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| Content Provider | PubMed Central |
|---|---|
| Author | Rene, Raphemot Weaver, C. David Denton, Jerod S. |
| Copyright Year | 2013 |
| Abstract | Specific members of the inward rectifier potassium (Kir) channel family are postulated drug targets for a variety of disorders, including hypertension, atrial fibrillation, and pain1,2. For the most part, however, progress toward understanding their therapeutic potential or even basic physiological functions has been slowed by the lack of good pharmacological tools. Indeed, the molecular pharmacology of the inward rectifier family has lagged far behind that of the S4 superfamily of voltage-gated potassium (Kv) channels, for which a number of nanomolar-affinity and highly selective peptide toxin modulators have been discovered3. The bee venom toxin tertiapin and its derivatives are potent inhibitors of Kir1.1 and Kir3 channels4,5, but peptides are of limited use therapeutically as well as experimentally due to their antigenic properties and poor bioavailability, metabolic stability and tissue penetrance. The development of potent and selective small-molecule probes with improved pharmacological properties will be a key to fully understanding the physiology and therapeutic potential of Kir channels. |
| Related Links | http://dx.doi.org/10.3791/4209 |
| Starting Page | 4209 |
| File Format | |
| ISSN | 1940087X |
| e-ISSN | 1940087X |
| Journal | Journal of Visualized Experiments : JoVE |
| Issue Number | 71 |
| Language | English |
| Publisher | MyJove Corporation |
| Publisher Date | 2013-01-01 |
| Access Restriction | Open |
| Rights Holder | MyJove Corporation |
| Subject Keyword | Biochemistry, Genetics and Molecular Biology(all) Immunology and Microbiology(all) Chemical Engineering(all) Neuroscience(all) Medicine(all) Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Neuroscience Immunology and Microbiology Biochemistry, Genetics and Molecular Biology Chemical Engineering |
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