Tryptophan scanning mutagenesis in TM4 of the GABA(A) receptor alpha1 subunit: implications for modulation by inhaled anesthetics and ion channel structure.

PubWeight™: 1.08‹?› | Rank: Top 10%

🔗 View Article (PMID 12367612)

Published in Neuropharmacology on September 01, 2002

Authors

Andrew Jenkins1, Alyson Andreasen, James R Trudell, Neil L Harrison

Author Affiliations

1: Department of Anesthesiology, Weill Medical College of Cornell University, New York, NY 10021, USA. anj2005@med.cornell.edu

Articles citing this

A unitary anesthetic binding site at high resolution. J Biol Chem (2009) 1.34

Secondary structure and gating rearrangements of transmembrane segments in rat P2X4 receptor channels. J Gen Physiol (2005) 1.30

General anesthetic actions on GABA(A) receptors. Curr Neuropharmacol (2010) 1.16

Modeling anesthetic binding sites within the glycine alpha one receptor based on prokaryotic ion channel templates: the problem with TM4. J Chem Inf Model (2010) 1.05

General anesthetics have additive actions on three ligand gated ion channels. Anesth Analg (2008) 1.03

New insights into the molecular mechanisms of general anaesthetics. Br J Pharmacol (2010) 1.02

GABA(A) receptor transmembrane amino acids are critical for alcohol action: disulfide cross-linking and alkyl methanethiosulfonate labeling reveal relative location of binding sites. J Neurochem (2013) 0.88

The natural products magnolol and honokiol are positive allosteric modulators of both synaptic and extra-synaptic GABA(A) receptors. Neuropharmacology (2012) 0.86

Modulating inhibitory ligand-gated ion channels. AAPS J (2006) 0.86

Control of ethanol sensitivity of the glycine receptor α3 subunit by transmembrane 2, the intracellular splice cassette and C-terminal domains. J Pharmacol Exp Ther (2015) 0.81

The relative orientation of the TM3 and TM4 domains varies between α1 and α3 glycine receptors. ACS Chem Neurosci (2012) 0.81

Fourier transform coupled to tryptophan-scanning mutagenesis: lessons from its application to the prediction of secondary structure in the acetylcholine receptor lipid-exposed transmembrane domains. Biochim Biophys Acta (2008) 0.79

Tryptophan scanning of the acetylcholine receptor's betaM4 transmembrane domain: decoding allosteric linkage at the lipid-protein interface with ion-channel gating. Channels (Austin) (2008) 0.79

Normal mode gating motions of a ligand-gated ion channel persist in a fully hydrated lipid bilayer model. ACS Chem Neurosci (2010) 0.79

Fourier transform coupled tryptophan scanning mutagenesis identifies a bending point on the lipid-exposed δM3 transmembrane domain of the Torpedo californica nicotinic acetylcholine receptor. Channels (Austin) (2011) 0.78

Tryptophan scanning mutagenesis reveals distortions in the helical structure of the δM4 transmembrane domain of the Torpedo californica nicotinic acetylcholine receptor. Channels (Austin) (2012) 0.77

Recognition of anesthetic barbiturates by a protein binding site: a high resolution structural analysis. PLoS One (2012) 0.77

The Molecular Mechanisms of Anesthetic Action: Updates and Cutting Edge Developments from the Field of Molecular Modeling. Pharmaceuticals (Basel) (2010) 0.75

Articles by these authors

Derivation of midbrain dopamine neurons from human embryonic stem cells. Proc Natl Acad Sci U S A (2004) 7.51

Neural subtype specification of fertilization and nuclear transfer embryonic stem cells and application in parkinsonian mice. Nat Biotechnol (2003) 3.43

Emerging molecular mechanisms of general anesthetic action. Trends Pharmacol Sci (2005) 2.91

Coupling of agonist binding to channel gating in the GABA(A) receptor. Nature (2003) 2.89

Extrasynaptic GABAA receptors: form, pharmacology, and function. J Neurosci (2009) 2.39

An extrasynaptic GABAA receptor mediates tonic inhibition in thalamic VB neurons. J Neurophysiol (2005) 2.22

Ethanol's molecular targets. Sci Signal (2008) 2.06

Structural basis for alcohol modulation of a pentameric ligand-gated ion channel. Proc Natl Acad Sci U S A (2011) 1.52

Taurine is a potent activator of extrasynaptic GABA(A) receptors in the thalamus. J Neurosci (2008) 1.45

Microsecond simulations indicate that ethanol binds between subunits and could stabilize an open-state model of a glycine receptor. Biophys J (2011) 1.42

Normal acute behavioral responses to moderate/high dose ethanol in GABAA receptor alpha 4 subunit knockout mice. Alcohol Clin Exp Res (2007) 1.39

Evidence that ethanol acts on a target in Loop 2 of the extracellular domain of alpha1 glycine receptors. J Neurochem (2007) 1.26

Ethanol modulates synaptic and extrasynaptic GABAA receptors in the thalamus. J Pharmacol Exp Ther (2008) 1.22

Alcohol regulates gene expression in neurons via activation of heat shock factor 1. J Neurosci (2007) 1.19

Charged residues in the beta2 subunit involved in GABAA receptor activation. J Biol Chem (2003) 1.18

Loop 2 structure in glycine and GABA(A) receptors plays a key role in determining ethanol sensitivity. J Biol Chem (2009) 1.16

Sites of excitatory and inhibitory actions of alcohols on neuronal alpha2beta4 nicotinic acetylcholine receptors. J Pharmacol Exp Ther (2003) 1.14

Knockin mice with ethanol-insensitive alpha1-containing gamma-aminobutyric acid type A receptors display selective alterations in behavioral responses to ethanol. J Pharmacol Exp Ther (2006) 1.14

A highly conserved aspartic acid residue in the signature disulfide loop of the alpha 1 subunit is a determinant of gating in the glycine receptor. J Biol Chem (2003) 1.14

Prolongation of hippocampal miniature inhibitory postsynaptic currents in mice lacking the GABA(A) receptor alpha1 subunit. J Neurophysiol (2002) 1.14

Isoflurane is a potent modulator of extrasynaptic GABA(A) receptors in the thalamus. J Pharmacol Exp Ther (2007) 1.13

The common chemical motifs within anesthetic binding sites. Anesth Analg (2007) 1.13

4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor. J Med Chem (2002) 1.11

Channel gating of the glycine receptor changes accessibility to residues implicated in receptor potentiation by alcohols and anesthetics. J Biol Chem (2004) 1.10

A novel hyperekplexia-causing mutation in the pre-transmembrane segment 1 of the human glycine receptor alpha1 subunit reduces membrane expression and impairs gating by agonists. J Biol Chem (2004) 1.09

The actions of sevoflurane and desflurane on the gamma-aminobutyric acid receptor type A: effects of TM2 mutations in the alpha and beta subunits. Anesthesiology (2003) 1.08

Accessibility to residues in transmembrane segment four of the glycine receptor. Neuropharmacology (2005) 1.08

Cross-linking of sites involved with alcohol action between transmembrane segments 1 and 3 of the glycine receptor following activation. J Neurochem (2007) 1.08

Effect of isoflurane and other potent inhaled anesthetics on minimum alveolar concentration, learning, and the righting reflex in mice engineered to express alpha1 gamma-aminobutyric acid type A receptors unresponsive to isoflurane. Anesthesiology (2007) 1.07

Propofol block of I(h) contributes to the suppression of neuronal excitability and rhythmic burst firing in thalamocortical neurons. Eur J Neurosci (2006) 1.06

Modeling anesthetic binding sites within the glycine alpha one receptor based on prokaryotic ion channel templates: the problem with TM4. J Chem Inf Model (2010) 1.05

General anesthetics have additive actions on three ligand gated ion channels. Anesth Analg (2008) 1.03

Molecular targets and mechanisms for ethanol action in glycine receptors. Pharmacol Ther (2010) 1.03

Impairment of hyperpolarization-activated, cyclic nucleotide-gated channel function by the intravenous general anesthetic propofol. J Pharmacol Exp Ther (2005) 1.03

Endothelial fate mapping in mice with pulmonary hypertension. Circulation (2013) 1.02

Targets for ethanol action and antagonism in loop 2 of the extracellular domain of glycine receptors. J Neurochem (2008) 1.02

Striatal D2 receptors regulate dendritic morphology of medium spiny neurons via Kir2 channels. J Neurosci (2012) 1.02

Ivermectin antagonizes ethanol inhibition in purinergic P2X4 receptors. J Pharmacol Exp Ther (2010) 1.01

Homology modeling of a human glycine alpha 1 receptor reveals a plausible anesthetic binding site. J Chem Inf Model (2005) 1.01

Anesthetic and ethanol effects on spontaneously opening glycine receptor channels. J Neurochem (2002) 1.00

Transcriptional regulation of the mouse gene encoding the alpha-4 subunit of the GABAA receptor. J Biol Chem (2004) 0.99

Alcohol-binding sites in distinct brain proteins: the quest for atomic level resolution. Alcohol Clin Exp Res (2011) 0.99

Zinc enhances ethanol modulation of the alpha1 glycine receptor. Neuropharmacology (2009) 0.99

Characterization of two mutations, M287L and Q266I, in the α1 glycine receptor subunit that modify sensitivity to alcohols. J Pharmacol Exp Ther (2011) 0.99

GABAA receptors in the thalamus: alpha4 subunit expression and alcohol sensitivity. Alcohol (2007) 0.98

The pre-M1 segment of the alpha1 subunit is a transduction element in the activation of the GABAA receptor. J Physiol (2006) 0.98

The modulation of synaptic GABA(A) receptors in the thalamus by eszopiclone and zolpidem. J Pharmacol Exp Ther (2008) 0.97

Cross-linking of glycine receptor transmembrane segments two and three alters coupling of ligand binding with channel opening. J Neurochem (2004) 0.97

Normal-mode analysis of the glycine alpha1 receptor by three separate methods. J Chem Inf Model (2007) 0.96

Molecular mechanism for the dual alcohol modulation of Cys-loop receptors. PLoS Comput Biol (2012) 0.95

Multiple sites of ethanol action in alpha1 and alpha2 glycine receptors suggested by sensitivity to pressure antagonism. J Neurochem (2004) 0.95

A transmembrane amino acid in the GABAA receptor β2 subunit critical for the actions of alcohols and anesthetics. J Pharmacol Exp Ther (2010) 0.94

Ethanol potentiation of glycine receptors expressed in Xenopus oocytes antagonized by increased atmospheric pressure. Alcohol Clin Exp Res (2003) 0.94

Disruption of an intersubunit electrostatic bond is a critical step in glycine receptor activation. Proc Natl Acad Sci U S A (2010) 0.93

Evaluation of a proposed mechanism of ligand-gated ion channel activation in the GABAA and glycine receptors. Neurosci Lett (2004) 0.93

Alanine-scanning mutagenesis in the signature disulfide loop of the glycine receptor alpha 1 subunit: critical residues for activation and modulation. Biochemistry (2004) 0.93

Molecular volume determines the activity of the halogenated alkane bromoform at wild-type and mutant GABA(A) receptors. Brain Res (2003) 0.92

Agonist-dependent single channel current and gating in alpha4beta2delta and alpha1beta2gamma2S GABAA receptors. J Gen Physiol (2008) 0.92

Molecular modeling and mutagenesis reveals a tetradentate binding site for Zn2+ in GABA(A) alphabeta receptors and provides a structural basis for the modulating effect of the gamma subunit. J Chem Inf Model (2008) 0.91

Roles for loop 2 residues of alpha1 glycine receptors in agonist activation. J Biol Chem (2008) 0.90

Seeking structural specificity: direct modulation of pentameric ligand-gated ion channels by alcohols and general anesthetics. Pharmacol Rev (2014) 0.90

Charge and geometry of residues in the loop 2 β hairpin differentially affect agonist and ethanol sensitivity in glycine receptors. J Pharmacol Exp Ther (2012) 0.90

The regulation of neuronal gene expression by alcohol. Pharmacol Ther (2009) 0.90

Assessment of homology templates and an anesthetic binding site within the γ-aminobutyric acid receptor. Anesthesiology (2013) 0.90

Transmembrane residues define the action of isoflurane at the GABAA receptor alpha-3 subunit. Brain Res (2005) 0.90

Stabilization of the GluCl ligand-gated ion channel in the presence and absence of ivermectin. Biophys J (2013) 0.90

Are sobriety and consciousness determined by water in protein cavities? Alcohol Clin Exp Res (2004) 0.89

The activation mechanism of alpha1beta2gamma2S and alpha3beta3gamma2S GABAA receptors. J Gen Physiol (2010) 0.89

Molecular mechanisms and binding site location for the noncompetitive antagonist crystal violet on nicotinic acetylcholine receptors. Biochemistry (2006) 0.89

GABA(A) receptor transmembrane amino acids are critical for alcohol action: disulfide cross-linking and alkyl methanethiosulfonate labeling reveal relative location of binding sites. J Neurochem (2013) 0.88

Noncompetitive antagonist binding sites in the torpedo nicotinic acetylcholine receptor ion channel. Structure-activity relationship studies using adamantane derivatives. Biochemistry (2003) 0.88

Structural models of ligand-gated ion channels: sites of action for anesthetics and ethanol. Alcohol Clin Exp Res (2013) 0.88

Isoflurane modulates excitability in the mouse thalamus via GABA-dependent and GABA-independent mechanisms. Neuropharmacology (2008) 0.86

The effects of isoflurane on desensitized wild-type and alpha 1(S270H) gamma-aminobutyric acid type A receptors. Anesth Analg (2004) 0.86

Effect of cobratoxin binding on the normal mode vibration within acetylcholine binding protein. J Chem Inf Model (2008) 0.86

Mutation of a zinc-binding residue in the glycine receptor α1 subunit changes ethanol sensitivity in vitro and alcohol consumption in vivo. J Pharmacol Exp Ther (2012) 0.86

Zinc-dependent modulation of α2- and α3-glycine receptor subunits by ethanol. Alcohol Clin Exp Res (2013) 0.85

Inhibition versus potentiation of ligand-gated ion channels can be altered by a single mutation that moves ligands between intra- and intersubunit sites. Structure (2013) 0.85

Identifying the binding site(s) for antidepressants on the Torpedo nicotinic acetylcholine receptor: [3H]2-azidoimipramine photolabeling and molecular dynamics studies. Biochim Biophys Acta (2008) 0.84

Anesthetics interfere with axon guidance in developing mouse neocortical neurons in vitro via a γ-aminobutyric acid type A receptor mechanism. Anesthesiology (2013) 0.84

Unique general anesthetic binding sites within distinct conformational states of the nicotinic acetylcholine receptor. Int Rev Neurobiol (2003) 0.84

Effects of isoflurane on gamma-aminobutyric acid type A receptors activated by full and partial agonists. Anesthesiology (2003) 0.83

Brief alcohol exposure alters transcription in astrocytes via the heat shock pathway. Brain Behav (2013) 0.82

The TM2 6' position of GABA(A) receptors mediates alcohol inhibition. J Pharmacol Exp Ther (2011) 0.82

GABA(A)-R alpha1 subunit knockin mutation leads to abnormal EEG and anesthetic-induced seizure-like activity in mice. Brain Res (2006) 0.80

Alcohol-induced tolerance and physical dependence in mice with ethanol insensitive alpha1 GABA A receptors. Alcohol Clin Exp Res (2008) 0.79

Normal mode gating motions of a ligand-gated ion channel persist in a fully hydrated lipid bilayer model. ACS Chem Neurosci (2010) 0.79

Hemoglobin metabolites mimic benzodiazepines and are possible mediators of hepatic encephalopathy. Blood (2003) 0.77

Knockin' on the door of general anesthetic mechanisms: but will U.S. researchers be shut out? Anesth Analg (2003) 0.76

Molecular modeling of a tandem two pore domain potassium channel reveals a putative binding site for general anesthetics. ACS Chem Neurosci (2014) 0.76

The minimum alveolar anesthetic concentration of 2-, 3-, and 4-alcohols and ketones in rats: relevance to anesthetic mechanisms. Anesth Analg (2006) 0.76

Induced changes in protein receptors conferring resistance to anesthetics. Curr Opin Anaesthesiol (2012) 0.75

Acetaldehyde, not ethanol, impairs myelin formation and viability in primary mouse oligodendrocytes. Alcohol Clin Exp Res (2015) 0.75

General anesthesia research: aroused from a deep sleep? Nat Neurosci (2002) 0.75