Editors' ChoicePharmacology

Dissecting Serotonin Receptors

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Science Signaling  07 May 2013:
Vol. 6, Issue 274, pp. ec102
DOI: 10.1126/scisignal.2004304

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). Wang et al. and Wacker et al. 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.

C. Wang, Y. Jiang, J. Ma, H. Wu, D. Wacker, V. Katritch, G. W. Han, W. Liu, X.-P. Huang, E. Vardy, J. D. McCorvy, X. Gao, X. E. Zhou, K. Melcher, C. Zhang, F. Bai, H. Yang, L. Yang, H. Jiang, B. L. Roth, V. Cherezov, R. C. Stevens, H. E. Xu, Structural basis for molecular recognition at serotonin receptors. Science 340, 610–614 (2013). [Abstract] [Full Text]

D. Wacker, C. Wang, V. Katritch, G. W. Han, X.-P. Huang, E. Vardy, J. D. McCorvy, Y. Jiang, M. Chu, F. Y. Siu, W. Liu, H. E. Xu, V. Cherezov, B. L. Roth, R. C. Stevens, Structural features for functional selectivity at serotonin receptors. Science 340, 615–619 (2013). [Abstract] [Full Text]

K. Palczewski, P. D. Kiser, As good as chocolate. Science 340, 562–563 (2013). [Abstract] [Full Text]

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