RDF/XMLNTriplesTurtleShow queryShare
SubjectPredicateObject
http://purl.uniprot.org/citations/19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/19620239http://www.w3.org/2000/01/rdf-schema#comment"Nicotinic acetylcholine receptor (nAChR) agonists, such as epibatidine and its molecular derivatives, are potential therapeutic agents for a variety of neurological disorders. In order to identify determinants for subtype-selective agonist binding, it is important to determine whether an agonist binds in a common orientation in different nAChR subtypes. To compare the mode of binding of epibatidine in a muscle and a neuronal nAChR, we photolabeled Torpedo alpha(2)betagammadelta and expressed human alpha4beta2 nAChRs with [(3)H]epibatidine and identified by Edman degradation the photolabeled amino acids. Irradiation at 254 nm resulted in photolabeling of alphaTyr(198) in agonist binding site Segment C of the principal (+) face in both alpha subunits and of gammaLeu(109) and gammaTyr(117) in Segment E of the complementary (-) face, with no labeling detected in the delta subunit. For affinity-purified alpha4beta2 nAChRs, [(3)H]epibatidine photolabeled alpha4Tyr(195) (equivalent to Torpedo alphaTyr(190)) in Segment C as well as beta2Val(111) and beta2Ser(113) in Segment E (equivalent to Torpedo gammaLeu(109) and gammaTyr(111), respectively). Consideration of the location of the photolabeled amino acids in homology models of the nAChRs based upon the acetylcholine-binding protein structure and the results of ligand docking simulations suggests that epibatidine binds in a single preferred orientation within the alpha-gamma transmitter binding site, whereas it binds in two distinct orientations in the alpha4beta2 nAChR."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.org/dc/terms/identifier"doi:10.1074/jbc.m109.019083"xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/author"Srivastava S."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/author"Blanton M.P."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/author"Cohen J.B."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/author"Duddempudi P.K."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/author"Hamouda A.K."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/author"Pandhare A."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/author"Sanghvi M."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/date"2009"xsd:gYear
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/name"J Biol Chem"xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/pages"24939-24947"xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/title"[(3)H]Epibatidine photolabels non-equivalent amino acids in the agonist binding site of Torpedo and alpha4beta2 nicotinic acetylcholine receptors."xsd:string
http://purl.uniprot.org/citations/19620239http://purl.uniprot.org/core/volume"284"xsd:string
http://purl.uniprot.org/citations/19620239http://www.w3.org/2004/02/skos/core#exactMatchhttp://purl.uniprot.org/pubmed/19620239
http://purl.uniprot.org/citations/19620239http://xmlns.com/foaf/0.1/primaryTopicOfhttps://pubmed.ncbi.nlm.nih.gov/19620239
http://purl.uniprot.org/uniprot/#_B4DK78-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239
http://purl.uniprot.org/uniprot/#_P43681-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239
http://purl.uniprot.org/uniprot/#_Q4VAQ3-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239
http://purl.uniprot.org/uniprot/#_Q5EIU9-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239
http://purl.uniprot.org/uniprot/#_Q5EIV0-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239
http://purl.uniprot.org/uniprot/#_P17787-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239
http://purl.uniprot.org/uniprot/#_Q59FV0-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239
http://purl.uniprot.org/uniprot/#_Q5RLM1-mappedCitation-19620239http://www.w3.org/1999/02/22-rdf-syntax-ns#objecthttp://purl.uniprot.org/citations/19620239