Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist-Reference-Cited by-同舟云学术

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

Published:2010-11-19 Issue:6007 Volume:330 Page:1091-1095
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Chien Ellen Y. T.¹,Liu Wei¹,Zhao Qiang¹,Katritch Vsevolod²,Won Han Gye¹,Hanson Michael A.³,Shi Lei⁴,Newman Amy Hauck⁵,Javitch Jonathan A.⁶,Cherezov Vadim¹,Stevens Raymond C.¹

Affiliation:

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

2. Skaggs School of Pharmacy and Pharmaceutical Sciences, and San Diego Supercomputer Center, University of California, San Diego, La Jolla, CA 92093, USA.

3. Receptos, 10835 Road to the Cure, Suite 205, San Diego, CA 92121, USA.

4. Department of Physiology and Biophysics and HRH Prince Alwaleed Bin Talal Bin Abdulaziz Alsaud Institute for Computational Biomedicine, Weill Cornell Medical College, Cornell University, 1300 York Avenue, New York, NY 10021, USA.

5. Medicinal Chemistry Section, National Institute on Drug Abuse–Intramural Research Program, Baltimore, MD 21224, USA.

6. Center for Molecular Recognition and Departments of Psychiatry and Pharmacology, Columbia University College of Physicians and Surgeons, 630 West 168th, New York, NY 10032, USA.

Abstract

Tweaking Dopamine Reception Dopamine modulates many cognitive and emotional functions of the human brain by activating G protein–coupled receptors. Antipsychotic drugs that block two of the receptor subtypes are used to treat schizophrenia but have multiple side effects. Chien et al. (p. 1091 ; see the Research Article by Wu et al. ) resolved the crystal structure of one receptor in complex with a small-molecule inhibitor at 3.15 angstrom resolution. Homology modeling with other receptor subtypes might be a promising route to reveal potential structural differences that can be exploited in the design of selective therapeutic inhibitors having fewer side effects.

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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