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PubMed:27645992 JSONTXT

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sentences

Id Subject Object Predicate Lexical cue
T1 0-121 Sentence denotes Unorthodox Acetylcholine Binding Sites Formed by α5 and β3 Accessory Subunits in α4β2* Nicotinic Acetylcholine Receptors.
T2 122-304 Sentence denotes All nicotinic acetylcholine receptors (nAChRs) evolved from homomeric nAChRs in which all five subunits are involved in forming acetylcholine (ACh) binding sites at their interfaces.
T3 305-725 Sentence denotes Heteromeric α4β2* nAChRs typically have two ACh binding sites at α4/β2 interfaces and a fifth accessory subunit surrounding the central cation channel. β2 accessory subunits do not form ACh binding sites, but α4 accessory subunits do at the α4/α4 interface in (α4β2)2α4 nAChRs. α5 and β3 are closely related subunits that had been thought to act only as accessory subunits and not take part in forming ACh binding sites.
T4 726-930 Sentence denotes The effect of agonists at various subunit interfaces was determined by blocking homologous sites at these interfaces using the thioreactive agent 2-((trimethylammonium)ethyl) methanethiosulfonate (MTSET).
T5 931-1031 Sentence denotes We found that α5/α4 and β3/α4 interfaces formed ACh binding sites in (α4β2)2α5 and (α4β2)2β3 nAChRs.
T6 1032-1104 Sentence denotes The α4/α5 interface in (β2α4)2α5 nAChRs also formed an ACh binding site.
T7 1105-1207 Sentence denotes Blocking of these sites with MTSET reduced the maximal ACh evoked responses of these nAChRs by 30-50%.
T8 1208-1376 Sentence denotes However, site-selective agonists NS9283 (for the α4/α4 site) and sazetidine-A (for the α4/β2 site) did not act on the ACh sites formed by the α5/α4 or β3/α4 interfaces.
T9 1377-1473 Sentence denotes This suggests that unorthodox sites formed by α5 and β3 subunits have unique ligand selectivity.
T10 1474-1642 Sentence denotes Agonists or antagonists for these unorthodox sites might be selective and effective drugs for modulating nAChR function to treat nicotine addiction and other disorders.