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Identifying Motifs Essential for Selective Activation of Nicotinic Acetylcholine Receptors

Marotta, Christopher and Lester, Henry A. and Dougherty, Dennis A. (2014) Identifying Motifs Essential for Selective Activation of Nicotinic Acetylcholine Receptors. Biophysical Journal, 106 (2). 341A. ISSN 0006-3495. http://resolver.caltech.edu/CaltechAUTHORS:20140710-092155936

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Abstract

Neuronal Nicotinic acetylcholine receptors (nAChRs) are found throughout the brain and have vital roles in memory and learning. In addition, these ligand gated ion channel are major targets of drug research for neurological disorders. Here, the two stoichiometries of α4β2 nAChRs expressed in Xenopus oocytes were probed using two agonists that display stoichiometry selectivity: Sazetidine A and NS9283. The results from these studies led to the following conclusions that may be generalized to the nAChR family: 1) an agonist must be bound to each α subunit in the receptor in order to fully activate the receptor and 2) three key residues located on the complementary side of the subunit dictate agonist selectivity. Through better understanding of agonist binding, more potent and selective responses with minimized off target responses can be obtained.


Item Type:Article
Related URLs:
URLURL TypeDescription
http://dx.doi.org/10.1016/j.bpj.2013.11.1951DOIArticle
http://www.sciencedirect.com/science/article/pii/S0006349513032098PublisherArticle
http://www.biophysics.org/2014meeting/Main/tabid/4177/Default.aspxOrganizationConference Website
ORCID:
AuthorORCID
Lester, Henry A.0000-0002-5470-5255
Dougherty, Dennis A.0000-0003-1464-2461
Additional Information:© 2014 Biophysical Society. Published by Elsevier Inc.
Record Number:CaltechAUTHORS:20140710-092155936
Persistent URL:http://resolver.caltech.edu/CaltechAUTHORS:20140710-092155936
Official Citation:Christopher Marotta, Henry A. Lester, Dennis A. Dougherty, Identifying Motifs Essential for Selective Activation of Nicotinic Acetylcholine Receptors, Biophysical Journal, Volume 106, Issue 2, Supplement 1, 28 January 2014, Page 341a, ISSN 0006-3495, http://dx.doi.org/10.1016/j.bpj.2013.11.1951. (http://www.sciencedirect.com/science/article/pii/S0006349513032098)
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:47127
Collection:CaltechAUTHORS
Deposited By: Tony Diaz
Deposited On:10 Jul 2014 19:37
Last Modified:03 Nov 2017 21:54

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