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

Claus J. Loland, Connie Sanchez, Per Plenge, Klaus P. Bøgesø, Benny Bang-Andersen

Abstract

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.

OriginalsprogEngelsk
TitelAllosterism in Drug Discovery
Antal sider21
ForlagRoyal Society of Chemistry
Publikationsdato2017
Sider360-380
Kapitel16
ISBN (Trykt)978-1-78262-459-2
ISBN (Elektronisk)978-1-78262-969-6
DOI
StatusUdgivet - 2017
NavnRSC Drug Discovery Series
Nummer56
ISSN2041-3203

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