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Crystal structures of serotonin (5-HT) receptor-bound agonists

Crystal structures of agonists bound to 5-HT receptors could aid the development of new compounds selective for 5-HT receptor subtypes. The crystal structures of serotonin (5-HT1B) receptor and serotonin (5-HT2B) receptor bound to ergotamine and dihydroergotamine showed that the small molecules occupy an orthosteric binding pocket on the receptors. Biochemical studies showed that ergotamine preferentially activated noncanonical arrestin-b signaling pathways at 5-HT2B. Next steps include using the crystal structure data to aid the design of compounds specific for different 5-HT receptor subtypes.
Ergotamine and dihydroergotamine are both generic migraine drugs.

SciBX 6(13); doi:10.1038/scibx.2013.321
Published online April 4, 2013

Findings from both studies unpatented; licensing status not applicable

Wang, C. et al. Science;
published online March 21, 2013;
doi:10.1126/science.1232807
Contact: H. Eric Xu, Chinese Academy of Sciences, Shanghai, China
e-mail:
eric.xu@vai.org
Contact: Raymond C. Stevens,
The Scripps Research Institute, La Jolla, Calif.
e-mail:
stevens@scripps.edu

Wacker, D. et al. Science;
published online March 21, 2013;
doi:10.1126/science.1232808
Contact: Bryan L. Roth, The University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, N.C.
e-mail:
bryan_roth@med.unc.edu
Contact: Raymond C. Stevens,
The Scripps Research Institute, La Jolla, Calif.
e-mail:
stevens@scripps.edu