Gold compounds as aquaporin inhibitors: New opportunities for therapy and imaging

Andreia de Almeida, Graca Soveral, Angela Casini*

*Corresponding author for this work

Research output: Contribution to journalReview articleAcademicpeer-review

22 Citations (Scopus)

Abstract

In recent years, gold-based compounds have been proved to hold promise in chemical biology being able to selectively inhibit proteins activities in cells and, therefore, to be exploited as either therapeutic agents or as chemical tools to detect protein/enzyme functions in living systems. In this area, we have recently described the properties of gold coordination complexes as potent and selective inhibitors of human aquaporins, protein channels involved in the transport of water and glycerol across biomembranes. Thus, we provide here an overview of the importance of aquaporins in various diseases and a detailed description of the state-of-the art progresses in the discovery of new inhibitors, including gold(III) complexes, and a description of their possible applications. Overall, the potential of coordination chemistry in providing compounds to modulate the activity of "elusive" drug targets, such as the aquaporins, will be discussed.

Original languageEnglish
Pages (from-to)1444-1453
Number of pages10
JournalMedChemComm
Volume5
Issue number10
DOIs
Publication statusPublished - Oct-2014

Keywords

  • WATER CHANNEL
  • PLASMODIUM-FALCIPARUM
  • GLYCEROL PERMEABILITY
  • CELL-MIGRATION
  • SELECTIVITY
  • EXPRESSION
  • AGENTS
  • MICE
  • AQUAGLYCEROPORINS
  • PERMEATION

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