ArticleThe Journal of biological chemistry2010
Biochemical characterization of kappaM-RIIIJ, a Kv1.2 channel blocker: evaluation of cardioprotective effects of kappaM-conotoxins.
Article in The Journal of biological chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 41 citations in OpenAlex.
- From Marine Peptides to Oncology: The Therapeutic Potential of Conotoxins in Cancer Treatment.Chemistry & biodiversity · 2026Review
- From marine predator to pharmacology: Conotoxin diversity, discovery, and therapeutic potential.Zoological research · 2026Review
- Conotoxin KM-RIIIJ reveals interplay between KScientific reports · 2024Article
- Transcriptional regulation of KCNA2 coding Kv1.2 by EWS::FLI1: involvement in controlling the YAP/Hippo signalling pathway and cell proliferation.Cell communication and signaling : CCS · 2024Article
- Peptide Toxins from MarineToxins · 2024Review
- Roles of KCNA2 in Neurological Diseases: from Physiology to Pathology.Molecular neurobiology · 2024Review
- Voltage-Gated KMarine drugs · 2024Review
- Electrophysiological evaluation of the effect of peptide toxins on voltage-gated ion channels: a scoping review on theoretical and methodological aspects with focus on the Central and South American experience.The journal of venomous animals and toxins including tropical diseases · 2024Article
- κO-SrVIA Conopeptide, a Novel Inhibitor Peptide for Two Members of the Human EAG Potassium Channel Family.International journal of molecular sciences · 2023Article
- Pathophysiological Responses to Conotoxin Modulation of Voltage-Gated Ion Currents.Marine drugs · 2022Review
- Refining Genotypes and Phenotypes inInternational journal of molecular sciences · 2021Article
- A novel proline-rich M-superfamily conotoxin that can simultaneously affect sodium, potassium and calcium currents.The journal of venomous animals and toxins including tropical diseases · 2021Article
- Curses or Cures: A Review of the Numerous Benefits Versus the Biosecurity Concerns of Conotoxin Research.Biomedicines · 2020Review
- Marine Toxins Targeting Kv1 Channels: Pharmacological Tools and Therapeutic Scaffolds.Marine drugs · 2020Review
- An integrative approach to the facile functional classification of dorsal root ganglion neuronal subclasses.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Structural and Functional Analyses of Cone Snail Toxins.Marine drugs · 2019Review
- Conotoxin κM-RIIIJ, a tool targeting asymmetric heteromeric KProceedings of the National Academy of Sciences of the United States of America · 2019Article
- Discovery Methodology of Novel Conotoxins fromMarine drugs · 2018Review
- The Role of Kv1.2 Channel in Electrotaxis Cell Migration.Journal of cellular physiology · 2016Article
- Phosphoinositide Modulation of Heteromeric Kv1 Channels Adjusts Output of Spiral Ganglion Neurons from Hearing Mice.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2015Article
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Authors and funding
5 authors at 4 institutions in 3 countries.
Funding
Abstract
Conus snail (Conus) venoms are a valuable source of pharmacologically active compounds; some of the peptide toxin families from the snail venoms are known to interact with potassium channels. We report the purification, synthesis, and characterization of kappaM-conotoxin RIIIJ from the venom of a fish-hunting species, Conus radiatus. This conopeptide, like a previously characterized peptide in the same family, kappaM-RIIIK, inhibits the homotetrameric human Kv1.2 channels. When tested in Xenopus oocytes, kappaM-RIIIJ has an order of magnitude higher affinity (IC(50) = 33 nm) to Kv1.2 than kappaM-RIIIK (IC(50) = 352 nm). Chimeras of RIIIK and RIIIJ tested on the human Kv1.2 channels revealed that Lys-9 from kappaM-RIIIJ is a determinant of its higher potency against hKv1.2. However, when compared in a model of ischemia/reperfusion, kappaM-RIIIK (100 mug/kg of body weight), administered just before reperfusion, significantly reduces the infarct size in rat hearts in vivo without influencing hemodynamics, providing a potential compound for cardioprotective therapeutics. In contrast, kappaM-RIIIJ does not exert any detectable cardioprotective effect. kappaM-RIIIJ shows more potency for Kv1.2-Kv1.5 and Kv1.2-Kv1.6 heterodimers than kappaM-RIIIK, whereas the affinity of kappaM-RIIIK to Kv1.2-Kv1.7 heterodimeric channels is higher (IC(50) = 680 nm) than that of kappaM-RIIIJ (IC(50) = 3.15 mum). Thus, the cardioprotection seems to correlate to antagonism to heteromultimeric channels, involving the Kv1.2 alpha-subunit rather than antagonism to Kv1.2 homotetramers. Furthermore, kappaM-RIIIK and kappaM-RIIIJ provide a valuable set of probes for understanding the underlying mechanism of cardioprotection.
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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.