Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands

The D2 dopamine receptor (DRD2) is one of the most well-established therapeutic targets for neuropsychiatric and endocrine disorders. Here, the authors report the crystal structure of the antipsychotic drug haloperidol bound to DRD2 via an extended binding pocket that distinguishes it from other D2-...

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Main Authors:	Luyu Fan, Liang Tan, Zhangcheng Chen, Jianzhong Qi, Fen Nie, Zhipu Luo, Jianjun Cheng, Sheng Wang
Format:	Article
Language:	English
Published:	Nature Publishing Group 2020-02-01
Series:	Nature Communications
Online Access:	https://doi.org/10.1038/s41467-020-14884-y

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spelling	doaj-1936baecc46a4ba180565c58eeea11872021-05-11T08:49:22ZengNature Publishing GroupNature Communications2041-17232020-02-0111111110.1038/s41467-020-14884-yHaloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligandsLuyu Fan0Liang Tan1Zhangcheng Chen2Jianzhong Qi3Fen Nie4Zhipu Luo5Jianjun Cheng6Sheng Wang7State Key Laboratory of Molecular Biology, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Biochemistry and Cell Biology, Chinese Academy of Sciences, University of Chinese Academy of SciencesiHuman Institute, ShanghaiTech UniversityState Key Laboratory of Molecular Biology, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Biochemistry and Cell Biology, Chinese Academy of Sciences, University of Chinese Academy of SciencesState Key Laboratory of Molecular Biology, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Biochemistry and Cell Biology, Chinese Academy of Sciences, University of Chinese Academy of SciencesState Key Laboratory of Molecular Biology, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Biochemistry and Cell Biology, Chinese Academy of Sciences, University of Chinese Academy of SciencesInstitute of Molecular Enzymology, Soochow UniversityiHuman Institute, ShanghaiTech UniversityState Key Laboratory of Molecular Biology, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Biochemistry and Cell Biology, Chinese Academy of Sciences, University of Chinese Academy of SciencesThe D2 dopamine receptor (DRD2) is one of the most well-established therapeutic targets for neuropsychiatric and endocrine disorders. Here, the authors report the crystal structure of the antipsychotic drug haloperidol bound to DRD2 via an extended binding pocket that distinguishes it from other D2-like subtypes.https://doi.org/10.1038/s41467-020-14884-y
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Luyu Fan Liang Tan Zhangcheng Chen Jianzhong Qi Fen Nie Zhipu Luo Jianjun Cheng Sheng Wang
spellingShingle	Luyu Fan Liang Tan Zhangcheng Chen Jianzhong Qi Fen Nie Zhipu Luo Jianjun Cheng Sheng Wang Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands Nature Communications
author_facet	Luyu Fan Liang Tan Zhangcheng Chen Jianzhong Qi Fen Nie Zhipu Luo Jianjun Cheng Sheng Wang
author_sort	Luyu Fan
title	Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands
title_short	Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands
title_full	Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands
title_fullStr	Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands
title_full_unstemmed	Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands
title_sort	haloperidol bound d2 dopamine receptor structure inspired the discovery of subtype selective ligands
publisher	Nature Publishing Group
series	Nature Communications
issn	2041-1723
publishDate	2020-02-01
description	The D2 dopamine receptor (DRD2) is one of the most well-established therapeutic targets for neuropsychiatric and endocrine disorders. Here, the authors report the crystal structure of the antipsychotic drug haloperidol bound to DRD2 via an extended binding pocket that distinguishes it from other D2-like subtypes.
url	https://doi.org/10.1038/s41467-020-14884-y
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Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands

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