Structure-function Analysis of α-conotoxin PeIA and the Inhibition of Rat α3β4 Nicotinic Acetylcholine Receptors

Update item information
Publication Type poster
School or College College of Science
Department Biology
Author Kearns, Ireland
Contributor Hone, Arik J.; McIntosh, J. Michael
Title Structure-function Analysis of α-conotoxin PeIA and the Inhibition of Rat α3β4 Nicotinic Acetylcholine Receptors
Date 2018
Description The α3β4 nicotinic acetylcholine receptor (nAChR) subtype is widely expressed by neurons of the peripheral nervous system including those of dorsal root ganglion (DRG). Characterizing α3β4 nAChRs pharmacologically has been hampered by the lack of selective ligands capable of distinguishing among closely related subtypes, particularly between α3β4 and α6β4. In an effort to remedy this situation, we conducted structure-activity studies on α-conotoxin PeIA in order to identify residues of the peptide that influenced the potency for α3β4 nAChRs. Select substitutions of positions known to be important for PeIA activity were made and the resulting analogs tested for their ability to inhibit acetylcholine-gated currents mediated by rat α3β4 nAChRs heterologously expressed in Xenopus oocytes. Several of these analogs showed favorable increases in potency. The results of these studies offer important insights into the interactions of ligands with α3β4 nAChRs, and may inform future experiments developing analogs of PeIA that selectively and potently interact with the α3β4 subtype. Presented at the 2018 ACCESS Symposium at the University of Utah.
Type Text
Publisher University of Utah
Subject Conotoxin; Nicotinic acetylcholine receptor; PeIA; Conus pergrandis; Peptides
Language eng
Rights Management (c) ireland Kearns, Arik J. Hone, J. Michael McIntosh
Format Medium application/pdf
ARK ark:/87278/s6nd0497
Setname ir_uw
Date Created 2018-05-21
Date Modified 2018-05-21
ID 1323900
Reference URL https://collections.lib.utah.edu/ark:/87278/s6nd0497
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