Aquaporins in drug discovery and pharmacotherapy

Mol Aspects Med. Oct-Dec 2012;33(5-6):691-703. doi: 10.1016/j.mam.2012.01.002. Epub 2012 Jan 24.

Abstract

Identification of the aquaporin (AQP) protein family more than twenty years ago has ushered in an era where water and neutral solute trafficking is considered a prime target for pharmacological intervention. Using AQP modulation as a basis for the treatment of human disorders has been suggested by phenotype analysis involving specific AQP-null animals, as well as by pathohistological studies. Based on those reports, a wide variety of disorders, such as cerebral edema, cancer and malaria, are considered indications for AQP modulators. Recent studies have also identified several small molecule AQP modulators that can be used to test those hypotheses in disease models. We believe these studies and compounds form the basis from which future treatments and diagnostic protocols of aquaporin-based disorders will be developed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acetazolamide / pharmacology
  • Animals
  • Aquaporins / antagonists & inhibitors
  • Aquaporins / chemistry
  • Aquaporins / metabolism*
  • Biological Transport / drug effects
  • Brain Edema / drug therapy*
  • Brain Edema / metabolism
  • Brain Edema / pathology
  • Bumetanide / pharmacology
  • Drug Discovery
  • Humans
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Niacinamide / analogs & derivatives
  • Niacinamide / pharmacology
  • Thiadiazoles / pharmacology
  • Water / metabolism*
  • Water-Electrolyte Balance / drug effects
  • Water-Electrolyte Imbalance / drug therapy*
  • Water-Electrolyte Imbalance / metabolism
  • Water-Electrolyte Imbalance / pathology

Substances

  • 2-(nicotinamide)-1,3,4-thiadiazole
  • Aquaporins
  • Thiadiazoles
  • Water
  • Bumetanide
  • Niacinamide
  • Acetazolamide