Structural Features for Functional Selectivity at Serotonin Receptors

Author:

Wacker Daniel1,Wang Chong1,Katritch Vsevolod1,Han Gye Won1,Huang Xi-Ping2,Vardy Eyal2,McCorvy John D.2,Jiang Yi13,Chu Meihua1,Siu Fai Yiu1,Liu Wei1,Xu H. Eric34,Cherezov Vadim1,Roth Bryan L.2,Stevens Raymond C.1

Affiliation:

1. Department of Integrative Structural and Computational Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

2. National Institute of Mental Health Psychoactive Drug Screening Program, Department of Pharmacology and Division of Chemical Biology and Medicinal Chemistry, University of North Carolina Chapel Hill Medical School, Chapel Hill, NC 27599, USA.

3. Van Andel Research Institute/Shanghai Institute of Materia Medica Center, CAS-Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.

4. Laboratory of Structural Sciences, Van Andel Research Institute, 333 Bostwick Ave NE, Grand Rapids, MI 49503, USA.

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.

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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