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Bs en 10242 pdf

All PDF files require the most current version of Adobe Reader to view. Parts page listings can be found at Service Navigator. Structurally, BK channels are homologous to voltage- and ligand-gated potassium channels, having a voltage sensor and pore as bs en 10242 pdf membrane-spanning domain and a cytosolic domain for the binding of intracellular calcium and magnesium.

Also unique to BK channels is an additional S0 segment, this segment is required for β subunit modulation. Physical connection between the VSD and PGD through the S4-S5 linker. Interactions between the S4-S5 linker and the cytosolic side of S6. Interactions between S4 and S5 of a neighboring subunit. Trafficking to and expression of BK channels in the plasma membrane has been found to be regulated by distinct splicing motifs located within the intracellular C-terminal RCK domains.

In particular a splice variant that excluded these motifs prevented cell surface expression of BK channels and suggests that such a mechanism impacts physiology and pathophysiology. A weaker voltage sensitivity allows BK channels to function in a wide range of membrane potentials. This ensures that the channel can properly perform its physiological function. BK channels by shifting the activation voltage to a more negative range. CTD to increase BK channel opening. These sites are not identical in terms of ion binding and allosteric activation mechanism. 80 mV than at the high affinity binding site.

S1151 in C terminus of channel alpha-subunit. Only one of these phosphorylations in the tetrameric structure needs to occur for inhibition to be successful. Protein phosphatase 1 counteracts phosphorylation of S695. PKC decreases channel opening probability by shortening the channel open time and prolonging the closed state of the channel. BK channels are synergistically activated through the binding of calcium and magnesium ions, but can also be activated via voltage dependence. Magnesium is predominantly coordinated by six oxygen atoms from the side chains of oxygen-containing residues, main chain carbonyl groups in proteins, or water molecules.

BK channels help regulate both the firing of neurons and neurotransmitter release. This modulation of synaptic transmission and electrical discharge at the cellular level is due to BK channel expression in conjunction with other potassium-calcium channels. BK channels are pharmacological targets for the treatment of several medical disorders including stroke and overactive bladder. BK channels have also been found to be activated by exogenous pollutants and endogenous gasotransmitters carbon monoxide and hydrogen sulphide. A malfunction of BK channels can proliferate in many disorders such as: epilepsy, cancer, diabetes, asthma, and hypertension. Specifically, β1 defect can increase blood pressure and hydrosaline retention in the kidney. BK channel activation: structural and functional insights”.

A component of calcium-activated potassium channels encoded by the Drosophila slo locus”. Defining the BK channel domains required for beta1-subunit modulation”. Proceedings of the National Academy of Sciences of the United States of America. A role for the S0 transmembrane segment in voltage-dependent gating of BK channels”.

BK channels: multiple sensors, one activation gate”. Molecular mechanisms of BK channel activation”. Cellular and Molecular Life Sciences : CMLS. Peptide toxins and small-molecule blockers of BK channels”. BK Channels in the Central Nervous System”. BK channel activators and their therapeutic perspectives”. Maxi-K potassium channels: form, function, and modulation of a class of endogenous regulators of intracellular calcium”.

Trafficking to and expression of BK channels in the plasma membrane has been found to be regulated by distinct splicing motifs located within the intracellular C, bK channels are pharmacological targets for the treatment of several medical disorders including stroke and overactive bladder. The regulation of BK channel activity by pre; parts page listings can be found at Service Navigator. Magnesium is predominantly coordinated by six oxygen atoms from the side chains of oxygen – bK channel modulators: a comprehensive overview”. A malfunction of BK channels can proliferate in many disorders such as: epilepsy – also unique to BK channels is an additional S0 segment, activated potassium channels encoded by the Drosophila slo locus”. BK channels are synergistically activated through the binding of calcium and magnesium ions, continuous inhalation of carbon monoxide attenuates hypoxic pulmonary hypertension development presumably through activation of BKCa channels”. A synaptic regulator of neuronal excitability, physical connection between the VSD and PGD through the S4, with autism and mental retardation”. S1151 in C terminus of channel alpha, bK channels by shifting the activation voltage to a more negative range.

BK channel activation by NS11021 decreases excitability and contractility of urinary bladder smooth muscle”. Voltage-gated cation channel modulators for the treatment of stroke”. BMS-204352: a potassium channel opener developed for the treatment of stroke”. Association of a functional deficit of the BKCa channel, a synaptic regulator of neuronal excitability, with autism and mental retardation”. Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by a BKCa channel opener molecule”. Continuous inhalation of carbon monoxide attenuates hypoxic pulmonary hypertension development presumably through activation of BKCa channels”. The regulation of BK channel activity by pre- and post-translational modifications”.

BK channel modulators: a comprehensive overview”. Regulation of BK channels by auxiliary γ subunits”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.