Results 41 to 50 of about 2,282 (189)
PIP2-dependent coupling of voltage sensor and pore domains in Kv7.2 channel
Communications Biology, 2021 Pant et al. describe the mechanism by which PIP2 might regulate homomeric Kv7.2 channels. They identify sites important in the binding of the PIP2 lipid to Kv7.2 channels and propose that the PIP2 binding to a specific site results in the coupling ...
Shashank Pant +5 more
doaj +1 more source
An Anthrone-Based Kv7.2/7.3 Channel Blocker with Improved Properties for the Investigation of Psychiatric and Neurodegenerative Disorders [PDF]
, 2019 A set of novel Kv7.2/7.3 (KCNQ2/3) channel blockers was synthesized to address several liabilities of the known compounds XE991 (metabolic instability and CYP inhibition) and the clinical compound DMP 543 (acid instability, insolubility, and ...
C. David, Weaver +7 more
core +4 more sources
Neurobiology of Disease, 2018 Neuronal Kv7/KCNQ channels are voltage-gated potassium channels composed of Kv7.2/KCNQ2 and Kv7.3/KCNQ3 subunits. Enriched at the axonal membrane, they potently suppress neuronal excitability. De novo and inherited dominant mutations in Kv7.2 cause early
Eung Chang Kim +9 more
doaj +1 more source
Molecular Insights Into Binding and Activation of the Human KCNQ2 Channel by Retigabine
Frontiers in Molecular Biosciences, 2022 Voltage-gated potassium channels of the Kv7.x family are involved in a plethora of biological processes across many tissues in animals, and their misfunctioning could lead to several pathologies ranging from diseases caused by neuronal hyperexcitability,
Barbara Garofalo +5 more
doaj +1 more source
Kv7 channels can function without constitutive calmodulin tethering.
PLoS ONE, 2011 M-channels are voltage-gated potassium channels composed of Kv7.2-7.5 subunits that serve as important regulators of neuronal excitability. Calmodulin binding is required for Kv7 channel function and mutations in Kv7.2 that disrupt calmodulin binding ...
Juan Camilo Gómez-Posada +11 more
doaj +1 more source
The acrylamide (S)-2 as a positive and negative modulator of Kv7 channels expressed in Xenopus laevis oocytes. [PDF]
PLoS ONE, 2009 BACKGROUND: Activation of voltage-gated potassium channels of the Kv7 (KCNQ) family reduces cellular excitability. These channels are therefore attractive targets for treatment of diseases characterized by hyperexcitability, such as epilepsy, migraine ...
Sigrid Marie Blom +2 more
doaj +1 more source
EBioMedicine, 2022 Summary: Background: Prior studies have revealed remarkable phenotypic heterogeneity in KCNQ2-related disorders, correlated with effects on biophysical features of heterologously expressed channels. Here, we assessed phenotypes and functional properties
Francesco Miceli +33 more
doaj +1 more source
Calcium-Independent Potentation of Kv7.2 Current Density by Calmodulin [PDF]
Biophysical Journal, 2014 Calmodulin (CaM) confers calcium-dependent regulation to a large array of intracellular proteins, although calcium independent functions have also been described. In KCNQ/Kv7 channels, the molecular determinants of the M-current, a slow voltage-dependent non-inactivating neuronal potassium-selective current, CaM binding is essential for channel ...
Gomis-Perez, Carolina +8 more
openaire +1 more source
Epilepsy-causing mutations in Kv7.2 C-terminus affect binding and functional modulation by calmodulin [PDF]
, 2015 Mutations in the KCNQ2 gene, encoding for voltage-gated Kv7.2K(+) channel subunits, are responsible for early-onset epileptic diseases with widely-diverging phenotypic presentation, ranging from Benign Familial Neonatal Seizures (BFNS) to epileptic ...
Scambia, Giovanni +24 more
core +1 more source
Cannabidiol activates neuronal Kv7 channels
eLife, 2022 Cannabidiol (CBD), a chemical found in the Cannabis sativa plant, is a clinically effective antiepileptic drug whose mechanism of action is unknown. Using a fluorescence-based thallium flux assay, we performed a large-scale screen and found enhancement ...
Han-Xiong Bear Zhang +12 more
doaj +1 more source