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PubMed:22033932 JSONTXT 23 Projects

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Id Subject Object Predicate Lexical cue
T1 0-103 Sentence denotes Probing binding pocket of serotonin transporter by single molecular force spectroscopy on living cells.
T2 104-212 Sentence denotes The serotonin transporter (SERT) terminates neurotransmission by removing serotonin from the synaptic cleft.
T3 213-352 Sentence denotes In addition, it is the site of action of antidepressants (which block the transporter) and of amphetamines (which induce substrate efflux).
T4 353-447 Sentence denotes The interaction energies involved in binding of such compounds to the transporter are unknown.
T5 448-625 Sentence denotes Here, we used atomic force microscopy (AFM) to probe single molecular interactions between the serotonin transporter and MFZ2-12 (a potent cocaine analog) in living CHOK1 cells.
T6 626-731 Sentence denotes For the AFM measurements, MFZ2-12 was immobilized on AFM tips by using a heterobifunctional cross-linker.
T7 732-915 Sentence denotes By varying the pulling velocity in force distance cycles drug-transporter complexes were ruptured at different force loadings allowing for mapping of the interaction energy landscape.
T8 916-1207 Sentence denotes We derived chemical rate constants from these recordings and compared them with those inferred from inhibition of transport and ligand binding: koff values were in good agreement with those derived from uptake experiments; in contrast, the kon values were scaled down when determined by AFM.
T9 1208-1321 Sentence denotes Our observations generated new insights into the energy landscape of the interaction between SERT and inhibitors.
T10 1322-1481 Sentence denotes They thus provide a useful framework for molecular dynamics simulations by exploring the range of forces and energies that operate during the binding reaction.