Screening for adiponectin secretion regulators

Vitam Horm. 2012:90:125-41. doi: 10.1016/B978-0-12-398313-8.00005-1.


Adiponectin is an adipokine secreted from adipocytes and plays important roles in the suppression of metabolic syndromes that can result in type 2 diabetes, obesity, and atherosclerosis. Adiponectin is a promising drug target because a number of studies have shown that upregulation of adiponectin has a number of therapeutic benefits. Extensive efforts have revealed various adiponectin regulators, such as cytokines, transcription factors, and drugs. Cytokines, such as tumor necrosis factor α, IL-6, and IL-18, downregulate adiponectin production. On the other hand, transcription factors such as peroxisome proliferator-activated receptor-γ (PPARγ), CCAAT-enhancer-binding protein α, and forkhead box O1 (FoxO1) upregulate adiponectin expression, although the activating transcription factor 3 and cAMP response element-binding protein downregulate it. Although a number of therapeutic drugs have been reported as adiponectin secretion regulators, most of them act through PPARγ-dependent mechanisms, leaving PPARγ-derived side effects as a concern. Using high-throughput screening, we have identified PPARγ-independent adiponectin secretion regulators as potential drug candidates with a novel mechanism of action.

Publication types

  • Review

MeSH terms

  • 3T3-L1 Cells
  • Adipocytes / metabolism*
  • Adiponectin / genetics
  • Adiponectin / metabolism*
  • Animals
  • CCAAT-Enhancer-Binding Protein-alpha / physiology
  • Cytokines / physiology*
  • Forkhead Box Protein O1
  • Forkhead Transcription Factors / physiology
  • Gene Expression Regulation
  • Humans
  • Mice
  • PPAR gamma / physiology
  • Transcription Factors / physiology*


  • Adiponectin
  • CCAAT-Enhancer-Binding Protein-alpha
  • Cytokines
  • FOXO1 protein, human
  • Forkhead Box Protein O1
  • Forkhead Transcription Factors
  • PPAR gamma
  • Transcription Factors