Ligand discovery from a dopamine D3 receptor homology model and crystal structure
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چکیده
منابع مشابه
Ligand Discovery from a Dopamine D3 Receptor Homology Model and Crystal Structure
G protein-coupled receptors (GPCRs) are intensely studied as drug targets and for their role in signaling. With the determination of the first crystal structures, interest in structure-based ligand discovery increased. Unfortunately, for most GPCRs no experimental structures are available. The determination of the D(3) receptor structure and the challenge to the community to predict it enabled ...
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Dopamine (DA) is one of the main catecholamines in the brain and is crucial for movement coordination, endocrine function, reward, mood, memory and emotions. The dopaminergic system is the primary therapeutic target in the treatment of Parkinson’s disease (PD), drug addiction and schizophrenia. Notwithstanding, dysfunction of central dopaminergic neurotransmission has also been associated to de...
متن کاملp139: role of dopamine receptor d3 in depression and anxiety
dopamine (da) is one of the main catecholamines in the brain and is crucial for movement coordination, endocrine function, reward, mood, memory and emotions. the dopaminergic system is the primary therapeutic target in the treatment of parkinson’s disease (pd), drug addiction and schizophrenia. notwithstanding, dysfunction of central dopaminergic neurotransmission has also been associated to de...
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Dopamine modulates movement, cognition, and emotion through activation of dopamine G protein-coupled receptors in the brain. The crystal structure of the human dopamine D3 receptor (D3R) in complex with the small molecule D2R/D3R-specific antagonist eticlopride reveals important features of the ligand binding pocket and extracellular loops. On the intracellular side of the receptor, a locked co...
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ژورنال
عنوان ژورنال: Nature Chemical Biology
سال: 2011
ISSN: 1552-4450,1552-4469
DOI: 10.1038/nchembio.662