Allosteric Binding in the Serotonin Transporter - Pharmacology, Structure, Function and Potential Use as a Novel Drug Target
Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Allosteric Binding in the Serotonin Transporter - Pharmacology, Structure, Function and Potential Use as a Novel Drug Target. / Loland, Claus J.; Sanchez, Connie; Plenge, Per; Bøgesø, Klaus P.; Bang-Andersen, Benny.
Allosterism in Drug Discovery. Royal Society of Chemistry, 2017. p. 360-380 (RSC Drug Discovery Series; No. 56).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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TY - CHAP
T1 - Allosteric Binding in the Serotonin Transporter - Pharmacology, Structure, Function and Potential Use as a Novel Drug Target
AU - Loland, Claus J.
AU - Sanchez, Connie
AU - Plenge, Per
AU - Bøgesø, Klaus P.
AU - Bang-Andersen, Benny
PY - 2017
Y1 - 2017
N2 - 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.
AB - 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.
U2 - 10.1039/9781782629276-00360
DO - 10.1039/9781782629276-00360
M3 - Book chapter
AN - SCOPUS:85006355217
SN - 978-1-78262-459-2
T3 - RSC Drug Discovery Series
SP - 360
EP - 380
BT - Allosterism in Drug Discovery
PB - Royal Society of Chemistry
ER -
ID: 188452966