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Aquaporin modulators: a patent review (2010-2015)

Soveral, Graça and Casini, Angela 2017. Aquaporin modulators: a patent review (2010-2015). Expert Opinion on Therapeutic Patents 27 (1) , pp. 49-62. 10.1080/13543776.2017.1236085

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Introduction: Since the discovery of aquaporin-1 (AQP1) as a water channel, more than 2,000 articles, reviews and chapters have been published. The wide tissue expression, functional and biological roles have documented the major and essential physiological importance of these channels both in health and disease. Thus, over the years, studies have revealed essential importance of aquaporins in mammalian pathophysiology revealing aquaporins as potential drug targets. Areas covered: Starting from a brief description of the main structural and functional features of aquaporins, their roles in physiology and pathophysiology of different human diseases, this review describes the main classes of small molecules and biologicals patented, published from 2010 to 2015, able to regulate AQPs for diagnostic and therapeutic applications. Expert opinion: Several patents report on AQP modulators, mostly inhibitors, and related pharmaceutical formulations, to be used for treatments of water imbalance disorders, such as edema. Noteworthy, a unique class of gold-based compounds as selective inhibitors of aquaglyceroporin isoforms may provide new chemical tools for therapeutic applications, especially in cancer. AQP4-targeted therapies for neuromyelitis optica, enhancement of AQP2 function for nephrogenic diabetes insipidus and AQP1-5 gene transfer for the Sjogren’s syndrome represent promising therapies that deserve further investigation by clinical trials.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Uncontrolled Keywords: aquaporins, small-molecule inhibitors, gold compounds, biologicals, cancer, edema, nephrogenic diabetes insipidus, neuromyelitis optica,
Publisher: Informa Healthcare
ISSN: 1354-3776
Funders: EU COST Action CM1106
Date of First Compliant Deposit: 14 September 2016
Date of Acceptance: 2 September 2016
Last Modified: 27 Nov 2020 20:58

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