Structures of the amphetamine-binding receptor will aid drug discovery
Structures of the amphetamine-binding receptor will aid drug discovery
High-resolution structures of TAAR1 — the receptor bound by amphetamines and molecules called trace amines — reveal detailed interactions with ligand molecules that will inform efforts to design antipsychotic drugs. - Harald H. Sitte
- Harald H. Sitte is at the Center for Physiology and Pharmacology, Institute of Pharmacology, and at the Center for Addiction Research and Science, Medical University of Vienna, 1090 Vienna, Austria.
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Small molecules known as trace amines have been reported in biological materials for nearly 150 years1. They are present in the nervous systems of mammals at low levels — about 100 times lower than the concentrations of the structurally related 'monoamine' neurotransmitter compounds, such as dopamine and serotonin2 — and bind to proteins known as trace amine-associated receptors (TAARs). One of these receptors, TAAR1, has a potential role in a range of neuropsychiatric conditions, and is associated with diabetes, obesity and immune disorders. Writing in Nature, Xu et al.3 and Liu et al.4 present an astonishing 12 cryo-electron microscopy structures of human and mouse TAAR1 in complex with an array of ligand molecules. The findings will aid the development of therapeutics that bind to TAAR1. Access options
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- Read the paper: Ligand recognition and G-protein coupling of trace amine receptor TAAR1
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