ArticleProceedings of the National Academy of Sciences of the United States of America2008
Engineered specific and high-affinity inhibitor for a subtype of inward-rectifier K+ channels.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Classical conditioning of Purkinje cell responsesBiochemistry and biophysics reports · 2026Article
- Characterizing molecular and behavioral changes arising from ROMK potassium channel deficiency in the cerebellum.Frontiers in behavioral neuroscience · 2025Article
- Neuromedin B excites central lateral amygdala neurons and reduces cardiovascular output and fear-potentiated startle.Journal of cellular physiology · 2023Article
- Roles of PLCβ, PIPJournal of cellular physiology · 2022Article
- Oxytocin receptors excite lateral nucleus of central amygdala by phospholipase Cβ- and protein kinase C-dependent depression of inwardly rectifying KThe Journal of physiology · 2020Article
- Antidepressive effect of an inward rectifier K+ channel blocker peptide, tertiapin-RQ.PloS one · 2020Article
- Identification ofToxins · 2019Article
- µ-Opioid receptors inhibit the exercise pressor reflex by closing N-type calcium channels but not by opening GIRK channels in rats.American journal of physiology. Regulatory, integrative and comparative physiology · 2018Article
- A computational design approach for virtual screening of peptide interactions across K(+) channel families.Computational and structural biotechnology journal · 2015Article
- Differential phospholipase C-dependent modulation of TASK and TREK two-pore domain K+ channels in rat thalamocortical relay neurons.The Journal of physiology · 2015Article
- Inward rectifier potassium (Kir) current in dopaminergic periglomerular neurons of the mouse olfactory bulb.Frontiers in cellular neuroscience · 2014Article
- Novel molecular targets for atrial fibrillation therapy.Nature reviews. Drug discovery · 2012Review
- Article
- Review
- The nociceptive and anti-nociceptive effects of bee venom injection and therapy: a double-edged sword.Progress in neurobiology · 2010Review
- A designer ligand specific for Kv1.3 channels from a scorpion neurotoxin-based library.Proceedings of the National Academy of Sciences of the United States of America · 2009Article
- Random mutagenesis screening indicates the absence of a separate H(+)-sensor in the pH-sensitive Kir channels.Channels (Austin, Tex.)Article
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Authors and funding
3 authors.
Funding
Abstract
Inward-rectifier K(+) (Kir) channels play many important biological roles and are emerging as important therapeutic targets. Subtype-specific inhibitors would be useful tools for studying the channels' physiological functions. Unfortunately, available K(+) channel inhibitors generally lack the necessary specificity for their reliable use as pharmacological tools to dissect the various kinds of K(+) channel currents in situ. The highly conserved nature of the inhibitor targets accounts for the great difficulty in finding inhibitors specific for a given class of K(+) channels or, worse, individual subtypes within a class. Here, by modifying a toxin from the honey bee venom, we have successfully engineered an inhibitor that blocks Kir1 with high (1 nM) affinity and high (>250-fold) selectivity over many commonly studied Kir subtypes. This success not only yields a highly desirable tool but, perhaps more importantly, demonstrates the practical feasibility of engineering subtype-specific K(+) channel inhibitors.
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Registered trials
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.