Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels.

PubWeight™: 1.50‹?› | Rank: Top 4%

🔗 View Article (PMID 17967784)

Published in Circ Res on October 25, 2007

Authors

Christopher A Ahern1, Amy L Eastwood, Dennis A Dougherty, Richard Horn

Author Affiliations

1: Department of Molecular Physiology & Biophysics, Institute of Hyperexcitability, Jefferson Medical College, Philadelphia, PA, USA. Christopher.Ahern@UBC.ca

Articles citing this

Y1767C, a novel SCN5A mutation, induces a persistent Na+ current and potentiates ranolazine inhibition of Nav1.5 channels. Am J Physiol Heart Circ Physiol (2010) 1.66

Intermediate state trapping of a voltage sensor. J Gen Physiol (2012) 1.20

Sodium channel molecular conformations and antiarrhythmic drug affinity. Trends Cardiovasc Med (2010) 1.20

Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J Gen Physiol (2008) 1.18

Molecular model of anticonvulsant drug binding to the voltage-gated sodium channel inner pore. Mol Pharmacol (2010) 1.16

Using lidocaine and benzocaine to link sodium channel molecular conformations to state-dependent antiarrhythmic drug affinity. Circ Res (2009) 1.16

Molecular determinants of local anesthetic action of beta-blocking drugs: Implications for therapeutic management of long QT syndrome variant 3. J Mol Cell Cardiol (2009) 1.05

The hitchhiker's guide to the voltage-gated sodium channel galaxy. J Gen Physiol (2016) 1.03

Bisphenol A binds to the local anesthetic receptor site to block the human cardiac sodium channel. PLoS One (2012) 1.03

The sodium channel as a target for local anesthetic drugs. Front Pharmacol (2011) 1.01

Targeting of sodium channel blockers into nociceptors to produce long-duration analgesia: a systematic study and review. Br J Pharmacol (2011) 1.00

Ion conduction and conformational flexibility of a bacterial voltage-gated sodium channel. Proc Natl Acad Sci U S A (2014) 0.99

Mutant bacterial sodium channels as models for local anesthetic block of eukaryotic proteins. Channels (Austin) (2016) 0.95

Molecular Insights into the Local Anesthetic Receptor within Voltage-Gated Sodium Channels Using Hydroxylated Analogs of Mexiletine. Front Pharmacol (2012) 0.93

In vivo incorporation of non-canonical amino acids by using the chemical aminoacylation strategy: a broadly applicable mechanistic tool. Chembiochem (2014) 0.90

Local anesthetic and antiepileptic drug access and binding to a bacterial voltage-gated sodium channel. Proc Natl Acad Sci U S A (2014) 0.89

Cross-species conservation of open-channel block by Na channel β4 peptides reveals structural features required for resurgent Na current. J Neurosci (2011) 0.88

Mechanism of sodium channel block by local anesthetics, antiarrhythmics, and anticonvulsants. J Gen Physiol (2017) 0.87

A homology model of the pore domain of a voltage-gated calcium channel is consistent with available SCAM data. J Gen Physiol (2010) 0.86

The opioid methadone induces a local anaesthetic-like inhibition of the cardiac Na⁺ channel, Na(v)1.5. Br J Pharmacol (2014) 0.86

Contributions of conserved residues at the gating interface of glycine receptors. J Biol Chem (2011) 0.86

Atom-by-atom engineering of voltage-gated ion channels: magnified insights into function and pharmacology. J Physiol (2015) 0.85

Structural determinants of drugs acting on the Nav1.8 channel. J Biol Chem (2009) 0.84

Analysis of the action of lidocaine on insect sodium channels. Insect Biochem Mol Biol (2010) 0.83

State-Dependent Inhibition of Sodium Channels by Local Anesthetics: A 40-Year Evolution. Biochem (Mosc) Suppl Ser A Membr Cell Biol (2012) 0.82

Investigating the size and dynamics of voltage-gated sodium channel fenestrations. Channels (Austin) (2014) 0.82

Molecular determinants of state-dependent block of voltage-gated sodium channels by pilsicainide. Br J Pharmacol (2010) 0.82

RNA editing in eag potassium channels: biophysical consequences of editing a conserved S6 residue. Channels (Austin) (2012) 0.82

Locating the route of entry and binding sites of benzocaine and phenytoin in a bacterial voltage gated sodium channel. PLoS Comput Biol (2014) 0.81

Classification of drugs based on properties of sodium channel inhibition: a comparative automated patch-clamp study. PLoS One (2010) 0.81

Use-dependent block of the voltage-gated Na(+) channel by tetrodotoxin and saxitoxin: effect of pore mutations that change ionic selectivity. J Gen Physiol (2012) 0.81

Chemical tools for K(+) channel biology. Biochemistry (2009) 0.80

Block of human cardiac sodium channels by lacosamide: evidence for slow drug binding along the activation pathway. Mol Pharmacol (2014) 0.79

Novel molecular determinants in the pore region of sodium channels regulate local anesthetic binding. Mol Pharmacol (2009) 0.79

Trans-channel interactions in batrachotoxin-modified skeletal muscle sodium channels: voltage-dependent block by cytoplasmic amines, and the influence of mu-conotoxin GIIIA derivatives and permeant ions. Biophys J (2008) 0.79

Antagonism of lidocaine inhibition by open-channel blockers that generate resurgent Na current. J Neurosci (2013) 0.78

Molecular and functional determinants of local anesthetic inhibition of NaChBac. Channels (Austin) (2012) 0.78

Lidocaine partially depolarizes the S4 segment in domain IV of the sodium channel. Pflugers Arch (2010) 0.77

Increased sensitivity to local anesthetic drugs: bedside to bench. Circ Res (2008) 0.75

Effect of flecainide derivatives on sarcoplasmic reticulum calcium release suggests a lack of direct action on the cardiac ryanodine receptor. Br J Pharmacol (2016) 0.75

Lacosamide Inhibition of Nav1.7 Voltage-Gated Sodium Channels: Slow Binding to Fast-Inactivated States. Mol Pharmacol (2017) 0.75

Articles by these authors

A gating charge transfer center in voltage sensors. Science (2010) 3.60

Cys-loop receptors: new twists and turns. Trends Neurosci (2004) 3.58

Cis-trans isomerization at a proline opens the pore of a neurotransmitter-gated ion channel. Nature (2005) 3.18

Cation-pi interactions in ligand recognition and catalysis. Trends Pharmacol Sci (2002) 2.75

Cation-pi interactions in ligand recognition by serotonergic (5-HT3A) and nicotinic acetylcholine receptors: the anomalous binding properties of nicotine. Biochemistry (2002) 2.22

Nicotine binding to brain receptors requires a strong cation-pi interaction. Nature (2009) 2.21

Focused electric field across the voltage sensor of potassium channels. Neuron (2005) 2.19

Nicotine is a selective pharmacological chaperone of acetylcholine receptor number and stoichiometry. Implications for drug discovery. AAPS J (2009) 1.68

A unified view of the role of electrostatic interactions in modulating the gating of Cys loop receptors. J Biol Chem (2005) 1.61

Specificity of charge-carrying residues in the voltage sensor of potassium channels. J Gen Physiol (2004) 1.60

A cation-pi binding interaction with a tyrosine in the binding site of the GABAC receptor. Chem Biol (2005) 1.53

Investigating the putative glycine hinge in Shaker potassium channel. J Gen Physiol (2005) 1.50

Stirring up controversy with a voltage sensor paddle. Trends Neurosci (2004) 1.50

Unnatural amino acid mutagenesis of the GABA(A) receptor binding site residues reveals a novel cation-pi interaction between GABA and beta 2Tyr97. J Neurosci (2007) 1.45

Using physical chemistry to differentiate nicotinic from cholinergic agonists at the nicotinic acetylcholine receptor. J Am Chem Soc (2005) 1.38

Investigating lipid composition effects on the mechanosensitive channel of large conductance (MscL) using molecular dynamics simulations. Biophys J (2003) 1.36

Tyrosine residues that control binding and gating in the 5-hydroxytryptamine3 receptor revealed by unnatural amino acid mutagenesis. J Neurosci (2004) 1.35

A fluorophore attached to nicotinic acetylcholine receptor beta M2 detects productive binding of agonist to the alpha delta site. Proc Natl Acad Sci U S A (2004) 1.34

Generation and evaluation of a large mutational library from the Escherichia coli mechanosensitive channel of large conductance, MscL: implications for channel gating and evolutionary design. J Biol Chem (2003) 1.34

A cation-pi interaction discriminates among sodium channels that are either sensitive or resistant to tetrodotoxin block. J Biol Chem (2007) 1.26

Voltage-dependent hydration and conduction properties of the hydrophobic pore of the mechanosensitive channel of small conductance. Biophys J (2006) 1.22

Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines. Proc Natl Acad Sci U S A (2012) 1.22

Different binding orientations for the same agonist at homologous receptors: a lock and key or a simple wedge? J Am Chem Soc (2003) 1.19

Tail end of the s6 segment: role in permeation in shaker potassium channels. J Gen Physiol (2002) 1.19

In vivo incorporation of multiple unnatural amino acids through nonsense and frameshift suppression. Proc Natl Acad Sci U S A (2006) 1.19

A cation-pi interaction in the binding site of the glycine receptor is mediated by a phenylalanine residue. J Neurosci (2008) 1.18

Nicotinic pharmacophore: the pyridine N of nicotine and carbonyl of acetylcholine hydrogen bond across a subunit interface to a backbone NH. Proc Natl Acad Sci U S A (2010) 1.18

Movement and crevices around a sodium channel S3 segment. J Gen Physiol (2002) 1.18

A cation-pi interaction between extracellular TEA and an aromatic residue in potassium channels. J Gen Physiol (2006) 1.17

Unnatural amino acid mutagenesis in mapping ion channel function. Curr Opin Neurobiol (2003) 1.16

An intersubunit hydrogen bond in the nicotinic acetylcholine receptor that contributes to channel gating. J Biol Chem (2008) 1.14

Effect of S6 tail mutations on charge movement in Shaker potassium channels. Biophys J (2003) 1.14

Chemical-scale studies on the role of a conserved aspartate in preorganizing the agonist binding site of the nicotinic acetylcholine receptor. Biochemistry (2007) 1.12

A hydrogen bond in loop A is critical for the binding and function of the 5-HT3 receptor. Biochemistry (2008) 1.12

Two neuronal nicotinic acetylcholine receptors, alpha4beta4 and alpha7, show differential agonist binding modes. J Biol Chem (2011) 1.08

Regulated RNA editing and functional epistasis in Shaker potassium channels. J Gen Physiol (2009) 1.07

Long-range coupling in an allosteric receptor revealed by mutant cycle analysis. Biophys J (2009) 1.07

Establishing an ion pair interaction in the homomeric rho1 gamma-aminobutyric acid type A receptor that contributes to the gating pathway. J Biol Chem (2007) 1.06

Total chemical synthesis and electrophysiological characterization of mechanosensitive channels from Escherichia coli and Mycobacterium tuberculosis. Proc Natl Acad Sci U S A (2004) 1.03

Modulation of the cardiac sodium channel NaV1.5 by Fyn, a Src family tyrosine kinase. Circ Res (2005) 1.02

Probing the role of the cation-pi interaction in the binding sites of GPCRs using unnatural amino acids. Proc Natl Acad Sci U S A (2009) 1.01

Single-molecule imaging of a fluorescent unnatural amino acid incorporated into nicotinic receptors. Biophys J (2009) 1.01

Improved amber and opal suppressor tRNAs for incorporation of unnatural amino acids in vivo. Part 1: minimizing misacylation. RNA (2007) 1.00

Conformation-dependent hydrophobic photolabeling of the nicotinic receptor: electrophysiology-coordinated photochemistry and mass spectrometry. Proc Natl Acad Sci U S A (2003) 0.99

Variations in binding among several agonists at two stoichiometries of the neuronal, α4β2 nicotinic receptor. J Am Chem Soc (2012) 0.98

Caged phosphoproteins. J Am Chem Soc (2005) 0.98

Characterization of five RNA editing sites in Shab potassium channels. Channels (Austin) (2008) 0.98

Pharmacological chaperoning of nicotinic acetylcholine receptors reduces the endoplasmic reticulum stress response. Mol Pharmacol (2012) 0.98

Site-specific incorporation of unnatural amino acids into receptors expressed in Mammalian cells. Chem Biol (2003) 0.97

MALDI-TOF mass spectrometry methods for evaluation of in vitro aminoacyl tRNA production. RNA (2002) 0.95

Calcium block of single sodium channels: role of a pore-lining aromatic residue. Biophys J (2007) 0.95

Improved amber and opal suppressor tRNAs for incorporation of unnatural amino acids in vivo. Part 2: evaluating suppression efficiency. RNA (2007) 0.93

A cation-π interaction at a phenylalanine residue in the glycine receptor binding site is conserved for different agonists. Mol Pharmacol (2011) 0.92

Reconstitution of ion channels in agarose-supported silicon orifices. Biosens Bioelectron (2006) 0.91

The 5-HT3AB receptor shows an A3B2 stoichiometry at the plasma membrane. Biophys J (2013) 0.91

Live-cell imaging of single receptor composition using zero-mode waveguide nanostructures. Nano Lett (2012) 0.90

Caging proteins through unnatural amino acid mutagenesis. Methods Enzymol (2003) 0.89

Two amino acid residues contribute to a cation-π binding interaction in the binding site of an insect GABA receptor. J Neurosci (2011) 0.89

Förster resonance energy transfer (FRET) correlates of altered subunit stoichiometry in cys-loop receptors, exemplified by nicotinic α4β2. Int J Mol Sci (2012) 0.88

An electrostatic interaction between TEA and an introduced pore aromatic drives spring-in-the-door inactivation in Shaker potassium channels. J Gen Physiol (2009) 0.88

Probing the role of backbone hydrogen bonding in a critical beta sheet of the extracellular domain of a cys-loop receptor. Chembiochem (2009) 0.86

Functional probes of drug-receptor interactions implicated by structural studies: Cys-loop receptors provide a fertile testing ground. J Med Chem (2014) 0.86

Probing the Mg2+ blockade site of an N-methyl-D-aspartate (NMDA) receptor with unnatural amino acid mutagenesis. ACS Chem Biol (2006) 0.86

5-Fluorotryptamine is a partial agonist at 5-HT3 receptors, and reveals that size and electronegativity at the 5 position of tryptamine are critical for efficient receptor function. Eur J Pharmacol (2007) 0.86

A coupled array of noncovalent interactions impacts the function of the 5-HT3A serotonin receptor in an agonist-specific way. ACS Chem Neurosci (2012) 0.85

Binding interactions with the complementary subunit of nicotinic receptors. J Biol Chem (2013) 0.85

Evidence for an extended hydrogen bond network in the binding site of the nicotinic receptor: role of the vicinal disulfide of the alpha1 subunit. J Biol Chem (2011) 0.84

Chemical scale studies of the Phe-Pro conserved motif in the cys loop of Cys loop receptors. J Biol Chem (2010) 0.83

Ondansetron and granisetron binding orientation in the 5-HT(3) receptor determined by unnatural amino acid mutagenesis. ACS Chem Biol (2012) 0.83

Multiple Tyrosine Residues Contribute to GABA Binding in the GABA(C) Receptor Binding Pocket. ACS Chem Neurosci (2011) 0.83

Dissecting the functions of conserved prolines within transmembrane helices of the D2 dopamine receptor. ACS Chem Biol (2011) 0.82

RNA editing in eag potassium channels: biophysical consequences of editing a conserved S6 residue. Channels (Austin) (2012) 0.82

Key binding interactions for memantine in the NMDA receptor. ACS Chem Neurosci (2012) 0.82

GABA binding to an insect GABA receptor: a molecular dynamics and mutagenesis study. Biophys J (2012) 0.82

Functionally important aromatic-aromatic and sulfur-π interactions in the D2 dopamine receptor. J Am Chem Soc (2012) 0.82

Functional evaluation of key interactions evident in the structure of the eukaryotic Cys-loop receptor GluCl. ACS Chem Biol (2014) 0.82

A stereochemical test of a proposed structural feature of the nicotinic acetylcholine receptor. J Am Chem Soc (2008) 0.82

An unusual pattern of ligand-receptor interactions for the α7 nicotinic acetylcholine receptor, with implications for the binding of varenicline. Mol Pharmacol (2013) 0.81

Human genome search in celiac disease: mutated gliadin T-cell-like epitope in two human proteins promotes T-cell activation. J Mol Biol (2002) 0.80

Using mutant cycle analysis to elucidate long-range functional coupling in allosteric receptors. Methods Mol Biol (2012) 0.80

New insights into the therapeutic inhibition of voltage-gated sodium channels. Channels (Austin) (2008) 0.80

Confirming the revised C-terminal domain of the MscL crystal structure. Biophys J (2008) 0.79

1-Oxo-5-hydroxytryptamine: a surprisingly potent agonist of the 5-HT3 (serotonin) receptor. Org Lett (2007) 0.79

Photochemical proteolysis of an unstructured linker of the GABAAR extracellular domain prevents GABA but not pentobarbital activation. Mol Pharmacol (2010) 0.79

A perturbed pK(a) at the binding site of the nicotinic acetylcholine receptor: implications for nicotine binding. J Am Chem Soc (2002) 0.78

Physiology: legacy of leaky channels. Nature (2007) 0.78

Selective ligand behaviors provide new insights into agonist activation of nicotinic acetylcholine receptors. ACS Chem Biol (2014) 0.78

Investigation of apparent mass deviations in electrospray ionization tandem mass spectrometry of a benzophenone-labeled peptide. Rapid Commun Mass Spectrom (2003) 0.78

Probing the effects of residues located outside the agonist binding site on drug-receptor selectivity in the nicotinic receptor. ACS Chem Biol (2012) 0.77

A selenide-based approach to photochemical cleavage of peptide and protein backbones at engineered backbone esters. J Org Chem (2009) 0.76