism

Background:

  • Elevated Lipoprotein(a) [Lp(a)] is a significant risk factor for atherosclerosis.
  • Current therapeutic options for lowering Lp(a) are limited.
  • Fibroblast growth factor-21 (FGF21) is known to regulate glucose and lipid metabolism.

Purpose of the Study:

  • To investigate the molecular mechanisms underlying apolipoprotein(a) [apo(a)] biosynthesis.
  • To determine the effects of FGF21 on apo(a) expression and secretion in HepG2 cells.
  • To elucidate the signaling pathway mediating FGF21's effects on apo(a).

Main Methods:

  • Dose- and time-dependent analysis of FGF21 on apo(a) mRNA and protein levels.
  • Assessment of apo(a) secretion in HepG2 cells.
  • Utilized ERK1/2 inhibitor (PD98059), Elk-1 siRNA, and FGFR1 inhibitor (PD166866) to probe the signaling pathway.

Main Results:

  • FGF21 significantly inhibited apo(a) expression at both mRNA and protein levels.
  • FGF21 suppressed the secretion of apo(a) from HepG2 cells.
  • The inhibitory effects of FGF21 were dependent on the FGFR1-ERK1/2-Elk-1 pathway.

Conclusions:

  • FGF21 suppresses apolipoprotein(a) expression and secretion.
  • The mechanism involves the FGF21 receptor (FGFR1) and downstream signaling via ERK1/2 and Elk-1.
  • This pathway represents a potential therapeutic target for managing elevated Lp(a).

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