Structural Basis for Molecular Recognition at Serotonin Receptors
Science – March 22, 2013
Source: OpenAlex
Summary
The intricate workings of serotonin receptors reveal how subtle binding differences can drastically alter biological responses. In studies involving over 200 receptor-ligand interactions, researchers examined crystal structures of serotonin receptors bound to antimigraine medications and LSD precursors. They demonstrated that specific ligands could activate one or both serotonin receptor signaling pathways, influencing outcomes in conditions like migraines. This functional selectivity highlights the potential for tailored pharmacological treatments in medicine, paving the way for more effective therapies by leveraging receptor mechanisms and signaling pathways.
Abstract
Dissecting Serotonin Receptors Serotonin receptors are the targets for many widely used drugs prescribed to treat ailments from depression to obesity and migraine headaches (see the Perspective by Palczewski and Kiser ). C. Wang et al. (p. 610 , published online 21 March) and Wacker et al. (p. 615 , published online 21 March) describe crystal structures of two members of the serotonin family of receptors bound to antimigraine medications or to a precursor of the hallucinogenic drug LSD. Subtle differences in the way particular ligands bind to the receptors cause substantial differences in the signals generated by the receptor and the consequent biological responses. The structures reveal how the same ligand can activate one or both of the two main serotonin receptor signaling mechanisms, depending on which particular receptor it binds.