Journal article
The pharmacology of cyclic nucleotide-gated channels: emerging from the darkness
Current pharmaceutical design, Vol.12(28), pp.3597-3613
2006
Handle:
https://hdl.handle.net/2376/111493
PMID: 17073662
Abstract
Cyclic nucleotide-gated (CNG) ion channels play a central role in vision and olfaction, generating the electrical responses to light in photoreceptors and to odorants in olfactory receptors. These channels have been detected in many other tissues where their functions are largely unclear. The use of gene knockouts and other methods have yielded some information, but there is a pressing need for potent and specific pharmacological agents directed at CNG channels. To date there has been very little systematic effort in this direction - most of what can be termed CNG channel pharmacology arose from testing reagents known to target protein kinases or other ion channels, or by accident when researchers were investigating other intracellular pathways that may regulate the activity of CNG channels. Predictably, these studies have not produced selective agents. However, taking advantage of emerging structural information and the increasing knowledge of the biophysical properties of these channels, some promising compounds and strategies have begun to emerge. In this review we discuss progress on two fronts, cyclic nucleotide analogs as both activators and competitive inhibitors, and inhibitors that target the pore or gating machinery of the channel. We also discuss the potential of these compounds for treating certain forms of retinal degeneration.
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Details
- Title
- The pharmacology of cyclic nucleotide-gated channels: emerging from the darkness
- Creators
- R Lane Brown - Neurological Sciences Institute, Oregon Health & Science University, Portland, OR 97239, USATimothy StrassmaierJames D BradyJeffrey W Karpen
- Publication Details
- Current pharmaceutical design, Vol.12(28), pp.3597-3613
- Academic Unit
- Integrative Physiology and Neuroscience, Department of
- Publisher
- United Arab Emirates
- Grant note
- EY012837 / NEI NIH HHS R01 EY012837 / NEI NIH HHS EY009275 / NEI NIH HHS R01 EY009275 / NEI NIH HHS R01 EY012837-03 / NEI NIH HHS
- Identifiers
- 99900547598701842
- Language
- English
- Resource Type
- Journal article