William A. Catterall

IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels (2009)

Harmar, Anthony J., Hills, Rebecca A., Rosser, Edward M., Jones, Martin, Buneman, O. Peter, Dunbar, Donald R., ...

The IUPHAR database (IUPHAR-DB) integrates peer-reviewed pharmacological, chemical, genetic, functional and anatomical information on the 354 nonsensory G protein-coupled receptors (GPCRs), 71...

The voltage-gated sodium channel Scn8a is a genetic modifier of severe myoclonic epilepsy of infancy (2007)

Martin, Melinda S., Tang, Bin, Papale, Ligia A., Yu, Frank H., Catterall, William A., Escayg, Andrew

The mammalian genome contains four voltage-gated sodium channel genes that are primarily expressed in the central nervous system: SCN1A, SCN2A, SCN3A and SCN8A. Mutations in SCN1A and SCN2A are...

Molecular Basis of Paralytic Neurotoxin Action on Voltage-Sensitive Sodium Channels (2005)

Catterall, William A.

In years 1-4 of this project, progress was made on several objectives: A. The sites and mechanisms of action on the sodium channel were examined and further defined for three new classes of...

Overview of the voltage-gated sodium channel family (2003)

Yu, Frank H, Catterall, William A

Abstract Selective permeation of sodium ions through voltage-dependent sodium channels is fundamental to the generation of action potentials in excitable cells such as neurons. These channels are...

Molecular Basis of Paraltyic Neurotoxin Action on Voltage-Sensitive Sodium Channels (2003)

Catterall, William A.

In year 1 of this project, progress was made on several objectives: A) The sites and mechanisms of action on the sodium channel were examined and further defined for three new classes of neurotoxins:...

Molecular Basis of Paralytic Neurotoxin Action on Voltage-Sensitive Sodium Channels (2003)

Catterall, William A.

In years 1 and 2 of this project, progress was made on several objectives: The sites and mechanisms of action on the sodium channel were examined and further defined for three new classes of...

Molecular Basis of Paralytic Neurotoxin Action on Voltage-Sensitive Sodium Channels (2003)

Catterall, William A.

In the third year of this project, we have continued to analyze the effects of newly described neurotoxins on voltage-sensitive sodium channels in mammalian neurons, prepared site-directed antisera...

Review Overview of the voltage-gated sodium channel family (2003)

Frank H Yu, William A Catterall

electronic version of this article is the complete one and can be

Molecular Basis of Paralytic Neurotoxin Action on Voltage-Sensitive Sodium Channels. (1998)

Catterall, William A.

In years 1 - 5 of this project, progress was made on several objectives: A. The sites and mechanisms of action on the sodium channel were examined and further defined for three new classes of...

Ralitoline (CI-946) and CI-953 block sustained repetitive sodium action potentials in cultured mouse spinal cord neurons and displace batrachotoxinin A 20-[alpha]-benzoate binding in vitro (1991)

Rock, David M., McLean, Michael J., Macdonald, Robert L., Catterall, William A., Taylor, Charles P.

Ralitoline and CI-953 are anticonvulsant compounds active in both maximal electroshock and kindling models of seizures with rodents. CI-953 (IC50 = 5 [mu]M) and ralitoline (IC50 = 2 [mu]M) both...

Tissue-specific expression of the RI and RII sodium channel subtypes (1987)

Gordon, Dalia, Merrick, Dawn, Auld, Vanessa, Dunn, Robert, Goldin, Alan L., Davidson, Norman, ...

Anti-peptide antibodies that distinguish between the rat brain sodium channel subtypes referred to as RI and RII were prepared and used to determine their relative expression in nerve and muscle...

Messenger RNA coding for only the alpha subunit of the rat brain Na channel is sufficient for expression of functional channels in Xenopus oocytes (1986)

Goldin, Alan L., Snutch, Terry P., Lübbert, Hermann, Dowsett, Andrew, Marshall, John, Auld, Vanessa, ...

Several cDNA clones coding for the high molecular weight (alpha) subunit of the voltage-sensitive Na channel have been selected by immunoscreening a rat brain cDNA library constructed in the...

Inhibition of cardiac L-type calcium channels by protein kinase C phosphorylation of two sites in the N-terminal domain

McHugh, Damian, Sharp, Elizabeth M., Scheuer, Todd, Catterall, William A.

We have investigated the mechanism underlying the modulation of the cardiac L-type Ca2+ current by protein kinase C (PKC). Using the patch-clamp technique, we found that PKC activation by...

Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CL

Carter, Adrian J., Grauert, Matthias, Pschorn, Uwe, Bechtel, Wolf Dietrich, Bartmann-Lindholm, Christina, Qu, Yusheng, ...

We have synthesized a new benzomorphan derivative, 2R-[2α,3(S*),6α]-1,2,3,4,5,6-hexahydro-6,11,11-trimethyl-3-[2-(phenylmethoxy)propyl]-2,6-methano-3-benzazocin-10-ol hydrochloride (BIII 890 CL),...

Type II regulatory subunits are not required for the anchoring-dependent modulation of Ca2+ channel activity by cAMP-dependent protein kinase

Burton, Kimberly A., Johnson, Barry D., Hausken, Zachary E., Westenbroek, Ruth E., Idzerda, Rejean L., Scheuer, Todd, ...

Preferential phosphorylation of specific proteins by cAMP-dependent protein kinase (PKA) may be mediated in part by the anchoring of PKA to a family of A-kinase anchor proteins (AKAPs) positioned in...

Evidence for a voltage-dependent enhancement of neurotransmitter release mediated via the synaptic protein interaction site of N-type Ca2+ channels

Mochida, Sumiko, Yokoyama, Charles T., Kim, D. Kyle, Itoh, Kanako, Catterall, William A.

Secretion of neurotransmitters is initiated by voltage-gated calcium influx through presynaptic, voltage-gated N-type calcium channels. These channels interact with the SNARE proteins, which are core...

Interaction of the synprint site of N-type Ca2+ channels with the C2B domain of synaptotagmin I

Sheng, Zu-Hang, Yokoyama, Charles T., Catterall, William A.

N-type Ca2+ channels mediate Ca2+ influx, which initiates fast exocytosis of neurotransmitters at synapses, and they interact directly with the SNARE proteins syntaxin and SNAP-25...

Interaction of batrachotoxin with the local anesthetic receptor site in transmembrane segment IVS6 of the voltage-gated sodium channel

Linford, Nancy J., Cantrell, Angela R., Qu, Yusheng, Scheuer, Todd, Catterall, William A.

The voltage-gated sodium channel is the site of action of more than six classes of neurotoxins and drugs that alter its function by interaction with distinct, allosterically coupled receptor sites....

Ca2+-dependent and -independent interactions of the isoforms of the α1A subunit of brain Ca2+ channels with presynaptic SNARE proteins

Kim, D. Kyle, Catterall, William A.

Fast neurotransmission requires that docked synaptic vesicles be located near the presynaptic N-type or P/Q-type calcium channels. Specific protein–protein interactions between a synaptic protein...

Construction of a high-affinity receptor site for dihydropyridine agonists and antagonists by single amino acid substitutions in a non-l-type Ca2+ channel

Hockerman, Gregory H., Peterson, Blaise Z., Sharp, Elizabeth, Tanada, Timothy N., Scheuer, Todd, Catterall, William A.

The activity of l-type Ca2+ channels is increased by dihydropyridine (DHP) agonists and inhibited by DHP antagonists, which are widely used in the therapy of cardiovascular disease. These drugs bind...

Interaction of voltage-gated sodium channels with the extracellular matrix molecules tenascin-C and tenascin-R

Srinivasan, Jayashree, Schachner, Melitta, Catterall, William A.

The type IIA rat brain sodium channel is composed of three subunits: a large pore-forming α subunit and two smaller auxiliary subunits, β1 and β2. The β subunits are single membrane-spanning...

Allosteric modulation of Ca2+ channels by G proteins, voltage-dependent facilitation, protein kinase C, and Cavβ subunits

Herlitze, Stefan, Zhong, Huijun, Scheuer, Todd, Catterall, William A.

N-type and P/Q-type Ca2+ channels are inhibited by neurotransmitters acting through G protein-coupled receptors in a membrane-delimited pathway involving Gβγ subunits. Inhibition is caused by a...

Control of gating mode by a single amino acid residue in transmembrane segment IS3 of the N-type Ca2+ channel

Zhong, Huijun, Li, Bin, Scheuer, Todd, Catterall, William A.

N-type Ca2+ channels can be inhibited by neurotransmitter-induced release of G protein βγ subunits. Two isoforms of Cav2.2 α1 subunits of N-type calcium channels from rat brain (Cav2.2a and...

Role of the C-terminal domain in inactivation of brain and cardiac sodium channels

Mantegazza, Massimo, Yu, Frank H., Catterall, William A., Scheuer, Todd

Inactivation is a fundamental characteristic of Na+ channels, and small changes cause skeletal muscle paralysis and myotonia, epilepsy, and cardiac arrhythmia. Brain Nav1.2a channels have faster...

An unexpected role for brain-type sodium channels in coupling of cell surface depolarization to contraction in the heart

Maier, Sebastian K. G., Westenbroek, Ruth E., Schenkman, Kenneth A., Feigl, Eric O., Scheuer, Todd, Catterall, William A.

Voltage-gated sodium channels composed of pore-forming α and auxiliary β subunits are responsible for the rising phase of the action potential in cardiac muscle, but the functional roles of...

Reduced sodium channel density, altered voltage dependence of inactivation, and increased susceptibility to seizures in mice lacking sodium channel β2-subunits

Chen, Chunling, Bharucha, Vandana, Chen, Yuan, Westenbroek, Ruth E., Brown, Angus, Malhotra, Jyoti Dhar, ...

Sodium channel β-subunits modulate channel gating, assembly, and cell surface expression in heterologous cell systems. We generated β2−/− mice to investigate the role of β2 in control of...

Subtype-selective reconstitution of synaptic transmission in sympathetic ganglion neurons by expression of exogenous calcium channels

Mochida, Sumiko, Westenbroek, Ruth E., Yokoyama, Charles T., Itoh, Kanako, Catterall, William A.

Fast cholinergic neurotransmission between superior cervical ganglion neurons (SCGNs) in cell culture is initiated by N-type Ca2+ currents through Cav2.2 channels. To test the ability of different...

Requirement for the synaptic protein interaction site for reconstitution of synaptic transmission by P/Q-type calcium channels

Mochida, Sumiko, Westenbroek, Ruth E., Yokoyama, Charles T., Zhong, Huijun, Myers, Scott J., Scheuer, Todd, ...

Cav2.1 channels, which conduct P/Q-type Ca2+ currents, were expressed in superior cervical ganglion neurons in cell culture, and neurotransmission initiated by these exogenously expressed Ca2+...

An unexpected requirement for brain-type sodium channels for control of heart rate in the mouse sinoatrial node

Maier, Sebastian K. G., Westenbroek, Ruth E., Yamanushi, T. T., Dobrzynski, H., Boyett, Mark R., Catterall, William A., ...

Voltage-gated Na+ channels are composed of pore-forming α and auxiliary β subunits. The majority of Na+ channels in the heart contain tetrodotoxin (TTX)-insensitive Nav1.5 α subunits, but...

Overview of the voltage-gated sodium channel family

Yu, Frank H, Catterall, William A

Different sodium channels have remarkably similar functional properties, but small changes in sodium-channel function are biologically relevant, as underscored by mutations that cause several human...

β-Adrenergic regulation requires direct anchoring of PKA to cardiac CaV1.2 channels via a leucine zipper interaction with A kinase-anchoring protein 15

Hulme, Joanne T., Lin, Teddy W.-C., Westenbroek, Ruth E., Scheuer, Todd, Catterall, William A.

Activation of β-adrenergic receptors and consequent phosphorylation by cAMP-dependent protein kinase A (PKA) greatly increases the L-type Ca2+ current through CaV1.2 channels in isolated cardiac...

Molecular determinants of Ca2+/calmodulin-dependent regulation of Cav2.1 channels

Lee, Amy, Zhou, Hong, Scheuer, Todd, Catterall, William A.

Ca2+-dependent facilitation and inactivation (CDF and CDI) of Cav2.1 channels modulate presynaptic P/Q-type Ca2+ currents and contribute to activity-dependent synaptic plasticity. This dual feedback...

Deficiency of Uncoupler-Stimulated Adenosine Triphosphatase Activity in Tightly Coupled Hepatoma Mitochondria

Pedersen, Peter L., Eska, Terry, Morris, Harold P., Catterall, William A.

Tightly coupled mitochondria from the well-differentiated hepatoma 7800 failed to exhibit a significant 2,4-dinitrophenol-activated ATPase activity at concentrations of uncoupler sufficient to...

Sodium Uptake Associated with Activation of Action Potential Ionophores of Cultured Neuroblastoma and Muscle Cells

Catterall, William A., Nirenberg, Marshall

Veratridine, an activator of action potential Na+ ionophores, stimulated passive Na+ uptake by electrically excitable neuroblastoma and muscle cells but had no effect on clonal cell lines defective...

Reversed voltage-dependent gating of a bacterial sodium channel with proline substitutions in the S6 transmembrane segment

Zhao, Yong, Scheuer, Todd, Catterall, William A.

Members of the voltage-gated-like ion channel superfamily have a conserved pore structure. Transmembrane helices that line the pore (M2 or S6) are thought to gate it at the cytoplasmic end by bending...

Convergent regulation of skeletal muscle Ca2+ channels by dystrophin, the actin cytoskeleton, and cAMP-dependent protein kinase

Johnson, Barry D., Scheuer, Todd, Catterall, William A.

The skeletal muscle L-type Ca2+ channel (CaV1.1), which is responsible for initiating muscle contraction, is regulated by phosphorylation by cAMP-dependent protein kinase (PKA) in a voltage-dependent...

Sites of proteolytic processing and noncovalent association of the distal C-terminal domain of CaV1.1 channels in skeletal muscle

Hulme, Joanne T., Konoki, Keiichi, Lin, Teddy W.-C., Gritsenko, Marina A., Camp, David G., Bigelow, Diana J., ...

In skeletal muscle cells, voltage-dependent potentiation of Ca2+ channel activity requires phosphorylation by cAMP-dependent protein kinase (PKA) anchored via an A-kinase anchoring protein (AKAP15),...

Differential modulation of Cav2.1 channels by calmodulin and Ca2+-binding protein 1

Lee, Amy, Westenbroek, Ruth E., Haeseleer, Françoise, Palczewski, Krzysztof, Scheuer, Todd, Catterall, William A.

Cav2.1 channels, which mediate P/Q-type Ca2+ currents, undergo Ca2+/calmodulin (CaM)-dependent inactivation and facilitation that can significantly alter synaptic efficacy. Here we report that the...

Voltage sensor conformations in the open and closed states in rosetta structural models of K+ channels

Yarov-Yarovoy, Vladimir, Baker, David, Catterall, William A.

Voltage-gated ion channels control generation and propagation of action potentials in excitable cells. Significant progress has been made in understanding structure and function of the voltage-gated...

Inhibition of cardiac L-type calcium channels by protein kinase C phosphorylation of two sites in the N-terminal domain

McHugh, Damian, Sharp, Elizabeth M., Scheuer, Todd, Catterall, William A.

We have investigated the mechanism underlying the modulation of the cardiac L-type Ca2+ current by protein kinase C (PKC). Using the patch-clamp technique, we found that PKC activation by...

Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CL

Carter, Adrian J., Grauert, Matthias, Pschorn, Uwe, Bechtel, Wolf Dietrich, Bartmann-Lindholm, Christina, Qu, Yusheng, ...

We have synthesized a new benzomorphan derivative, 2R-[2α,3(S*),6α]-1,2,3,4,5,6-hexahydro-6,11,11-trimethyl-3-[2-(phenylmethoxy)propyl]-2,6-methano-3-benzazocin-10-ol hydrochloride (BIII 890 CL),...

Type II regulatory subunits are not required for the anchoring-dependent modulation of Ca2+ channel activity by cAMP-dependent protein kinase

Burton, Kimberly A., Johnson, Barry D., Hausken, Zachary E., Westenbroek, Ruth E., Idzerda, Rejean L., Scheuer, Todd, ...

Preferential phosphorylation of specific proteins by cAMP-dependent protein kinase (PKA) may be mediated in part by the anchoring of PKA to a family of A-kinase anchor proteins (AKAPs) positioned in...

Evidence for a voltage-dependent enhancement of neurotransmitter release mediated via the synaptic protein interaction site of N-type Ca2+ channels

Mochida, Sumiko, Yokoyama, Charles T., Kim, D. Kyle, Itoh, Kanako, Catterall, William A.

Secretion of neurotransmitters is initiated by voltage-gated calcium influx through presynaptic, voltage-gated N-type calcium channels. These channels interact with the SNARE proteins, which are core...

Interaction of the synprint site of N-type Ca2+ channels with the C2B domain of synaptotagmin I

Sheng, Zu-Hang, Yokoyama, Charles T., Catterall, William A.

N-type Ca2+ channels mediate Ca2+ influx, which initiates fast exocytosis of neurotransmitters at synapses, and they interact directly with the SNARE proteins syntaxin and SNAP-25...

Interaction of batrachotoxin with the local anesthetic receptor site in transmembrane segment IVS6 of the voltage-gated sodium channel

Linford, Nancy J., Cantrell, Angela R., Qu, Yusheng, Scheuer, Todd, Catterall, William A.

The voltage-gated sodium channel is the site of action of more than six classes of neurotoxins and drugs that alter its function by interaction with distinct, allosterically coupled receptor sites....

Ca2+-dependent and -independent interactions of the isoforms of the α1A subunit of brain Ca2+ channels with presynaptic SNARE proteins

Kim, D. Kyle, Catterall, William A.

Fast neurotransmission requires that docked synaptic vesicles be located near the presynaptic N-type or P/Q-type calcium channels. Specific protein–protein interactions between a synaptic protein...

Construction of a high-affinity receptor site for dihydropyridine agonists and antagonists by single amino acid substitutions in a non-l-type Ca2+ channel

Hockerman, Gregory H., Peterson, Blaise Z., Sharp, Elizabeth, Tanada, Timothy N., Scheuer, Todd, Catterall, William A.

The activity of l-type Ca2+ channels is increased by dihydropyridine (DHP) agonists and inhibited by DHP antagonists, which are widely used in the therapy of cardiovascular disease. These drugs bind...

Interaction of voltage-gated sodium channels with the extracellular matrix molecules tenascin-C and tenascin-R

Srinivasan, Jayashree, Schachner, Melitta, Catterall, William A.

The type IIA rat brain sodium channel is composed of three subunits: a large pore-forming α subunit and two smaller auxiliary subunits, β1 and β2. The β subunits are single membrane-spanning...

Allosteric modulation of Ca2+ channels by G proteins, voltage-dependent facilitation, protein kinase C, and Cavβ subunits

Herlitze, Stefan, Zhong, Huijun, Scheuer, Todd, Catterall, William A.

N-type and P/Q-type Ca2+ channels are inhibited by neurotransmitters acting through G protein-coupled receptors in a membrane-delimited pathway involving Gβγ subunits. Inhibition is caused by a...

Control of gating mode by a single amino acid residue in transmembrane segment IS3 of the N-type Ca2+ channel

Zhong, Huijun, Li, Bin, Scheuer, Todd, Catterall, William A.

N-type Ca2+ channels can be inhibited by neurotransmitter-induced release of G protein βγ subunits. Two isoforms of Cav2.2 α1 subunits of N-type calcium channels from rat brain (Cav2.2a and...

Role of the C-terminal domain in inactivation of brain and cardiac sodium channels

Mantegazza, Massimo, Yu, Frank H., Catterall, William A., Scheuer, Todd

Inactivation is a fundamental characteristic of Na+ channels, and small changes cause skeletal muscle paralysis and myotonia, epilepsy, and cardiac arrhythmia. Brain Nav1.2a channels have faster...

An unexpected role for brain-type sodium channels in coupling of cell surface depolarization to contraction in the heart

Maier, Sebastian K. G., Westenbroek, Ruth E., Schenkman, Kenneth A., Feigl, Eric O., Scheuer, Todd, Catterall, William A.

Voltage-gated sodium channels composed of pore-forming α and auxiliary β subunits are responsible for the rising phase of the action potential in cardiac muscle, but the functional roles of...

Reduced sodium channel density, altered voltage dependence of inactivation, and increased susceptibility to seizures in mice lacking sodium channel β2-subunits

Chen, Chunling, Bharucha, Vandana, Chen, Yuan, Westenbroek, Ruth E., Brown, Angus, Malhotra, Jyoti Dhar, ...

Sodium channel β-subunits modulate channel gating, assembly, and cell surface expression in heterologous cell systems. We generated β2−/− mice to investigate the role of β2 in control of...

Subtype-selective reconstitution of synaptic transmission in sympathetic ganglion neurons by expression of exogenous calcium channels

Mochida, Sumiko, Westenbroek, Ruth E., Yokoyama, Charles T., Itoh, Kanako, Catterall, William A.

Fast cholinergic neurotransmission between superior cervical ganglion neurons (SCGNs) in cell culture is initiated by N-type Ca2+ currents through Cav2.2 channels. To test the ability of different...

Requirement for the synaptic protein interaction site for reconstitution of synaptic transmission by P/Q-type calcium channels

Mochida, Sumiko, Westenbroek, Ruth E., Yokoyama, Charles T., Zhong, Huijun, Myers, Scott J., Scheuer, Todd, ...

Cav2.1 channels, which conduct P/Q-type Ca2+ currents, were expressed in superior cervical ganglion neurons in cell culture, and neurotransmission initiated by these exogenously expressed Ca2+...

An unexpected requirement for brain-type sodium channels for control of heart rate in the mouse sinoatrial node

Maier, Sebastian K. G., Westenbroek, Ruth E., Yamanushi, T. T., Dobrzynski, H., Boyett, Mark R., Catterall, William A., ...

Voltage-gated Na+ channels are composed of pore-forming α and auxiliary β subunits. The majority of Na+ channels in the heart contain tetrodotoxin (TTX)-insensitive Nav1.5 α subunits, but...

Overview of the voltage-gated sodium channel family

Yu, Frank H, Catterall, William A

Different sodium channels have remarkably similar functional properties, but small changes in sodium-channel function are biologically relevant, as underscored by mutations that cause several human...

β-Adrenergic regulation requires direct anchoring of PKA to cardiac CaV1.2 channels via a leucine zipper interaction with A kinase-anchoring protein 15

Hulme, Joanne T., Lin, Teddy W.-C., Westenbroek, Ruth E., Scheuer, Todd, Catterall, William A.

Activation of β-adrenergic receptors and consequent phosphorylation by cAMP-dependent protein kinase A (PKA) greatly increases the L-type Ca2+ current through CaV1.2 channels in isolated cardiac...

Molecular determinants of Ca2+/calmodulin-dependent regulation of Cav2.1 channels

Lee, Amy, Zhou, Hong, Scheuer, Todd, Catterall, William A.

Ca2+-dependent facilitation and inactivation (CDF and CDI) of Cav2.1 channels modulate presynaptic P/Q-type Ca2+ currents and contribute to activity-dependent synaptic plasticity. This dual feedback...

Deficiency of Uncoupler-Stimulated Adenosine Triphosphatase Activity in Tightly Coupled Hepatoma Mitochondria

Pedersen, Peter L., Eska, Terry, Morris, Harold P., Catterall, William A.

Tightly coupled mitochondria from the well-differentiated hepatoma 7800 failed to exhibit a significant 2,4-dinitrophenol-activated ATPase activity at concentrations of uncoupler sufficient to...

Sodium Uptake Associated with Activation of Action Potential Ionophores of Cultured Neuroblastoma and Muscle Cells

Catterall, William A., Nirenberg, Marshall

Veratridine, an activator of action potential Na+ ionophores, stimulated passive Na+ uptake by electrically excitable neuroblastoma and muscle cells but had no effect on clonal cell lines defective...

Reversed voltage-dependent gating of a bacterial sodium channel with proline substitutions in the S6 transmembrane segment

Zhao, Yong, Scheuer, Todd, Catterall, William A.

Members of the voltage-gated-like ion channel superfamily have a conserved pore structure. Transmembrane helices that line the pore (M2 or S6) are thought to gate it at the cytoplasmic end by bending...

Convergent regulation of skeletal muscle Ca2+ channels by dystrophin, the actin cytoskeleton, and cAMP-dependent protein kinase

Johnson, Barry D., Scheuer, Todd, Catterall, William A.

The skeletal muscle L-type Ca2+ channel (CaV1.1), which is responsible for initiating muscle contraction, is regulated by phosphorylation by cAMP-dependent protein kinase (PKA) in a voltage-dependent...

Sites of proteolytic processing and noncovalent association of the distal C-terminal domain of CaV1.1 channels in skeletal muscle

Hulme, Joanne T., Konoki, Keiichi, Lin, Teddy W.-C., Gritsenko, Marina A., Camp, David G., Bigelow, Diana J., ...

In skeletal muscle cells, voltage-dependent potentiation of Ca2+ channel activity requires phosphorylation by cAMP-dependent protein kinase (PKA) anchored via an A-kinase anchoring protein (AKAP15),...

Voltage sensor conformations in the open and closed states in rosetta structural models of K+ channels

Yarov-Yarovoy, Vladimir, Baker, David, Catterall, William A.

Voltage-gated ion channels control generation and propagation of action potentials in excitable cells. Significant progress has been made in understanding structure and function of the voltage-gated...

Phosphorylation of serine 1928 in the distal C-terminal domain of cardiac CaV1.2 channels during β1-adrenergic regulation

Hulme, Joanne T., Westenbroek, Ruth E., Scheuer, Todd, Catterall, William A.

During the fight-or-flight response, epinephrine and norepinephrine released by the sympathetic nervous system increase L-type calcium currents conducted by CaV1.2a channels in the heart, which...

Dopamine modulation of neuronal Na+ channels requires binding of A kinase-anchoring protein 15and PKA by a modified leucine zipper motif

Few, W. Preston, Scheuer, Todd, Catterall, William A.

In hippocampal pyramidal cells, dopamine acts at D1 receptors to reduce peak Na+ currents by activation of phosphorylation by PKA anchored via an A kinase-anchoring protein (AKAP15). However, the...

Autoinhibitory control of the CaV1.2 channel by its proteolytically processed distal C-terminal domain

Hulme, Joanne T, Yarov-Yarovoy, Vladimir, Lin, Teddy W-C, Scheuer, Todd, Catterall, William A

Voltage-gated Ca2+ channels of the CaV1 family initiate excitation–contraction coupling in cardiac, smooth, and skeletal muscle and are primary targets for regulation by the sympathetic nervous...

Neutralization of Gating Charges in Domain II of the Sodium Channel α Subunit Enhances Voltage-Sensor Trapping by a β-Scorpion Toxin

Cestèle, Sandrine, Scheuer, Todd, Mantegazza, Massimo, Rochat, Hervé, Catterall, William A.

β-Scorpion toxins shift the voltage dependence of activation of sodium channels to more negative membrane potentials, but only after a strong depolarizing prepulse to fully activate the channels....

Kinetic Analysis of Block of Open Sodium Channels by a Peptide Containing the Isoleucine, Phenylalanine, and Methionine (IFM) Motif from the Inactivation Gate

Eaholtz, Galen, Zagotta, William N., Catterall, William A.

We analyzed the kinetics of interaction between the peptide KIFMK, containing the isoleucine, phen-ylalanine, and methionine (IFM) motif from the inactivation gate, and the brain type IIA sodium...

Molecular Analysis of the Putative Inactivation Particle in the Inactivation Gate of Brain Type IIA Na+ Channels

Kellenberger, Stephan, West, James W., Scheuer, Todd, Catterall, William A.

Fast Na+ channel inactivation is thought to involve binding of phenylalanine 1489 in the hydrophobic cluster IFM in LIII-IV of the rat brain type IIA Na+ channel. We have analyzed macroscopic and...

Molecular Analysis of Potential Hinge Residues in the Inactivation Gate of Brain Type IIA Na+ Channels

Kellenberger, Stephan, West, James W., Catterall, William A., Scheuer, Todd

During inactivation of Na+ channels, the intracellular loop connecting domains III and IV is thought to fold into the channel protein and occlude the pore through interaction of the hydrophobic motif...

Block of Brain Sodium Channels by Peptide Mimetics of the Isoleucine, Phenylalanine, and Methionine (IFM) Motif from the Inactivation Gate

Eaholtz, Galen, Colvin, Anita, Leonard, Daniele, Taylor, Charles, Catterall, William A.

Inactivation of sodium channels is thought to be mediated by an inactivation gate formed by the intracellular loop connecting domains III and IV. A hydrophobic motif containing the amino acid...

Increased Expression of the Cardiac L-type Calcium Channel in Estrogen Receptor–deficient Mice

Johnson, Barry D., Zheng, Wei, Korach, Kenneth S., Scheuer, Todd, Catterall, William A., Rubanyi, Gabor M.

Steroid hormones control the expression of many cellular regulators, and a role for estrogen in cardiovascular function and disease has been well documented. To address whether the activity of the...

Sodium channel β1 and β3 subunits associate with neurofascin through their extracellular immunoglobulin-like domain

Ratcliffe, Charlotte F., Westenbroek, Ruth E., Curtis, Rory, Catterall, William A.

Sequence homology predicts that the extracellular domain of the sodium channel β1 subunit forms an immunoglobulin (Ig) fold and functions as a cell adhesion molecule. We show here that β1 subunits...

Modulation of CaV2.1 channels by Ca2+/calmodulin-dependent protein kinase II bound to the C-terminal domain

Jiang, Xin, Lautermilch, Nathan J., Watari, Hirofumi, Westenbroek, Ruth E., Scheuer, Todd, Catterall, William A.

Ca2+/calmodulin-dependent protein kinase II (CaMKII) is a key regulator of synaptic responses in the postsynaptic density, but understanding of its mechanisms of action in the presynaptic neuron is...

Disulfide locking a sodium channel voltage sensor reveals ion pair formation during activation

DeCaen, Paul G., Yarov-Yarovoy, Vladimir, Zhao, Yong, Scheuer, Todd, Catterall, William A.

The S4 transmembrane segments of voltage-gated ion channels move outward on depolarization, initiating a conformational change that opens the pore, but the mechanism of S4 movement is unresolved. One...

IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels

Harmar, Anthony J., Hills, Rebecca A., Rosser, Edward M., Jones, Martin, Buneman, O. Peter, Dunbar, Donald R., ...

The IUPHAR database (IUPHAR-DB) integrates peer-reviewed pharmacological, chemical, genetic, functional and anatomical information on the 354 nonsensory G protein-coupled receptors (GPCRs), 71...

Depolarization-activated gating pore current conducted by mutant sodium channels in potassium-sensitive normokalemic periodic paralysis

Sokolov, Stanislav, Scheuer, Todd, Catterall, William A.

Some inherited periodic paralyses are caused by mutations in skeletal muscle NaV1.4 sodium channels that alter channel gating and impair action potential generation. In the case of hypokalemic...

Temperature- and age-dependent seizures in a mouse model of severe myoclonic epilepsy in infancy

Oakley, John C., Kalume, Franck, Yu, Frank H., Scheuer, Todd, Catterall, William A.

Heterozygous loss-of-function mutations in the α subunit of the type I voltage-gated sodium channel NaV1.1 cause severe myoclonic epilepsy in infancy (SMEI), an infantile-onset epileptic...

Cooperative regulation of Cav1.2 channels by intracellular Mg2+, the proximal C-terminal EF-hand, and the distal C-terminal domain

Brunet, Sylvain, Scheuer, Todd, Catterall, William A.

L-type Ca2+ currents conducted by Cav1.2 channels initiate excitation–contraction coupling in cardiac myocytes. Intracellular Mg2+ (Mgi) inhibits the ionic current of Cav1.2 channels. Because Mgi...

Sequential formation of ion pairs during activation of a sodium channel voltage sensor

DeCaen, Paul G., Yarov-Yarovoy, Vladimir, Sharp, Elizabeth M., Scheuer, Todd, Catterall, William A.

Electrical signaling in biology depends upon a unique electromechanical transduction process mediated by the S4 segments of voltage-gated ion channels. These transmembrane segments are driven outward...

Molecular Requirements for Recognition of Brain Voltage-gated Sodium Channels by Scorpion α-Toxins*

Kahn, Roy, Karbat, Izhar, Ilan, Nitza, Cohen, Lior, Sokolov, Stanislav, Catterall, William A., ...

The scorpion α-toxin Lqh2 (from Leiurus quinquestriatus hebraeus) is active at various mammalian voltage-gated sodium channels (Navs) and is inactive at insect Navs. To resolve the molecular basis...