Cover image for Vol. 11 Issue 12

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.968

ISI Journal Citation Reports © Ranking: 2014: 19/59 (Chemistry Medicinal); 83/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

July 28, 2011

VIP: (S)- and (R)-Fluoxetine as Native Markers in MS Binding Assays Addressing the Serotonin Transporter

VIP: (S)- and (R)-Fluoxetine as Native Markers in MS Binding Assays Addressing the Serotonin TransporterMarielle Hess, Georg Höfner, and Klaus Theodor Wanner*

MS binding assays are a highly versatile technique in the drug discovery process to characterize the affinity of a ligand for a target. This label-free screening approach offers all the advantages of conventional and widely accepted radioligand binding assays without such drawbacks as the need for labeling and the handling of hazardous radioactive material. The concept of MS binding assays was recently introduced by the research group of Klaus T. Wanner at the Ludwig Maximilians University of Munich in Germany.

In this work, the team focused on implementing this approach to the serotonin transporter (SERT). As SERT regulates levels of serotonin (5-HT) in the synaptic cleft, it is the primary target in the treatment of emotional disorders such as depression, obsessive–compulsive disorder, and anxiety. The search for SERT inhibitors for the development of new drugs with improved therapeutic profile is of great importance.

Wanner and co-workers demonstrated the feasibility of SERT MS binding assays by using (S)-fluoxetine as native (non-labeled) marker. The results obtained in saturation, kinetic, and competitive experiments are in good agreement with corresponding radioligand binding assays. Hence, the developed label-free binding assay is an easy way to characterize potential inhibitors for their affinity toward SERT in screening campaigns.

Received May 19, 2011; published online July 26, 2011, DOI: 10.1002/cmdc.201100251.

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