Journal ArticleDOI
Cyclic Nucleotide-Gated Ion Channels
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TLDR
A picture is beginning to emerge for how the binding of cyclic nucleotide is transduced into the opening of the pore and how this allosteric transition is modulated by various physiological effectors.Abstract:
▪ Abstract Cyclic nucleotide-gated (CNG) ion channels were first discovered in rod photoreceptors, where they are responsible for the primary electrical signal of the photoreceptor in response to light. CNG channels are highly specialized membrane proteins that open an ion-permeable pore across the membrane in response to the direct binding of intracellular cyclic nucleotides. CNG channels have been identified in a number of other tissues, including the brain, where their roles are only beginning to be appreciated. Recently, significant progress has been made in understanding the molecular mechanisms underlying their functional specializations. From these studies, a picture is beginning to emerge for how the binding of cyclic nucleotide is transduced into the opening of the pore and how this allosteric transition is modulated by various physiological effectors.read more
Citations
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Cyclic nucleotide phosphodiesterase (PDE) superfamily: a new target for the development of specific therapeutic agents.
TL;DR: By inhibiting specifically the up-regulated PDE isozyme(s) with newly synthesized potent and isozyme-selective PDE inhibitors, it may be potentially possible to restore normal intracellular signaling selectively, providing therapy with reduced adverse effects.
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CNG AND HCN CHANNELS: Two Peas, One Pod
TL;DR: How similarities in structure and activation mechanisms result in common biophysical models, allowing CNG and HCN channels to be viewed as a single genre, is focused on.
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From molecule to malady
TL;DR: An explosion in the number of crystal structures of ion channels has led to a marked increase in understanding of how ion channels open and close, and select between permeant ions.
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Cyclic nucleotide phosphodiesterase (PDE) isozymes as targets of the intracellular signalling network: benefits of PDE inhibitors in various diseases and perspectives for future therapeutic developments
Thérèse Keravis,Claire Lugnier +1 more
TL;DR: The investigation of PDE isozyme alterations related to various pathologies and the design of specific PDE inhibitors might lead to the development of new specific therapeutic strategies in numerous pathologies.
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Signaling by G-protein-coupled receptor (GPCR): Studies on the GnRH receptor
TL;DR: Understanding these molecular mechanisms triggered by the GnRHR through biochemical and 'Systems Biology' approaches would provide the basis for the construction of the dynamic connectivity maps, which operate in the various cell types (endocrine, cancer, and immune system) targeted by GnRH.
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The Structure of the Potassium Channel: Molecular Basis of K+ Conduction and Selectivity
Declan A. Doyle,João H.Morais Cabral,Richard A. Pfuetzner,Anling Kuo,Jacqueline M. Gulbis,Steven L. Cohen,Brian T. Chait,Roderick MacKinnon +7 more
TL;DR: The architecture of the pore establishes the physical principles underlying selective K+ conduction, which promotes ion conduction by exploiting electrostatic repulsive forces to overcome attractive forces between K+ ions and the selectivity filter.
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Crystal structure and mechanism of a calcium-gated potassium channel
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HERG, a Human Inward Rectifier in the Voltage-Gated Potassium Channel Family
TL;DR: The properties of HERG channels are consistent with the gating properties of Eag-related and other outwardly rectifying, S4-containing potassium channels, but with the addition of an inactivation mechanism that attenuates potassium efflux during depolarization.