Diet1 is a regulator of fibroblast growth factor 15/19-dependent bile acid synthesis

Dig Dis. 2015;33(3):307-13. doi: 10.1159/000371649. Epub 2015 May 27.

Abstract

Background: A fascinating aspect of bile acid homeostasis is the coordination between bile acid uptake in intestine and hepatic bile acid synthesis. In response to bile acid uptake in enterocytes, farnesoid X receptor is activated and induces transcription of fibroblast growth factor (FGF)15 in mice, or FGF19 in humans. FGF15/19 is secreted into the enterohepatic circulation, and through activation of hepatic receptors, leads to repression of Cyp7a1, a rate-limiting enzyme for bile acid synthesis. Using a genetic approach, we identified a novel protein, Diet1, as a control point for FGF15/19 production.

Key messages: Mice with a Diet1-null mutation have reduced FGF15 secretion, causing impaired feedback repression of hepatic bile acid synthesis, and increased fecal bile acid excretion. As a result, Diet1-deficient mice constitutively convert cholesterol to bile acids and are resistant to diet-induced hypercholesterolemia and atherosclerosis. Diet1 affects FGF15/19 production at the posttranscriptional level, and the proteins appear to have overlapping subcellular localization in enterocytes. Diet1 appears to be a control point for the production of FGF15/19 in enterocytes, and thus a regulator of bile acid and lipid homeostasis. Studies to evaluate the role of common and rare DIET1 genetic variants in human health and disease are warranted.

Conclusions: Further elucidation of the Diet1-FGF15/19 interaction will provide new insights into the intricate regulatory mechanisms underlying bile acid metabolism.

MeSH terms

  • Animals
  • Bile Acids and Salts / biosynthesis*
  • Carrier Proteins / genetics
  • Carrier Proteins / metabolism*
  • Cholesterol 7-alpha-Hydroxylase / antagonists & inhibitors
  • Enterocytes / metabolism
  • Fibroblast Growth Factors / genetics
  • Fibroblast Growth Factors / metabolism*
  • Glucose / metabolism
  • HT29 Cells
  • Homeostasis*
  • Humans
  • Mice
  • Polymorphism, Genetic
  • RNA, Messenger / metabolism
  • Rats
  • Receptors, LDL / genetics
  • Receptors, LDL / metabolism*

Substances

  • Bile Acids and Salts
  • Carrier Proteins
  • Diet1 protein, mouse
  • FGF19 protein, human
  • MALRD1 protein, human
  • RNA, Messenger
  • Receptors, LDL
  • fibroblast growth factor 15, mouse
  • Fibroblast Growth Factors
  • CYP7A1 protein, human
  • Cholesterol 7-alpha-Hydroxylase
  • Cyp7a1 protein, mouse
  • Glucose