Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Preferential interaction of omega-conotoxins with inactivated N-type Ca2+ channels.
Stocker JW, Nadasdi L, Aldrich RW, Tsien RW.
???displayArticle.abstract???
The selective block of N-type Ca2+ channels by omega-conotoxins has been a hallmark of these channels, critical in delineating their biological roles and molecular characteristics. Here we report that the omega-conotoxin-channel interaction depends strongly on channel gating. N-type channels (alpha1B, alpha2, and beta1) expressed in Xenopus oocytes were blocked with a variety of omega-conotoxins, including omega-CTx-GVIA, omega-CTx-MVIIA, and SNX-331, a derivative of omega-CTx-MVIIC. Changes in holding potential (HP) markedly altered the severity of toxin block and the kinetics of its onset and removal. Notably, strong hyperpolarization renders omega-conotoxin block completely reversible. These effects could be accounted for by a modulated receptor model, in which toxin dissociation from the inactivated state is approximately 60-fold slower than from the resting state. Because omega-conotoxins act exclusively outside cells, our results suggest that voltage-dependent inactivation of Ca2+ channels must be associated with an externally detectable conformational change.
Aiyar,
Topology of the pore-region of a K+ channel revealed by the NMR-derived structures of scorpion toxins.
1995, Pubmed
Aiyar,
Topology of the pore-region of a K+ channel revealed by the NMR-derived structures of scorpion toxins.
1995,
Pubmed Aosaki,
Characterization of two kinds of high-voltage-activated Ca-channel currents in chick sensory neurons. Differential sensitivity to dihydropyridines and omega-conotoxin GVIA.
1989,
Pubmed Armstrong,
Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axons.
1971,
Pubmed Armstrong,
Inactivation of the potassium conductance and related phenomena caused by quaternary ammonium ion injection in squid axons.
1969,
Pubmed Basus,
Solution structure of omega-conotoxin MVIIA using 2D NMR spectroscopy.
1995,
Pubmed Baukrowitz,
Modulation of K+ current by frequency and external [K+]: a tale of two inactivation mechanisms.
1995,
Pubmed Baukrowitz,
Use-dependent blockers and exit rate of the last ion from the multi-ion pore of a K+ channel.
1996,
Pubmed Bean,
Lidocaine block of cardiac sodium channels.
1983,
Pubmed Bean,
Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state.
1984,
Pubmed Bezprozvanny,
Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967).
1995,
Pubmed
,
Xenbase Bezprozvanny,
Functional impact of syntaxin on gating of N-type and Q-type calcium channels.
1995,
Pubmed
,
Xenbase Boland,
omega-Conotoxin block of N-type calcium channels in frog and rat sympathetic neurons.
1994,
Pubmed Carbone,
Neuronal calcium channels: kinetics, blockade and modulation.
1989,
Pubmed Catterall,
Structure and function of voltage-gated ion channels.
1993,
Pubmed Catterall,
Membrane potential-dependent binding of scorpion toxin to the action potential Na+ ionophore. Studies with a toxin derivative prepared by lactoperoxidase-catalyzed iodination.
1977,
Pubmed Choi,
Tetraethylammonium blockade distinguishes two inactivation mechanisms in voltage-activated K+ channels.
1991,
Pubmed Dunlap,
Exocytotic Ca2+ channels in mammalian central neurons.
1995,
Pubmed Ellinor,
Structural determinants of the blockade of N-type calcium channels by a peptide neurotoxin.
1994,
Pubmed
,
Xenbase Farr-Jones,
Solution structure of omega-conotoxin MVIIC, a high affinity ligand of P-type calcium channels, using 1H NMR spectroscopy and complete relaxation matrix analysis.
1995,
Pubmed Feldman,
Omega Conus geographus toxin: a peptide that blocks calcium channels.
1987,
Pubmed French,
Interactions between a pore-blocking peptide and the voltage sensor of the sodium channel: an electrostatic approach to channel geometry.
1996,
Pubmed Fujita,
Primary structure and functional expression of the omega-conotoxin-sensitive N-type calcium channel from rabbit brain.
1993,
Pubmed Hering,
Transfer of high sensitivity for benzothiazepines from L-type to class A (BI) calcium channels.
1996,
Pubmed
,
Xenbase Hidalgo,
Revealing the architecture of a K+ channel pore through mutant cycles with a peptide inhibitor.
1995,
Pubmed
,
Xenbase Hille,
Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction.
1977,
Pubmed Hirning,
Dominant role of N-type Ca2+ channels in evoked release of norepinephrine from sympathetic neurons.
1988,
Pubmed Hondeghem,
Time- and voltage-dependent interactions of antiarrhythmic drugs with cardiac sodium channels.
1977,
Pubmed Hoshi,
Biophysical and molecular mechanisms of Shaker potassium channel inactivation.
1990,
Pubmed
,
Xenbase Jones,
Calcium currents in bullfrog sympathetic neurons. II. Inactivation.
1989,
Pubmed Kasai,
Presynaptic Ca-antagonist omega-conotoxin irreversibly blocks N-type Ca-channels in chick sensory neurons.
1987,
Pubmed Komuro,
Selective role of N-type calcium channels in neuronal migration.
1992,
Pubmed Larsson,
Transmembrane movement of the shaker K+ channel S4.
1996,
Pubmed
,
Xenbase Lee,
Mechanism of calcium channel blockade by verapamil, D600, diltiazem and nitrendipine in single dialysed heart cells.
1983,
Pubmed Liu,
Dynamic rearrangement of the outer mouth of a K+ channel during gating.
1996,
Pubmed López-Barneo,
Effects of external cations and mutations in the pore region on C-type inactivation of Shaker potassium channels.
1993,
Pubmed
,
Xenbase McCleskey,
Omega-conotoxin: direct and persistent blockade of specific types of calcium channels in neurons but not muscle.
1987,
Pubmed McDonough,
Inhibition of calcium channels in rat central and peripheral neurons by omega-conotoxin MVIIC.
1996,
Pubmed McEnery,
Purified omega-conotoxin GVIA receptor of rat brain resembles a dihydropyridine-sensitive L-type calcium channel.
1991,
Pubmed Mintz,
P-type calcium channels in rat central and peripheral neurons.
1992,
Pubmed Nemoto,
Solution structure of omega-conotoxin MVIIC determined by NMR.
1995,
Pubmed Nowycky,
Three types of neuronal calcium channel with different calcium agonist sensitivity.
,
Pubmed Pallaghy,
Three-dimensional structure in solution of the calcium channel blocker omega-conotoxin.
1993,
Pubmed Pelzer,
Properties and regulation of calcium channels in muscle cells.
1990,
Pubmed Plummer,
Elementary properties and pharmacological sensitivities of calcium channels in mammalian peripheral neurons.
1989,
Pubmed Randall,
Pharmacological dissection of multiple types of Ca2+ channel currents in rat cerebellar granule neurons.
1995,
Pubmed
,
Xenbase Ranganathan,
Spatial localization of the K+ channel selectivity filter by mutant cycle-based structure analysis.
1996,
Pubmed Regan,
Ca2+ channels in rat central and peripheral neurons: high-threshold current resistant to dihydropyridine blockers and omega-conotoxin.
1991,
Pubmed Ruth,
Primary structure of the beta subunit of the DHP-sensitive calcium channel from skeletal muscle.
1989,
Pubmed Sakamoto,
A monoclonal antibody to the beta subunit of the skeletal muscle dihydropyridine receptor immunoprecipitates the brain omega-conotoxin GVIA receptor.
1991,
Pubmed Sather,
Distinctive biophysical and pharmacological properties of class A (BI) calcium channel alpha 1 subunits.
1993,
Pubmed
,
Xenbase Satin,
The saxitoxin/tetrodotoxin binding site on cloned rat brain IIa Na channels is in the transmembrane electric field.
1994,
Pubmed
,
Xenbase Sevilla,
Three-dimensional structure of omega-conotoxin GVIA determined by 1H NMR.
1993,
Pubmed Stampe,
Intimations of K+ channel structure from a complete functional map of the molecular surface of charybdotoxin.
1994,
Pubmed Stanley,
Characterization of a calcium current in a vertebrate cholinergic presynaptic nerve terminal.
1991,
Pubmed Stühmer,
Structural parts involved in activation and inactivation of the sodium channel.
1989,
Pubmed
,
Xenbase Vassilev,
Identification of an intracellular peptide segment involved in sodium channel inactivation.
1988,
Pubmed Wheeler,
Roles of N-type and Q-type Ca2+ channels in supporting hippocampal synaptic transmission.
1994,
Pubmed Williams,
Structure and functional expression of an omega-conotoxin-sensitive human N-type calcium channel.
1992,
Pubmed Yang,
Evidence for voltage-dependent S4 movement in sodium channels.
1995,
Pubmed Yellen,
An engineered cysteine in the external mouth of a K+ channel allows inactivation to be modulated by metal binding.
1994,
Pubmed Zagotta,
Restoration of inactivation in mutants of Shaker potassium channels by a peptide derived from ShB.
1990,
Pubmed
,
Xenbase Zhang,
Molecular determinants of voltage-dependent inactivation in calcium channels.
1994,
Pubmed
,
Xenbase
