Structural basis of open channel block in a prokaryotic pentameric ligand-gated ion channel.

PubWeight™: 1.36‹?› | Rank: Top 10%

🔗 View Article (PMID 21037567)

Published in Nat Struct Mol Biol on October 31, 2010

Authors

Ricarda J C Hilf1, Carlo Bertozzi, Iwan Zimmermann, Alwin Reiter, Dirk Trauner, Raimund Dutzler

Author Affiliations

1: Department of Biochemistry, University of Zürich, Zürich, Switzerland.

Articles citing this

Signal Transduction at the Domain Interface of Prokaryotic Pentameric Ligand-Gated Ion Channels. PLoS Biol (2016) 1.42

Mass spectrometry of intact membrane protein complexes. Nat Protoc (2013) 1.41

Structural basis for ion permeation mechanism in pentameric ligand-gated ion channels. EMBO J (2013) 1.37

Ligand activation of the prokaryotic pentameric ligand-gated ion channel ELIC. PLoS Biol (2011) 1.37

Structural basis for potentiation by alcohols and anaesthetics in a ligand-gated ion channel. Nat Commun (2013) 1.35

Multisite binding of a general anesthetic to the prokaryotic pentameric Erwinia chrysanthemi ligand-gated ion channel (ELIC). J Biol Chem (2013) 1.22

Desensitization mechanism in prokaryotic ligand-gated ion channel. J Biol Chem (2012) 1.07

Conformational transitions underlying pore opening and desensitization in membrane-embedded Gloeobacter violaceus ligand-gated ion channel (GLIC). J Biol Chem (2012) 1.04

General anesthetics predicted to block the GLIC pore with micromolar affinity. PLoS Comput Biol (2012) 1.02

Isoflurane alters the structure and dynamics of GLIC. Biophys J (2011) 1.00

Control over molecular motion using the cis-trans photoisomerization of the azo group. Beilstein J Org Chem (2012) 0.97

Inhibition of the prokaryotic pentameric ligand-gated ion channel ELIC by divalent cations. PLoS Biol (2012) 0.96

Engineering a prokaryotic Cys-loop receptor with a third functional domain. J Biol Chem (2011) 0.94

The pharmacological profile of ELIC, a prokaryotic GABA-gated receptor. Neuropharmacology (2012) 0.93

Expression and characterization of the bacterial mechanosensitive channel MscS in Xenopus laevis oocytes. J Gen Physiol (2011) 0.92

Bacterial voltage-gated sodium channels (BacNa(V)s) from the soil, sea, and salt lakes enlighten molecular mechanisms of electrical signaling and pharmacology in the brain and heart. J Mol Biol (2014) 0.91

Cys-loop receptor channel blockers also block GLIC. Biophys J (2011) 0.90

Experimental determination of the vertical alignment between the second and third transmembrane segments of muscle nicotinic acetylcholine receptors. J Neurochem (2013) 0.90

NMR resolved multiple anesthetic binding sites in the TM domains of the α4β2 nAChR. Biochim Biophys Acta (2012) 0.89

A predicted binding site for cholesterol on the GABAA receptor. Biophys J (2014) 0.86

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

Conduits of life's spark: a perspective on ion channel research since the birth of neuron. Neuron (2013) 0.84

Energy for wild-type acetylcholine receptor channel gating from different choline derivatives. Biophys J (2013) 0.84

Structural Basis for Xenon Inhibition in a Cationic Pentameric Ligand-Gated Ion Channel. PLoS One (2016) 0.83

Direct Pore Binding as a Mechanism for Isoflurane Inhibition of the Pentameric Ligand-gated Ion Channel ELIC. Sci Rep (2015) 0.82

The atypical cation-conduction and gating properties of ELIC underscore the marked functional versatility of the pentameric ligand-gated ion-channel fold. J Gen Physiol (2015) 0.81

Structural and functional characterization of an anesthetic binding site in the second cysteine-rich domain of protein kinase Cδ*. Biophys J (2012) 0.81

Distribution and dynamics of electron transport complexes in cyanobacterial thylakoid membranes. Biochim Biophys Acta (2015) 0.80

Functional Chimeras of GLIC Obtained by Adding the Intracellular Domain of Anion- and Cation-Conducting Cys-Loop Receptors. Biochemistry (2015) 0.80

Atomistic models of general anesthetics for use in in silico biological studies. J Phys Chem B (2014) 0.78

Conformational changes in acetylcholine binding protein investigated by temperature accelerated molecular dynamics. PLoS One (2014) 0.78

Ethanol Modulation is Quantitatively Determined by the Transmembrane Domain of Human α1 Glycine Receptors. Alcohol Clin Exp Res (2015) 0.77

Structural Studies of GABAA Receptor Binding Sites: Which Experimental Structure Tells us What? Front Mol Neurosci (2016) 0.77

Characterizing the fatty acid binding site in the cavity of potassium channel KcsA. Biochemistry (2012) 0.77

A Structural Model of the Human α7 Nicotinic Receptor in an Open Conformation. PLoS One (2015) 0.76

Structure and Pharmacologic Modulation of Inhibitory Glycine Receptors. Mol Pharmacol (2016) 0.76

Prediction and validation of protein intermediate states from structurally rich ensembles and coarse-grained simulations. Nat Commun (2016) 0.76

Pentameric Ligand-gated Ion Channels : Insights from Computation. Mol Simul (2014) 0.76

Muscle-Type Nicotinic Receptor Blockade by Diethylamine, the Hydrophilic Moiety of Lidocaine. Front Mol Neurosci (2016) 0.76

Allosteric binding site in a Cys-loop receptor ligand-binding domain unveiled in the crystal structure of ELIC in complex with chlorpromazine. Proc Natl Acad Sci U S A (2016) 0.75

The cellular membrane as a mediator for small molecule interaction with membrane proteins. Biochim Biophys Acta (2016) 0.75

Expressing and characterizing mechanosensitive channels in Xenopus oocytes. Methods Mol Biol (2015) 0.75

Crosslinking constraints and computational models as complementary tools in modeling the extracellular domain of the glycine receptor. PLoS One (2014) 0.75

Crystal structure and dynamics of a lipid-induced potential desensitized-state of a pentameric ligand-gated channel. Elife (2017) 0.75

Poly(ethylene glycol) as a scaffold for high-affinity open-channel blockers of the mouse nicotinic acetylcholine receptor. PLoS One (2014) 0.75

Articles cited by this

The CCP4 suite: programs for protein crystallography. Acta Crystallogr D Biol Crystallogr (1994) 187.88

Improved methods for building protein models in electron density maps and the location of errors in these models. Acta Crystallogr A (1991) 119.63

PHENIX: building new software for automated crystallographic structure determination. Acta Crystallogr D Biol Crystallogr (2002) 53.61

Ionic blockage of sodium channels in nerve. J Gen Physiol (1973) 20.47

Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axons. J Gen Physiol (1971) 14.23

Reduced surface: an efficient way to compute molecular surfaces. Biopolymers (1996) 10.62

Local anaesthetics transiently block currents through single acetylcholine-receptor channels. J Physiol (1978) 10.05

Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance. Nature (1988) 6.35

X-ray structure of a prokaryotic pentameric ligand-gated ion channel. Nature (2008) 6.02

Emerging structure of the nicotinic acetylcholine receptors. Nat Rev Neurosci (2002) 5.87

X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation. Nature (2008) 5.77

Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel. Nature (2008) 5.09

The permeability of endplate channels to monovalent and divalent metal cations. J Gen Physiol (1980) 4.72

Recent advances in Cys-loop receptor structure and function. Nature (2006) 4.20

Nicotinic receptors at the amino acid level. Annu Rev Pharmacol Toxicol (2000) 4.04

A prokaryotic proton-gated ion channel from the nicotinic acetylcholine receptor family. Nature (2006) 3.04

Common mode of action of three agents that decrease the transient change in sodium permeability in nerves. Nature (1966) 2.90

Evidence that the M2 membrane-spanning region lines the ion channel pore of the nicotinic receptor. Science (1988) 2.31

Heteromultimeric CLC chloride channels with novel properties. Proc Natl Acad Sci U S A (1996) 2.28

Monovalent and divalent cation permeation in acetylcholine receptor channels. Ion transport related to structure. J Gen Physiol (1987) 2.20

Mutations at two distinct sites within the channel domain M2 alter calcium permeability of neuronal alpha 7 nicotinic receptor. Proc Natl Acad Sci U S A (1993) 2.14

An open-channel blocker interacts with adjacent turns of alpha-helices in the nicotinic acetylcholine receptor. Neuron (1990) 2.06

Location of a delta-subunit region determining ion transport through the acetylcholine receptor channel. Nature (1987) 1.99

Structural basis of TEA blockade in a model potassium channel. Nat Struct Mol Biol (2005) 1.77

Rings of anionic amino acids as structural determinants of ion selectivity in the acetylcholine receptor channel. Proc Biol Sci (1991) 1.59

The intrinsic electrostatic potential and the intermediate ring of charge in the acetylcholine receptor channel. J Gen Physiol (2000) 1.56

Reaction of tetraethylammonium with the open and closed conformations of the acetylcholine receptor ionic channel complex. J Gen Physiol (1979) 1.54

The noncompetitive blocker [3H]chlorpromazine labels three amino acids of the acetylcholine receptor gamma subunit: implications for the alpha-helical organization of regions MII and for the structure of the ion channel. Proc Natl Acad Sci U S A (1990) 1.43

The alpha9alpha10 nicotinic acetylcholine receptor is permeable to and is modulated by divalent cations. Hear Res (2002) 1.37

A prokaryotic perspective on pentameric ligand-gated ion channel structure. Curr Opin Struct Biol (2009) 1.23

Monovalent and divalent cation permeability and block of neuronal nicotinic receptor channels in rat parasympathetic ganglia. J Gen Physiol (1995) 1.12

Delimiting the binding site for quaternary ammonium lidocaine derivatives in the acetylcholine receptor channel. J Gen Physiol (1998) 1.01

Molecular mechanisms of inhibition of nicotinic acetylcholine receptors by tricyclic antidepressants. Neuropharmacology (2003) 0.96

Structural effects of quinacrine binding in the open channel of the acetylcholine receptor. Proc Natl Acad Sci U S A (2003) 0.87

Chlorpromazine and QX222 block 5-HT3 receptors in N1E-115 neuroblastoma cells. Neuropharmacology (1994) 0.83

Articles by these authors

X-ray structure of a prokaryotic pentameric ligand-gated ion channel. Nature (2008) 6.02

Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel. Nature (2008) 5.09

Light-activated ion channels for remote control of neuronal firing. Nat Neurosci (2004) 4.42

Remote control of neuronal activity with a light-gated glutamate receptor. Neuron (2007) 3.45

Allosteric control of an ionotropic glutamate receptor with an optical switch. Nat Chem Biol (2005) 3.23

The B-Alkyl Suzuki-Miyaura Cross-Coupling Reaction: Development, Mechanistic Study, and Applications in Natural Product Synthesis A list of abbreviations can be found at the end of the article. Angew Chem Int Ed Engl (2001) 2.69

Optogenetic dissection of a behavioural module in the vertebrate spinal cord. Nature (2009) 2.61

Photochemical control of endogenous ion channels and cellular excitability. Nat Methods (2008) 2.30

Photochemical restoration of visual responses in blind mice. Neuron (2012) 2.16

Synergism between halide binding and proton transport in a CLC-type exchanger. J Mol Biol (2006) 1.90

Nucleotide recognition by the cytoplasmic domain of the human chloride transporter ClC-5. Nat Struct Mol Biol (2006) 1.85

Catalysis of 6pi electrocyclizations. Angew Chem Int Ed Engl (2008) 1.62

Mechanisms of photoswitch conjugation and light activation of an ionotropic glutamate receptor. Proc Natl Acad Sci U S A (2007) 1.62

Optochemical genetics. Angew Chem Int Ed Engl (2011) 1.61

The chemistry of marine furanocembranoids, pseudopteranes, gersolanes, and related natural products. Nat Prod Rep (2008) 1.57

Ion-binding properties of the ClC chloride selectivity filter. EMBO J (2005) 1.56

LiGluR restores visual responses in rodent models of inherited blindness. Mol Ther (2011) 1.53

All optical interface for parallel, remote, and spatiotemporal control of neuronal activity. Nano Lett (2007) 1.49

New photochemical tools for controlling neuronal activity. Curr Opin Neurobiol (2009) 1.48

Optical control of metabotropic glutamate receptors. Nat Neurosci (2013) 1.45

Signal Transduction at the Domain Interface of Prokaryotic Pentameric Ligand-Gated Ion Channels. PLoS Biol (2016) 1.42

The structure of the cytoplasmic domain of the chloride channel ClC-Ka reveals a conserved interaction interface. Structure (2007) 1.40

Tuning photochromic ion channel blockers. ACS Chem Neurosci (2011) 1.39

Ligand activation of the prokaryotic pentameric ligand-gated ion channel ELIC. PLoS Biol (2011) 1.37

A structural link between inactivation and block of a K+ channel. Nat Struct Mol Biol (2008) 1.36

Reversibly caged glutamate: a photochromic agonist of ionotropic glutamate receptors. J Am Chem Soc (2007) 1.35

Crystal structure of the cytoplasmic domain of the chloride channel ClC-0. Structure (2006) 1.35

Rapid optical control of nociception with an ion-channel photoswitch. Nat Methods (2012) 1.33

Exploring biosynthetic relationships among furanocembranoids: synthesis of (-)-bipinnatin J, (+)-intricarene, (+)-rubifolide, and (+)-isoepilophodione B. Org Lett (2006) 1.31

Biosynthetic and biomimetic electrocyclizations. Chem Rev (2005) 1.31

Enantioselective Nazarov reactions through catalytic asymmetric proton transfer. J Am Chem Soc (2004) 1.28

A light-gated, potassium-selective glutamate receptor for the optical inhibition of neuronal firing. Nat Neurosci (2010) 1.25

Concise synthesis of (+/-)-rhazinilam through direct coupling. Org Lett (2005) 1.25

A prokaryotic perspective on pentameric ligand-gated ion channel structure. Curr Opin Struct Biol (2009) 1.23

Photochromic blockers of voltage-gated potassium channels. Angew Chem Int Ed Engl (2009) 1.22

Optochemical control of genetically engineered neuronal nicotinic acetylcholine receptors. Nat Chem (2012) 1.21

Engineering light-gated ion channels. Biochemistry (2006) 1.20

Photochemical tools for remote control of ion channels in excitable cells. Nat Chem Biol (2005) 1.17

A versatile and efficient high-throughput cloning tool for structural biology. Biochemistry (2011) 1.17

Total synthesis of (+/-)-rhazinal using novel palladium-catalyzed cyclizations. J Org Chem (2009) 1.14

Nanosculpting reversed wavelength sensitivity into a photoswitchable iGluR. Proc Natl Acad Sci U S A (2009) 1.13

Concise total synthesis of (-)-frondosin B using a novel palladium-catalyzed cyclization. Angew Chem Int Ed Engl (2002) 1.12

Light-induced depolarization of neurons using a modified Shaker K(+) channel and a molecular photoswitch. J Neurophysiol (2006) 1.11

Molecular recognition and self-assembly special feature: Calix[4]arene-based conical-shaped ligands for voltage-dependent potassium channels. Proc Natl Acad Sci U S A (2009) 1.09

The V-ATPase-inhibitor archazolid abrogates tumor metastasis via inhibition of endocytic activation of the Rho-GTPase Rac1. Cancer Res (2012) 1.08

Mode of cell death induction by pharmacological vacuolar H+-ATPase (V-ATPase) inhibition. J Biol Chem (2012) 1.08

Synthetic studies toward the haouamines. Org Lett (2006) 1.07

Efficient Nazarov cyclizations of 2-alkoxy-1,4-pentadien-3-ones. Org Lett (2003) 1.06

Protein surface recognition by rational design: nanomolar ligands for potassium channels. J Am Chem Soc (2003) 1.02

An electrochemical approach to the guanacastepenes. Org Lett (2005) 1.02

Expedient synthesis of (+/-)-bipinnatin J. Org Lett (2006) 1.02

Synthetic studies toward SNF4435 C and SNF4435 D. Org Lett (2002) 1.00

Biomimetic synthesis of elysiapyrones A and B. Org Lett (2005) 0.99

Total synthesis of (-)-archazolid B. J Am Chem Soc (2007) 0.98

A red-shifted, fast-relaxing azobenzene photoswitch for visible light control of an ionotropic glutamate receptor. J Am Chem Soc (2013) 0.98

Label-free microscale thermophoresis discriminates sites and affinity of protein-ligand binding. Angew Chem Int Ed Engl (2012) 0.97

A photochromic agonist of AMPA receptors. Angew Chem Int Ed Engl (2012) 0.97

Total synthesis of (-)-heptemerone B and (-)-guanacastepene E. J Am Chem Soc (2006) 0.97

Extraction of photogenerated electrons and holes from a covalent organic framework integrated heterojunction. J Am Chem Soc (2014) 0.96

Inhibition of the prokaryotic pentameric ligand-gated ion channel ELIC by divalent cations. PLoS Biol (2012) 0.96

Azo-propofols: photochromic potentiators of GABA(A) receptors. Angew Chem Int Ed Engl (2012) 0.95

Polymorphism in an amyloid-like fibril-forming model peptide. Angew Chem Int Ed Engl (2008) 0.95

Mechanistic investigations of the acid-catalyzed cyclization of a vinyl ortho-quinone methide. Chemistry (2008) 0.95

Toward the total synthesis of maoecrystal V: establishment of contiguous quaternary stereocenters. Org Lett (2010) 0.95

Optogenetic photochemical control of designer K+ channels in mammalian neurons. J Neurophysiol (2011) 0.95

A photochromic agonist for μ-opioid receptors. Angew Chem Int Ed Engl (2014) 0.95

Pharmacology of ionotropic glutamate receptors: A structural perspective. Bioorg Med Chem (2010) 0.94

Reductive cyclization of delta-hydroxy nitriles: a new synthesis of glycosylamines. Org Lett (2003) 0.94

Characterization of a diffusible signaling factor from Xylella fastidiosa. MBio (2013) 0.93

Biomimetic synthesis of the shimalactones. Org Lett (2007) 0.93

Biomimetic synthesis of the calcineurin phosphatase inhibitor dibefurin. Angew Chem Int Ed Engl (2014) 0.93

Optical control of acetylcholinesterase with a tacrine switch. Angew Chem Int Ed Engl (2014) 0.92

Biomimetic synthesis of the IDO inhibitors exiguamine A and B. Nat Chem Biol (2008) 0.92

Reversible photomechanical switching of individual engineered molecules at a metallic surface. Phys Rev Lett (2007) 0.91

Synthesis of taiwaniaquinoids via Nazarov triflation. J Am Chem Soc (2006) 0.91

Borane-ammonia complexes stabilized by hydrogen bonding. Org Lett (2002) 0.91

Regulating enzymatic activity with a photoswitchable affinity label. Chembiochem (2008) 0.91

X-ray structure of the C-terminal domain of a prokaryotic cation-chloride cotransporter. Structure (2009) 0.91

Mining the tetraene manifold: total synthesis of complex pyrones from Placobranchus ocellatus. Angew Chem Int Ed Engl (2005) 0.91

Concise total syntheses of variecolortides A and B through an unusual hetero-Diels-Alder reaction. Angew Chem Int Ed Engl (2010) 0.89

ortho-Quinone methides from para-quinones: total synthesis of rubioncolin B. J Am Chem Soc (2008) 0.88

Biomimetic synthesis of (+/-)-pinnatal and (+/-)-sterekunthal A. J Am Chem Soc (2003) 0.88

Concise synthesis of the bacterial DNA primase inhibitor (+) -Sch 642305. Org Lett (2007) 0.87

Biomimetic synthesis of antimalarial naphthoquinones. J Am Chem Soc (2005) 0.86

Total synthesis of (-)-SNF4435 C and (+)-SNF4435 D. Org Lett (2005) 0.85

Biomimetic total synthesis of santalin Y. Angew Chem Int Ed Engl (2015) 0.85

Optical control of calcium-regulated exocytosis. Biochim Biophys Acta (2013) 0.85

Functional characterization of a ClC transporter by solid-supported membrane electrophysiology. J Gen Physiol (2013) 0.85

A Signal Processing Analysis of Purkinje Cells in vitro. Front Neural Circuits (2010) 0.85

Pericyclic reactions of prenylated naphthoquinones: biomimetic syntheses of mollugin and microphyllaquinone. Org Lett (2005) 0.85

Concise Stereoselective Routes to Advanced Intermediates Related to Natural and Unnatural Pinnaic Acid This work was supported by the National Institutes of Health (Grant Numbers: CA28824). Postdoctoral Fellowship support is gratefully acknowledged by M.W.C. (U.S. Army BCRP, DAMD17-98-1-8154), M.F.H. (5T32 CA62948-05), and D.T. (Schering Research Foundation, Berlin). We thank Dr. George Sukenick of the MSKCC NMR Core Facility for NMR and mass spectral analyses. Angew Chem Int Ed Engl (2001) 0.85

An efficient synthesis of loline alkaloids. Nat Chem (2011) 0.85

Total synthesis of (+/-)-photodeoxytridachione through a Lewis acid catalyzed cyclization. Angew Chem Int Ed Engl (2003) 0.84

The total synthesis of (-)-amathaspiramide F. Angew Chem Int Ed Engl (2002) 0.84

Heterocyclic amine directed synthesis of metal(II)-oxalates: investigating the magnetic properties of two complete series of chains with S = 5/2 to S = 1/2. Dalton Trans (2010) 0.83

A zinc phthalocyanine based periodic mesoporous organosilica exhibiting charge transfer to fullerenes. Chemistry (2014) 0.83

Dienophile twisting and substituent effects influence reaction rates of intramolecular Diels-Alder cycloadditions: a DFT study. J Am Chem Soc (2005) 0.82