Allosteric Binding in the Serotonin Transporter - Pharmacology, Structure, Function and Potential Use as a Novel Drug Target

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The serotonin transporter (SERT) is an important drug target and the majority of currently used antidepressants are potent inhibitors of SERT, binding primarily to the substrate binding site. However, even though the existence of an allosteric modulator site was realized more than 30 years ago, the research into this mechanism is still in its early days. The current knowledge about the allosteric site with respect to pharmacology, structure and function, and pharmacological tool compounds, is reviewed and a perspective is given on its potential as a drug target.

Original languageEnglish
Title of host publicationAllosterism in Drug Discovery
Number of pages21
PublisherRoyal Society of Chemistry
Publication date2017
ISBN (Print)978-1-78262-459-2
ISBN (Electronic)978-1-78262-969-6
Publication statusPublished - 2017
SeriesRSC Drug Discovery Series

ID: 188452966