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Agonist Selectivity...
Agonist Selectivity and Ion Permeation in the alpha 3 beta 4 Ganglionic Nicotinic Receptor
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- Gharpure, Anant (author)
- Univ Texas Southwestern Med Ctr Dallas, Dept Neurosci, Dallas, TX 75390 USA.
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- Teng, Jinfeng (author)
- Univ Texas Southwestern Med Ctr Dallas, Dept Neurosci, Dallas, TX 75390 USA.
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- Zhuang, Yuxuan (author)
- Stockholms universitet,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab)
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- Noviello, Colleen M. (author)
- Univ Texas Southwestern Med Ctr Dallas, Dept Neurosci, Dallas, TX 75390 USA.
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- Walsh, Richard M., Jr. (author)
- Univ Texas Southwestern Med Ctr Dallas, Dept Neurosci, Dallas, TX 75390 USA.;Harvard Med Sch, Dept Biol Chem & Mol Pharmacol, Boston, MA 02115 USA.
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- Cabuco, Rico (author)
- Univ Texas Southwestern Med Ctr Dallas, Dept Neurosci, Dallas, TX 75390 USA.
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- Howard, Rebecca J. (author)
- Stockholms universitet,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab)
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- Zaveri, Nurulain T. (author)
- Astraea Therapeut, Mountain View, CA 94043 USA.
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- Lindahl, Erik, 1972- (author)
- Stockholms universitet,KTH,SeRC - Swedish e-Science Research Centre,Tillämpad fysik,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab),KTH Royal Institute of Technology, Sweden
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- Hibbs, Ryan E. (author)
- Univ Texas Southwestern Med Ctr Dallas, Dept Neurosci, Dallas, TX 75390 USA.
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Univ Texas Southwestern Med Ctr Dallas, Dept Neurosci, Dallas, TX 75390 USA Institutionen för biokemi och biofysik (creator_code:org_t)
- CELL PRESS, 2019
- 2019
- English.
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In: Neuron. - : CELL PRESS. - 0896-6273 .- 1097-4199. ; 104:3, s. 501-
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https://doi.org/10.1...
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Abstract
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- Nicotinic acetylcholine receptors are pentameric ion channels that mediate fast chemical neurotransmission. The alpha 3 beta 4 nicotinic receptor subtype forms the principal relay between the central and peripheral nervous systems in the autonomic ganglia. This receptor is also expressed focally in brain areas that affect reward circuits and addiction. Here, we present structures of the alpha 3 beta 4 nicotinic receptor in lipidic and detergent environments, using functional reconstitution to define lipids appropriate for structural analysis. The structures of the receptor in complex with nicotine, as well as the alpha 3 beta 4-selective ligand AT-1001, complemented by molecular dynamics, suggest principles of agonist selectivity. The structures further reveal much of the architecture of the intracellular domain, where mutagenesis experiments and simulations define residues governing ion conductance.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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Neuron
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To the university's database
- By the author/editor
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Gharpure, Anant
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Teng, Jinfeng
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Zhuang, Yuxuan
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Noviello, Collee ...
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Walsh, Richard M ...
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Cabuco, Rico
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Howard, Rebecca ...
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Zaveri, Nurulain ...
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Lindahl, Erik, 1 ...
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Hibbs, Ryan E.
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Pharmacology and ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
- Articles in the publication
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Neuron
- By the university
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Royal Institute of Technology
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Stockholm University