CHAPTER 16: Allosteric Binding in the Serotonin Transporter – Pharmacology, Structure, Function and Potential Use as a Novel Drug Target Check Access
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Published:18 Nov 2016
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Special Collection: 2016 ebook collectionSeries: Drug Discovery Series
C. J. Loland, C. Sanchez, P. Plenge, K. P. Bøgesø, and B. Bang-Andersen, in Allosterism in Drug Discovery, ed. D. Doller, The Royal Society of Chemistry, 2016, pp. 360-380.
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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.
