ArticleScientific reports2015
Resin-acid derivatives as potent electrostatic openers of voltage-gated K channels and suppressors of neuronal excitability.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 25 citations in OpenAlex.
- Carboxyl-group compounds activate voltage-gated potassium channels via a distinct mechanism.The Journal of general physiology · 2024Article
- Therapeutic role of voltage-gated potassium channels in age-related neurodegenerative diseases.Frontiers in cellular neuroscience · 2024Review
- A novel Hv1 inhibitor reveals a new mechanism of inhibition of a voltage-sensing domain.The Journal of general physiology · 2021Article
- Resin-acid derivatives bind to multiple sites on the voltage-sensor domain of the Shaker potassium channel.The Journal of general physiology · 2021Article
- Coupling stabilizers open KProceedings of the National Academy of Sciences of the United States of America · 2020Article
- Kv1.1 Channelopathies: Pathophysiological Mechanisms and Therapeutic Approaches.International journal of molecular sciences · 2020Review
- Polyunsaturated fatty acids produce a range of activators for heterogeneous IKs channel dysfunction.The Journal of general physiology · 2020Article
- Optoelectronic control of single cells using organic photocapacitors.Science advances · 2019Article
- Biaryl sulfonamide motifs up- or down-regulate ion channel activity by activating voltage sensors.The Journal of general physiology · 2018Article
- Atom-by-atom tuning of the electrostatic potassium-channel modulator dehydroabietic acid.The Journal of general physiology · 2018Article
- A drug pocket at the lipid bilayer-potassium channel interface.Science advances · 2017Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Voltage-gated ion channels generate cellular excitability, cause diseases when mutated, and act as drug targets in hyperexcitability diseases, such as epilepsy, cardiac arrhythmia and pain. Unfortunately, many patients do not satisfactorily respond to the present-day drugs. We found that the naturally occurring resin acid dehydroabietic acid (DHAA) is a potent opener of a voltage-gated K channel and thereby a potential suppressor of cellular excitability. DHAA acts via a non-traditional mechanism, by electrostatically activating the voltage-sensor domain, rather than directly targeting the ion-conducting pore domain. By systematic iterative modifications of DHAA we synthesized 71 derivatives and found 32 compounds more potent than DHAA. The most potent compound, Compound 77, is 240 times more efficient than DHAA in opening a K channel. This and other potent compounds reduced excitability in dorsal root ganglion neurons, suggesting that resin-acid derivatives can become the first members of a new family of drugs with the potential for treatment of hyperexcitability diseases.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.