Abstract
Aquaporins (AQPs) have been proved to be important physiological 'partners' for metal and metalloid compounds, either as their transporters or as targets for inhibition. Here, we summarize the key findings on how AQP channels contribute to the accumulation of metalloids in cells. Specifically, the elucidation of the mechanisms of metalloids uptake by aquaporins provides an understanding of (1) inorganic elements toxicity and (2) how the delivery of arsenic and antimony-containing drugs is crucial in the treatment of certain forms of leukaemia and chemotherapy of diseases caused by pathogenic protozoa. Moreover, a description of the state-of-the-art progresses in the discovery of new metal-based inhibitors, after mercurial compounds and other transition metal ions, is provided. Among them, coordination gold(III) complexes as aquaglyceroporins inhibitors are presented with special focus on their mechanism of action at a molecular level, and with indication 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 language | English |
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Title of host publication | Aquaporins in Health and Disease |
Subtitle of host publication | New Molecular Targets for Drug Discovery |
Publisher | CRC Press |
Pages | 297-318 |
Number of pages | 22 |
ISBN (Electronic) | 9781498707848 |
ISBN (Print) | 9781498707831 |
State | Published - 6 Jan 2016 |
Externally published | Yes |