Fatty acid and mineral receptors as drug targets for gastrointestinal disorders

Future Med Chem. 2017 Mar;9(3):315-334. doi: 10.4155/fmc-2016-0205. Epub 2017 Feb 16.

Abstract

Nutrient-sensing receptors, including fatty acid receptors (FFA1-FFA4), Ca2+-sensing receptors and Zn2+-sensing receptors, are involved in several biological processes. These receptors are abundantly expressed in the GI tract, where they have been shown to play crucial roles in regulating GI function. This review provides an overview of the GI functions of fatty acid and mineral receptors, including the regulation of gastric and enteroendocrine functions, GI motility, ion transport and cell growth. Recently, several lines of evidence have implicated these receptors as promising therapeutic targets for the treatment of GI disorders, for example, inflammatory bowel disease, colorectal cancer, metabolic syndrome and diarrheal diseases. A future perspective on drug discovery research targeting these receptors is discussed.

Keywords: calcium-sensing receptor; fatty acid receptors; zinc-sensing receptor.

Publication types

  • Review

MeSH terms

  • Animals
  • Calcium / metabolism*
  • Colorectal Neoplasms / drug therapy
  • Colorectal Neoplasms / metabolism
  • Drug Discovery
  • Fatty Acids / metabolism*
  • Gastrointestinal Diseases / drug therapy*
  • Gastrointestinal Diseases / metabolism
  • Gastrointestinal Tract / drug effects
  • Humans
  • Inflammatory Bowel Diseases / drug therapy
  • Inflammatory Bowel Diseases / metabolism
  • Intestinal Mucosa / metabolism*
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / metabolism*
  • Zinc / metabolism*

Substances

  • Fatty Acids
  • Receptors, G-Protein-Coupled
  • Zinc
  • Calcium