Roles for novel pharmacological blockers of aquaporins in the treatment of brain oedema and cancer.

摘要: 1. Aquaporins (AQPs) are targets for drug discovery basic research and medicine. Human diseases involving fluid imbalances oedema of major concern involve tissues in which AQPs expressed. The range functional properties is continuing to expand steadily with ongoing the field. 2. Gating domains molecular sites actions. Discovery arylsulphonamide AqB013 as an antagonist AQP1 AQP4 provided first pharmacological agent translational promise treatment have been implicated. putative binding site internal vestibule AQP water pore involves amino acid residues that located loop D gating domain. 3. proposed novel cancer associated a surprising array important processes brain body, such angiogenesis, cell migration, development neuropathological diseases. Functions beyond their simple role channels suggested by subtype-specific regulation expression. In both oedema, current therapies limited new approaches focused on offer exciting potential clinical advances.