| Chapter title |
Aquaporin-Targeted Therapeutics: State-of-the-Field
|
|---|---|
| Chapter number | 16 |
| Book title |
Aquaporins
|
| Published in |
Advances in experimental medicine and biology, March 2017
|
| DOI | 10.1007/978-94-024-1057-0_16 |
| Pubmed ID | |
| Book ISBNs |
978-9-40-241055-6, 978-9-40-241057-0
|
| Authors |
Lukmanee Tradtrantip Ph.D., Bjung-Ju Jin Ph.D., Xiaoming Yao M.D., Marc O. Anderson Ph.D., Alan S. Verkman M.D., Ph.D., Lukmanee Tradtrantip, Bjung-Ju Jin, Xiaoming Yao, Marc O. Anderson, Alan S. Verkman, Tradtrantip, Lukmanee, Jin, Bjung-Ju, Yao, Xiaoming, Anderson, Marc O., Verkman, Alan S. |
| Editors |
Baoxue Yang |
| Abstract |
Drugs targeting aquaporins have broad potential clinical applications, including cancer, obesity, edema, glaucoma, skin diseases and others. The astrocyte water channel aquaporin-4 is a particularly compelling target because of its role of brain water movement, neuroexcitation and glia scarring, and because it is the target of pathogenic autoantibodies in the neuroinflammatory demyelinating disease neuromyelitis optica . There has been considerable interest in the identification of small molecule inhibitors of aquaporins, with various candidates emerging from testing of known ion transport inhibitors, as well as compound screening and computational chemistry. However, in general, the activity of reported aquaporin inhibitors has not been confirmed on retesting, which may be due to technical problems in water transport assays used in the original identification studies, and the challenges in modulating the activity of small, compact, pore-containing membrane proteins. We review here the state of the field of aquaporin-modulating small molecules and biologics, and the challenges and opportunities in moving forward. |
Mendeley readers
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 49 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 10 | 20% |
| Student > Ph. D. Student | 9 | 18% |
| Researcher | 7 | 14% |
| Student > Postgraduate | 2 | 4% |
| Student > Master | 2 | 4% |
| Other | 3 | 6% |
| Unknown | 16 | 33% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 8 | 16% |
| Medicine and Dentistry | 6 | 12% |
| Agricultural and Biological Sciences | 5 | 10% |
| Neuroscience | 5 | 10% |
| Immunology and Microbiology | 3 | 6% |
| Other | 6 | 12% |
| Unknown | 16 | 33% |