Aquaporins in drug discovery and pharmacotherapy

Down-regulated aquaporin 5 inhibits proliferation and migration of human epithelial ovarian cancer 3AO cells

“…Aquaporins are found to mainly function as molecular transporters and involve in many disease progresses such as various chronic kidney disease, systemic disease and cancers [7][8][9][10]. Recent studies suggest that Aquaporins could be a promising drug target [11,12].…”

The AQP-3 water channel and the ClC-3 chloride channel coordinate the hypotonicity-induced swelling volume in nasopharyngeal carcinoma cells

“…It has been reported that AQPs are abnormally expressed in specific tissues and cells, contributing to the development of obesity, diabetes, atherosclerosis, tumourigenesis, tumour proliferation, invasion and metastasis among others. AQPs have been considered potential targets for drug discovery to treat these disorders (Frede et al, 2013;He et al, 2008;Huber et al, 2012;Verkman, 2012). The aquaglyceroporin AQP-3 transports water as well as glycerol and possibly urea and other small solutes (Hara-Chikuma and Verkman, 2006;Wang et al, 2009).…”

“…ClC-3 chloride channels and AQPs are involved in the growth/proliferation, migration and/or invasion of cancer cells, and cell volume regulation plays a pivotal role in all of these processes (Frede et al, 2013;Huber et al, 2012;Liu et al, 2013;Mao et al, 2012Mao et al, , 2013Verkman, 2012;Zhang et al, 2013a,b;Zhu et al, 2012). The ClC-3 volume-sensitive Cl − channel has been confirmed to be expressed in cancerous nasopharyngeal epithelial cells by us previously, but the expression of AQPs in these cells has not been clarified.…”

Challenges and achievements in the therapeutic modulation of aquaporin functionality

“…AQP1 and AQP4 are expressed in the iris and the ciliar epithelium and are thought to carry the major portion of chamber water production (Zhang et al, 2002). Increased intraocular pressure, glaucoma, poses stress to the cells of the retina and the optic nerve (Huber et al, 2012). There are pharmacological agents for the treatment of both, wide-angle and narrow-angle glaucoma, and inhibitors of AQP1 and AQP4 may become alternatives to adjust water regulation in the eye.…”