Depression, obsessive-compulsive disorder, anxiety and stress are often linked to disturbances in the metabolism of the neurotransmitter serotonin.
Neurotransmitters are the buses that take messages from brain cell to brain cell. Technically, they are compounds released from the synapses at nerve cell endings and they activate the firing of the neighboring neuron in order to mediate the transmission of nerve impulses. The serotonin transporter (SERT) is responsible for the reuptake of the transmitter into neurons which terminates the action. SERT is the target for most drugs used to treat depression, ocd, and anxiety. The search for new and better inhibitors is always in play.
And the latest approach comes from a team led by Professor Klaus Wanner of the Department of Pharmacy in the Center for Pharmaceutical Research at Ludwig-Maximilians Universitat Munchen (LMU). It is a new binding assay based on the use of mass spectrometry (MS). It promises to simplify the search for potential SERT inhibitors.
Most drugs need to bind selectively to defined molecular targets. The target may be an enzyme found in certain cells or a protein found on a particular cell type. Drug candidates are measured on their ability to find and bind with a target. The ability of a test substance to interact with its target is measure din terms of how well it competes with a marker on the target cell. The greater the ability to bump the marker off the target cell, the better the effectiveness of the drug.
Wanner’s breakthrough is going to make it easier to test drugs because the marker cells do have to be marked radioactively as was previously necessary. “This label-free technique provides all the advantages offered y classical binding studies, while avoiding the need to work with radioactive compounds.” They will use his new technique in a study for a new SSRI compound. “Because SERT regulates the concentration of serotonin in the synaptic cleft, the protein serves as the major target for the treatment of depression, obsessive-compulsive disorders and anxiety states. The breakthrough may work for other types of cells as well.
Source: MedicalNewsToday, ChemMedChem
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