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    α-RgIA:  A Novel Conotoxin That Specifically and Potently Blocks the α9α10 nAChR†,‡
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    Departments of Biology, Pathology, and Psychiatry, University of Utah, Salt Lake City, Utah 84112, and Instituto Investigaciones en Ingeniería Genética y Biología Molecular, Consejo Nacional de Investigaciones Científicas y Técnicas-Universidad de Buenos Aires, Buenos Aires 1428, Argentina
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    Biochemistry

    Cite this: Biochemistry 2006, 45, 5, 1511–1517
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    https://doi.org/10.1021/bi0520129
    Published January 13, 2006
    Copyright © 2006 American Chemical Society
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    Abstract

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    The α9 and α10 nicotinic acetylcholine receptor (nAChR) subunits assemble to form the α9α10 nAChR subtype. This receptor is believed to mediate cholinergic synaptic transmission between efferent olivocochlear fibers and the hair cells of the cochlea. In addition α9 and/or α10 expression has been described in dorsal root ganglion neurons, lymphocytes, skin keratinocytes, and the pars tuberalis of the pituitary. Specific antagonists that selectively block the α9α10 channel could be valuable tools for elucidating its role in these diverse tissues. This study describes a novel α-conotoxin from the Western Atlantic species Conus regius, α-conotoxin RgIA (α-RgIA), that is a subtype specific blocker of the α9α10 nAChR. α-RgIA belongs to the α4/3 subfamily of the α-conotoxin family; sequence and subtype specificity comparisons between α-RgIA and previously characterized α4/3 toxins indicate that the amino acids in the C-terminal half of α-RgIA are responsible for its preferential inhibition of the α9α10 nAChR subtype.

    Copyright © 2006 American Chemical Society

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    †

     This work was supported by an International Research Scholar grant from the Howard Hughes Medical Institute, the Agencia Nacional de Promoción Científica y Tecnológica, the University of Buenos Aires (A.B.E.), and National Institutes of Health Grants GM48677 and MH53631.

    ‡

     The sequence of the fragment of the α-RgIA precursor gene has been deposited at GenBank (accession code DQ239610).

    *

     To whom correspondence should be addressed. Mailing address:  Department of Biology, University of Utah, 257 South 1400 East, Salt Lake City, UT 84112-0840. Tel:  (801) 581-8370. Fax:  (801) 585-5010. E-mail:  [email protected].

    §

     Department of Biology, University of Utah.

    ‖

     Consejo Nacional de Investigaciones Científicas y Técnicas-Universidad de Buenos Aires.

    ⊥

     Department of Pathology, University of Utah.

    #

     Department of Psychiatry, University of Utah.

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    Biochemistry

    Cite this: Biochemistry 2006, 45, 5, 1511–1517
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    https://doi.org/10.1021/bi0520129
    Published January 13, 2006
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