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Steric Hindrance Mutagenesis in the Conserved Extracellular Vestibule Impedes Allosteric Binding of Antidepressants to the Serotonin Transporter

The serotonin transporter (SERT) controls synaptic serotonin levels and is the primary target for antidepressants, including selective serotonin reuptake inhibitors (e.g. (S)-citalopram) and tricyclic antidepressants (e.g. clomipramine). In addition to a high affinity binding site, SERT possesses a...

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Autors principals: Plenge, Per, Shi, Lei, Beuming, Thijs, Te, Jerez, Newman, Amy Hauck, Weinstein, Harel, Gether, Ulrik, Loland, Claus J.
Format: Artigo
Idioma:Inglês
Publicat: American Society for Biochemistry and Molecular Biology 2012
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC3501018/
https://ncbi.nlm.nih.gov/pubmed/23007398
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.M112.371765
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