The molecular basis of the structure and function of the 5-HT3 receptor: A model ligand-gated ion channel (review)

Molecular Membrane Biology

Volumn 19, Issue 1, 2002, Pages 11-26

  Reeves, David C ^a   Lummis, Sarah C R ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

5 hydroxytryptamine3 receptor; Allosteric gating; Desensitization; Ligand gated ion channel; Permeability; Selectivity; Serotonin3 receptor

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; GLYCINE RECEPTOR; NEUROTRANSMITTER RECEPTOR; NICOTINIC RECEPTOR; SEROTONIN 3 RECEPTOR;

AGONIST; ALLOSTERISM; BINDING AFFINITY; BINDING SITE; CHANNEL GATING; EXTRACELLULAR SPACE; ION TRANSPORT; LIGAND BINDING; MODULATION; MOLECULAR CLONING; MOLECULAR RECOGNITION; NERVE CONDUCTION; NEUROTRANSMISSION; POROSITY; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN QUATERNARY STRUCTURE; PROTEIN SECONDARY STRUCTURE; PROTEIN STRUCTURE; PROTEIN TERTIARY STRUCTURE; REVIEW; SYNAPSE; TRANSPORT KINETICS;

ALLOSTERIC REGULATION; AMINO ACID SEQUENCE; ANIMALS; CALCIUM CHANNEL BLOCKERS; CATIONS; HUMANS; ION CHANNEL GATING; ION CHANNELS; LIGANDS; MICE; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; PROTEIN SUBUNITS; RATS; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT3; SEQUENCE ALIGNMENT; SEQUENCE HOMOLOGY, AMINO ACID; SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; STEROIDS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0036117729     PISSN: 09687688     EISSN: None     Source Type: Journal    
DOI: 10.1080/09687680110110048     Document Type: Review

References (201)

1. The permeability of endplate channels to monovalent and divalent metal cations
2. Identification of acetylcholine receptor channel-lining residues in the entire M2 segment of the α-subunit
3. Acetylcholine receptor channel structure probed in cysteine-substitution mutants
4. Inorganic, monovalent cations compete with agonists for the transmitter binding site of nicotinic acetylcholine receptors
5. A receptor needs two homologous domains of the beta-subunit for activation by GABA but not by pentobarbital
6. Ion permeation mechanism of the potassium channel
7. Role of local anesthetics on both cholinergic and serotonergic ionotropic receptors
8. 3 receptors in outside-out patches of N1E-115 neuroblastoma cells: Basic properties and effects of pentobarbital
9. 3 receptor of N1E-115 neuroblastoma cells
10. 3 receptor-mediated 14C-guanidinium influx in N1E-115 neuroblastoma cells
11. A review of central 5-HT receptors and their function
12. 3 receptor in mammalian NG108-15 cells
13. Mutations at two distinct sites within the channel domain M2 alter calcium permeability of neuronal α7 nicotinic receptor
14. 5-Hydroxytryptamine interaction with the nicotinic acetylcholine receptor
15. 3 receptor production with the Semliki forest virus expression system
16. 3 receptor
17. 3 receptors in NG108-15 neuroblastoma x glioma cells: Effect of the novel agonist 1-(m-chlorophenyl)-biguanide
18. 3 receptor using site directed mutagenesis: Importance of glutamate 106
19. Can thermodynamic measurements of receptor binding yield information on drug affinity and efficacy?
20. Assigning functions to residues in the acetylcholine receptor channel region
21. Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine
22. 3A/ receptors
23. 3 receptor
24. Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors
25. 3A)
26. 3A receptor isoforms
27. Neurosteroids modulate nicotinic receptor function in mouse striatal and thalamic synaptosomes
28. Association of two 3D QSAR analyses. Application to the study of partial agonist serotonin-3 ligands
29. Nicotinic receptors and brain plasticity
30. + permeability ratios of nicotinic acetylcholine receptors are reduced by mutations near the intracellular end of the M2 region
31. Mutational analysis of the charge selectivity filter of the alpha-7 nicotinic acetylcholine receptor
32. Nicotinic receptors at the amino acid level
33. Competitive antagonism of the mouse 5-hydroxytryptamine(3) receptor by bisindolylmaleimide I, a 'selective' protein kinase C inhibitor
34. Structural features of the pore lining M2 transmembrane segment of the serotonin-gated ion channel
35. Probing the role of a conserved M1 proline residue in 5-hydroxytryptamine(3) receptor gating
36. 3B subunit is a major determinant of serotonin-receptor function
37. 3 receptor
38. 3 receptors are membrane ion channels
39. 3R-A subunit expressed in Xenopus laevis oocytes
40. + conduction and selectivity
41. 3B receptor subunit
42. Allosteric transitions of the acetylcholine receptor
43. Chimaeric nicotinic-serotonergic receptor combines distinct ligand binding and channel specificities
44. Backbone mutations in transmembrane domains of a ligand-gated ion channel: Implications for the mechanism of gating
45. Effects of cocaine on the serotonin-induced inward current in rat nodose ganglion neurons
46. The role of conserved leucines in the M2 domain of the acetylcholine receptor in channel gating
47. 3 receptors do not contain nicotinic acetylcholine receptor subunits
48. A discrete site for general anesthetics on a postsynaptic receptor
49. Molecular and cellular mechanisms of general anesthesia
50. Two kinds of tryptamine receptor
51. Neurotransmitter-gated ion channels as unconventional allosteric proteins
52. Neuronal nicotinic receptors: Molecular organization and regulations
53. Identification of calcium binding sites that regulate potentiation of a neuronal nicotinic acetylcholine receptor
54. Mutations in the channel domain of a neuronal nicotinic receptor convert ion selectivity from cationic to anionic
55. 3 receptor stably expressed in HEK 293 cells
56. 2+ levels
57. 3 receptor splice variants isolated from a mouse hippocampal cell line
58. The transmembrane domains of the nicotinic acetylcholine receptor contain α-helical and α structures
59. Predicted structure of the extracellular region of ligand-gated ion-channel receptors shows SH2-like and SH3-like domains forming the ligand-binding site
60. 3 receptors provides new insights into their maturation and structure
61. 3 receptor antagonists. Clinical pharmacology and therapeutic applications
62. Mapping the conformational wave of acetylcholine receptor channel gating
63. Nicotinic receptors in wonderland
64. 3 receptors
65. 3A receptor from cationic to anionic reveals a conserved feature of the ligand-gated ion channel superfamily
66. 3A receptors
67. 3 receptors expressed in Xenopus oocytes
68. 3 receptors in rodents
69. 2+ channels
70. Ca2+ permeability of cloned and native 5-hydroxytryptamine type 3 receptors
71. Inefficient cell-surface expression of hybrid complexes formed by the co-assembly of neuronal nicotinic acetylcholine receptor and serotonin receptor subunits
72. 3A receptor subunits
73. 3 receptor A subunit
74. Protein mobility and GABA-induced conformational changes in GABA(A) receptor pore-lining M2 segment
75. 5-HT receptor classification and nomenclature: Towards a harmonization with the human genome
76. 3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding
77. 3 receptor is modulated by divalent cations
78. 3 receptor antagonists in the treatment of irritable bowel syndrome
79. Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance
80. 3 receptor channel
81. 3 receptors in N1E-115 neuroblastoma cells
82. 3 receptor reveals species-specific sensitivity to curare antagonism
83. 3 receptor channel desensitisation in rat glioma x mouse neuroblastoma hybrid NG108-15 cells
84. Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins
85. M2 pore mutations convert the glycine receptor channel from being anion- to cation-selective
86. Dynamic selectivity filters in ion channels
87. Conductance mutations of the nicotinic acetylcholine receptor do not act by a simple electrostatic mechanism
88. 3 receptor-mediated ion current in N1E-115 neuroblastoma cells
89. 3 receptor-mediated ion current at the agonist recognition site and prevent desensitization in cultured mouse neuroblastoma cells
90. Acetylcholine receptor gating is influenced by the polarity of amino acids at position 9′ in the M2 domain
91. 3 receptor subunit
92. Channel gating governed symmetrically by conserved leucine residues in the M2 domain of nicotinic receptors
93. 3 receptors in clonal cell lines studied by patch-clamp techniques
94. 3) receptor expressed in HEK293 cells
95. 3 receptor cDNA and its splice variants from guinea pig
96. Molecular evolution of the nicotinic acetylcholine-receptor - An example of multigene family in excitable cells
97. LGICdb: The ligand-gated ion channel database
98. Structure of ligand-gated ion channels: Critical assessment of biochemical data supports novel topology
99. Coupled proteolytic and mass spectrometry studies indicate a novel topology for the glycine receptor
100. A single amino-acid in the TM1 domain is an important determinant of the desensitization kinetics of recombinant human and guinea pig alpha-homomeric 5-hydroxytryptamine type 3 receptors
101. 3 receptor-mediated ion current by divalent metal cations in NCB-20 neuroblastoma cells
102. 3 receptors and the neural actions of alcohols: An increasingly exciting topic
103. 3 receptors
104. Building new function into glycine receptors: A structural model for the activation of the glycine-gated chloride channel
105. Identification of intracellular and extracellular domains mediating signal transduction in the inhibitory glycine receptor chloride channel
106. A receptor channels
107. 3 receptors expressed in Xenopus laevis oocytes
108. 3 serotonin receptor ligands
109. 3 receptors - A patchclamp study
110. 3 receptor, a serotonin-gated ion channel
111. 3 receptor
112. 3 receptor
113. 3 receptor extracellular domain: Search for ligand binding sites
114. Structure of the pore-farming transmembrane domain of a ligand-gated ion channel
115. Sites of alcohol and volatile anaesthetic action on GABA(A) and glycine receptors
116. 3 receptor splice variants in the rat
117. 3 receptor: Heterogeneity in distribution and function among species
118. Nicotinic acetylcholine receptor at 4.6 Å resolution: Transverse tunnels in the channel wall
119. 3 receptors
120. 3 receptor transiently expressed in HEK 293 cells
121. 3 receptor subunit
122. 3 receptor subunits A and B in the dorsal root ganglion
123. 3A serotonin receptors depends on subunit occupancy
124. 3 receptors by functional epitope tagging
125. Calcium changes induced by presynaptic 5-hydroxytryptamine-3 serotonin receptors on isolated terminals from various regions of the rat brain
126. 3 receptor-mediated electrical response in cultured mouse neuroblastoma cells
127. 3 receptor-induced increases in calcium levels in individual brain nerve terminals
128. 3 receptor splice variants: The role of the extra six amino acid segment
129. 3A receptor
130. Ligand- and voltage-gated ion channels
131. Monovalent and divalent-cation permeability and block of neuronal nicotinic receptor channels in rat parasympathetic ganglia
132. Evolutionary history of the ligand-gated ion-channel superfamily of receptors
133. 3 receptors: Focus on alcohols and anaesthetic agents
134. State-dependent accessibility and electrostatic potential in the channel of the acetylcholine receptor. Inferences from rates of reaction of thiosulfonates with substituted cysteines in the M2 segment of the alpha subunit
135. Spatial structure of the M2 transmembrane segment of the nicotinic acetylcholine receptor alpha-subunit
136. 3 receptor-induced currents in N1E-115 neuroblastoma cells
137. 3 receptors
138. 3 receptors
139. 3B receptor subunits in mammalian retinae: Potential pre-synaptic modulators of photoreceptors
140. 3 receptors
141. 3 receptor
142. Startle disease mutations reduce the agonist sensitivity of the human inhibitory glycine receptor
143. MOD-1 is a serotonin-gated chloride channel that modulates locomotory behaviour in C. elegans
144. Serum vasoconstrictor (Serotonin) V. The presence of creatinine in the complex. A proposed structure of the vasoconstrictor priciple
145. Purification of the substance which is responsible for vasoconstrictor activity of serum
146. Serum vasoconstrictor (Serotonin) IV. Isolation and characterization
147. Partial purification of the vasoconstrictor in beef serum
148. Serum vasoconstrictor (Serotonin) III. Chemical inactivation
149. Crystalline serotonin
150. 3A receptors
151. 3 receptor pore revealed by substituted cysteine accessibility mutagenesis
152. Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor
153. 3H]chlorpromazine labels three amino acids of the acetylcholine receptor α-subunit: Implications for the α-helical organization of regions MII and for the structure of the ion channel
154. An initial three-component pharmacophore for specific serotonin-3 receptor ligands
155. 3 receptor-gated currents in adult-rat dorsal-root ganglion neurons
156. 3 receptors induce rises in cytosolic and nuclear calcium in NG108-15 cells via calcium-induced calcium release
157. Mutation of glycine receptor subunit creates beta-alanine receptor responsive to GABA
158. 3 receptors in N1E-115 neuroblastoma cells
159. Acetylcholine-receptors - Too many channels, too few functions
160. The role of tryptophan residues in the 5-Hydroxytryptamine(3) receptor ligand binding domain
161. 3 receptor label both native and recombinant receptors (vol 67, pg 221, 1999)
162. Importance of phenylalanine 107 in agonist recognition by the 5-hydroxytryptamine(3A) receptor
163. 3 receptor
164. 3A and alpha 2 glycine receptors expressed in Xenopus oocytes
165. 5-HT(3) receptor function and potentiation by alcohols in frontal cortex neurons from transgenic mice overexpressing the receptor
166. Electrophysiological characterization of functionally distinct 5-hydroxytryptamine receptors on guinea-pig submucous plexus
167. Serotonin increases cytoplasmic Ca2+ concentration in PC12 cells: Effect of tachykinin peptides
168. Pharmacological analysis of intracellular Ca2+ signalling: Problems and pitfalls
169. Kinked-helices model of the nicotinic acetylcholine receptor ion channel and its complexes with blockers: Simulation by the Monte Carlo minimization method
170. Evolution of nicotinic acetylcholine receptor subunits
171. Pharmacological and anti-emetic properties of ondansetron
172. 3 receptor gene and assignment to human chromosome 11
173. Nicotinic acetylcholine receptor at 9 Å resolution
174. Acetylcholine receptor channel imaged in the open state
175. Projection structure of the nicotinic acetylcholine receptor: Distinct conformations of the alpha subunits
176. The nicotinic acetylcholine receptor of the Torpedo electric ray
177. Nicotinic acetylcholine receptor: Structure and mechanism
178. The Croonian Lecture 2000. Nicotinic acetylcholine receptor and the structural basis of fast synaptic transmission
179. Progesterone modulates a neuronal nicotinic acetylcholine-receptor
180. 3 receptor ligand-gated ion channels
181. 3 receptors and neurotransmitter release in the CNS: A nerve ending story?
182. 3 and nicotinic α4 receptor subunits into Ca(2+)-permeable ion channels
183. 3 receptor-mediated ion current in N1E-115 neuroblastoma cells by 5-hydroxyindole and analogues
184. Distinct agonist- and antagonist-binding sites on the glycine receptor
185. 3 receptor gene and functional expression of two splice variants
186. Functional antagonism of gonadal steroids at the 5-hydroxytryptamine type 3 receptor
187. Gamma-aminobutyric acid increases the water accessibility of M3 membrane-spanning segment residues in gamma-aminobutyric acid type A receptors
188. The location of the gate in the acetylcholine receptor channel
189. Inverse modulation of gamma-aminobutyric acid-induced and glycine-induced currents by progesterone
190. A receptor α1 subunit
191. 3 receptors mediate rapid responses in cultured hippocampus and a clonal cell line
192. Single amino acid substitution affects desensitization of the 5-hydroxytryptamine type 3 receptor expressed in Xenopus oocytes
193. 3 receptor
194. 3 receptor in a rat glioma x mouse neuroblastoma hybrid cell
195. 3 receptor
196. Ion permeation through 5-hydroxytryptamine-gated channels in neuroblastoma N18 cells
197. 3 receptor channels in dissociated rat superior cervical ganglion neurons
198. Ondansetron modulates GABA(A) current of rat central nervous system neurons
199. 3 receptors expressed in Xenopus oocytes
200. 3 receptor-channels on NCB-20 neuroblastoma cells by favouring and stabilizing the open channel state