Molecular simulation of the Kv7.4[ΔS269] mutant channel reveals that ion conduction in the cavity is perturbed due to hydrophobic gating
Sign Up to like & getrecommendations! Published in 2021 at "Biochemistry and Biophysics Reports"
DOI: 10.1016/j.bbrep.2020.100879
Abstract: Mutations in the voltage-gated potassium channel Kv7.4 (encoded as KCNQ4) lead to the early onset of non-syndromic hearing loss, which is significant during language acquisition. The deletion of the S269 pore residue (genetic Δ mutation)… read more here.
Keywords: ion conduction; s269; cavity; kv7 ... See more keywords
Pi(4,5)P2 Modulates Hysteresis and Pharmacology of KV7 Channels
Sign Up to like & getrecommendations! Published in 2017 at "Biophysical Journal"
DOI: 10.1016/j.bpj.2016.11.624
Abstract: KV7 channels are critical components of the plasma membrane in many excitable cells. The main function of KV7 channels is to contribute to the maintenance of the resting potential, thus regulating cellular electrical excitability. In… read more here.
Keywords: kv7 kv7; kv7; pharmacology; hysteretic behavior ... See more keywords
Lead Optimization of Positive Allosteric KV7.2/3 Channel Modulators toward Improved Balance of Lipophilicity and Aqueous Solubility.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c03112
Abstract: The voltage-gated potassium channel KV7.2/3 is gaining attention for its association with several medical indications. While recently reported, potent compounds aimed to fill the therapeutic gap left by market-withdrawn activators, key physicochemical parameters did not… read more here.
Keywords: lead optimization; aqueous solubility; channel; lipophilicity ... See more keywords
Discovery of a potent, Kv7.3-selective potassium channel opener from a Polynesian traditional botanical anticonvulsant
Sign Up to like & getrecommendations! Published in 2024 at "Communications Chemistry"
DOI: 10.1038/s42004-024-01318-9
Abstract: Plants remain an important source of biologically active small molecules with high therapeutic potential. The voltage-gated potassium (Kv) channel formed by Kv7.2/3 (KCNQ2/3) heteromers is a major target for anticonvulsant drug development. Here, we screened… read more here.
Keywords: channel opener; potassium channel; medicine; channel ... See more keywords
Ca2+-Calmodulin and PIP2 interactions at the proximal C-terminus of Kv7 channels
Sign Up to like & getrecommendations! Published in 2017 at "Channels"
DOI: 10.1080/19336950.2017.1388478
Abstract: ABSTRACT In the heart, co-assembly of Kv7.1 with KCNE1 produces the slow IKS potassium current, which repolarizes the cardiac action potential and mutations in human Kv7.1 and KCNE1 genes cause cardiac arrhythmias. The proximal Kv7.1… read more here.
Keywords: ca2 calmodulin; cam; terminus; pip2 ... See more keywords
Recombinant Production, Reconstruction in Lipid–Protein Nanodiscs, and Electron Microscopy of Full-Length α-Subunit of Human Potassium Channel Kv7.1
Sign Up to like & getrecommendations! Published in 2018 at "Biochemistry (Moscow)"
DOI: 10.1134/s0006297918050097
Abstract: Voltage-gated potassium channel Kv7.1 plays an important role in the excitability of cardiac muscle. The α-subunit of Kv7.1 (KCNQ1) is the main structural element of this channel. Tetramerization of KCNQ1 in the membrane results in… read more here.
Keywords: protein; microscopy; potassium channel; kv7 ... See more keywords
Kv7 channel activation reduces brain endothelial cell permeability and prevents kainic acid-induced blood-brain barrier damage
Sign Up to like & getrecommendations! Published in 2024 at "American Journal of Physiology - Cell Physiology"
DOI: 10.1152/ajpcell.00709.2023
Abstract: Ion channels in the blood brain barrier (BBB) play a main role in controlling interstitial fluid composition and cerebral blood flow, and their dysfunction contributes to the disruption of the BBB occurring in many neurological… read more here.
Keywords: brain; physiology; barrier; cell ... See more keywords
Genetic inhibition of KV7/M-channels increases the excitability of bronchopulmonary vagal nociceptive nerves
Sign Up to like & getrecommendations! Published in 2023 at "Physiology"
DOI: 10.1152/physiol.2023.38.s1.5732751
Abstract: The KV7/M-channel, encoded by Kcnq2-5 genes, generates a “braking” potassium current (IM) and contributes to the regulation of neuronal excitability. We have previously reported that the vagal sensory nerves terminated in the mouse lungs expressed… read more here.
Keywords: kv7; nodose neurons; kcnq2; physiology ... See more keywords
Kv7 channel isoforms contribute to H2O2-mediated vasodilation in the ischemic heart after exercise training
Sign Up to like & getrecommendations! Published in 2023 at "Physiology"
DOI: 10.1152/physiol.2023.38.s1.5733976
Abstract: Ischemic heart disease is a multifaceted pathological manifestation that continues to impose a significant burden on individuals and the healthcare system. As a potential therapeutic modality, exercise training has been reported to induce vascular adaptations… read more here.
Keywords: kv7; exercise training; vasodilation; physiology ... See more keywords
Inhibition of Kv7/M Channel Currents by Fangchinoline
Sign Up to like & getrecommendations! Published in 2022 at "Pharmacology"
DOI: 10.1159/000527464
Abstract: Introduction: Voltage-gated Kv7/M potassium channels play an essential role in the control of membrane potential and neuronal excitability. Fangchinoline, a bisbenzylisoquinoline alkaloid, displays extensive biological activities including antitumor, anti-inflammatory, and antihypertension effects. In this study,… read more here.
Keywords: channel currents; kv7; kv7 channels; kv7 channel ... See more keywords
The expression and function of KCNQ potassium channels in human chorionic plate arteries from women with normal pregnancies and pre-eclampsia
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DOI: 10.1371/journal.pone.0192122
Abstract: Pre-eclampsia is associated with altered maternal and placental vascular reactivity. Kv7 channels (encoded by KCNQ 1–5 genes) are a potential contributor to the regulation of vascular tone in CPAs (chorionic plate arteries) during normal pregnancy.… read more here.
Keywords: pre eclampsia; chorionic plate; kv7; expression ... See more keywords