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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
Cite this: Biochemistry 2006, 45, 5, 1511–1517
Publication Date (Web):January 13, 2006
Copyright © 2006 American Chemical Society

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    Abstract Image

    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.

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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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    6. Nan Zheng, Sean B. Christensen, Cheryl Dowell, Landa Purushottam, Jack J. Skalicky, J. Michael McIntosh, Danny Hung-Chieh Chou. Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain. Journal of Medicinal Chemistry 2021, 64 (13) , 9513-9524.
    7. Nan Zheng, Sean B. Christensen, Alan Blakely, Cheryl Dowell, Landa Purushottam, J. Michael McIntosh, Danny Hung-Chieh Chou. Development of Conformationally Constrained α-RgIA Analogues as Stable Peptide Antagonists of Human α9α10 Nicotinic Acetylcholine Receptors. Journal of Medicinal Chemistry 2020, 63 (15) , 8380-8387.
    8. Jiazhen Liang, Han-Shen Tae, Xiaoxiao Xu, Tao Jiang, David J. Adams, Rilei Yu. Dimerization of α-Conotoxins as a Strategy to Enhance the Inhibition of the Human α7 and α9α10 Nicotinic Acetylcholine Receptors. Journal of Medicinal Chemistry 2020, 63 (6) , 2974-2985.
    9. Mahsa Sadeghi, Bodil B. Carstens, Brid P. Callaghan, James T. Daniel, Han-Shen Tae, Tracey O’Donnell, Joel Castro, Stuart M. Brierley, David J. Adams, David J. Craik, Richard J. Clark. Structure–Activity Studies Reveal the Molecular Basis for GABAB-Receptor Mediated Inhibition of High Voltage-Activated Calcium Channels by α-Conotoxin Vc1.1. ACS Chemical Biology 2018, 13 (6) , 1577-1587.
    10. Sandeep Chhabra, Alessia Belgi, Peter Bartels, Bianca J. van Lierop, Samuel D. Robinson, Shiva N. Kompella, Andrew Hung, Brid P. Callaghan, David J. Adams, Andrea J. Robinson, and Raymond S. Norton . Dicarba Analogues of α-Conotoxin RgIA. Structure, Stability, and Activity at Potential Pain Targets. Journal of Medicinal Chemistry 2014, 57 (23) , 9933-9944.
    11. Kalyana B. Akondi, Markus Muttenthaler, Sébastien Dutertre, Quentin Kaas, David J. Craik, Richard J. Lewis, and Paul F. Alewood . Discovery, Synthesis, and Structure–Activity Relationships of Conotoxins. Chemical Reviews 2014, 114 (11) , 5815-5847.
    12. Sulan Luo, Dongting Zhangsun, Xiaopeng Zhu, Yong Wu, Yuanyan Hu, Sean Christensen, Peta J. Harvey, Muharrem Akcan, David J. Craik, and J. Michael McIntosh . Characterization of a Novel α-Conotoxin TxID from Conus textile That Potently Blocks Rat α3β4 Nicotinic Acetylcholine Receptors. Journal of Medicinal Chemistry 2013, 56 (23) , 9655-9663.
    13. Reena Halai, Brid Callaghan, Norelle L. Daly, Richard J. Clark, David J. Adams, and David J. Craik . Effects of Cyclization on Stability, Structure, and Activity of α-Conotoxin RgIA at the α9α10 Nicotinic Acetylcholine Receptor and GABAB Receptor. Journal of Medicinal Chemistry 2011, 54 (19) , 6984-6992.
    14. Steven Harris and Susan J. Schroeder. Nuclear Magnetic Resonance Structure of the Prohead RNA E-Loop Hairpin,. Biochemistry 2010, 49 (29) , 5989-5997.
    15. Marion L. Loughnan, Annette Nicke, Nicole Lawrence and Richard J. Lewis . Novel αD-Conopeptides and Their Precursors Identified by cDNA Cloning Define the D-Conotoxin Superfamily. Biochemistry 2009, 48 (17) , 3717-3729.
    16. An Luo, Jie He, Jinpeng Yu, Yong Wu, Peta J. Harvey, Igor E. Kasheverov, Denis S. Kudryavtsev, J. Michael McIntosh, Victor I. Tsetlin, David J. Craik, Dongting Zhangsun, Sulan Luo. Aspartic acid mutagenesis of αO-Conotoxin GeXIVA isomers reveals arginine residues crucial for inhibition of the α9α10 nicotinic acetylcholine receptor. International Journal of Biological Macromolecules 2024, 271 , 132472.
    17. Tianmiao Li, Han-Shen Tae, Jiazhen Liang, Zixuan Zhang, Xiao Li, Tao Jiang, David J. Adams, Rilei Yu. Rational Design of Potent α-Conotoxin PeIA Analogues with Non-Natural Amino Acids for the Inhibition of Human α9α10 Nicotinic Acetylcholine Receptors. Marine Drugs 2024, 22 (3) , 110.
    18. Minghe Wang, Zhouyuji Liao, Dongting Zhangsun, Yong Wu, Sulan Luo. Engineering Enhanced Antimicrobial Properties in α-Conotoxin RgIA through D-Type Amino Acid Substitution and Incorporation of Lysine and Leucine Residues. Molecules 2024, 29 (5) , 1181.
    19. Ana Novo de Oliveira, Andreimar Martins Soares, Saulo Luís Da Silva. Why to Study Peptides from Venomous and Poisonous Animals?. International Journal of Peptide Research and Therapeutics 2023, 29 (5)
    20. Alessandro Giraudo, Marco Pallavicini, Cristiano Bolchi. Small molecule ligands for α9 * and α7 nicotinic receptors: A survey and an update, respectively. Pharmacological Research 2023, 193 , 106801.
    21. Yong Wu, Junjie Zhang, Jie Ren, Xiaopeng Zhu, Rui Li, Dongting Zhangsun, Sulan Luo. Substitution of D-Arginine at Position 11 of α-RgIA Potently Inhibits α7 Nicotinic Acetylcholine Receptor. Marine Drugs 2023, 21 (6) , 326.
    22. Yuanyuan Zhang, Hakim Hiel, Philippe F.Y. Vincent, Megan B. Wood, Ana B. Elgoyhen, Wade Chien, Amanda Lauer, Paul A. Fuchs. Engineering olivocochlear inhibition to reduce acoustic trauma. Molecular Therapy - Methods & Clinical Development 2023, 29 , 17-31.
    23. Han-Shen Tae, David J. Adams. Nicotinic acetylcholine receptor subtype expression, function, and pharmacology: Therapeutic potential of α-conotoxins. Pharmacological Research 2023, 191 , 106747.
    24. Lydia J. Bye, Rocio K. Finol-Urdaneta, Han-Shen Tae, David J. Adams. Nicotinic acetylcholine receptors: Key targets for attenuating neurodegenerative diseases. The International Journal of Biochemistry & Cell Biology 2023, 157 , 106387.
    25. Irina Shelukhina, Andrei Siniavin, Igor Kasheverov, Lucy Ojomoko, Victor Tsetlin, Yuri Utkin. α7- and α9-Containing Nicotinic Acetylcholine Receptors in the Functioning of Immune System and in Pain. International Journal of Molecular Sciences 2023, 24 (7) , 6524.
    26. Ana Belén Elgoyhen. The α9α10 acetylcholine receptor: A non-neuronal nicotinic receptor. Pharmacological Research 2023, 190 , 106735.
    27. Bankala Krishnarjuna, Punnepalli Sunanda, Jeffrey Seow, Han-Shen Tae, Samuel D. Robinson, Alessia Belgi, Andrea J. Robinson, Helena Safavi-Hemami, David J. Adams, Raymond S. Norton. Characterisation of Elevenin-Vc1 from the Venom of Conus victoriae: A Structural Analogue of α-Conotoxins. Marine Drugs 2023, 21 (2) , 81.
    28. Helena B. Fiorotti, Suely G. Figueiredo, Fabiana V. Campos, Daniel C. Pimenta. Cone snail species off the Brazilian coast and their venoms: a review and update. Journal of Venomous Animals and Toxins including Tropical Diseases 2023, 29
    29. Igor Kasheverov, Yulia Logashina, Fedor Kornilov, Vladislav Lushpa, Ekaterina Maleeva, Yuliya Korolkova, Jinpeng Yu, Xiaopeng Zhu, Dongting Zhangsun, Sulan Luo, Klara Stensvåg, Denis Kudryavtsev, Konstantin Mineev, Yaroslav Andreev. Peptides from the Sea Anemone Metridium senile with Modified Inhibitor Cystine Knot (ICK) Fold Inhibit Nicotinic Acetylcholine Receptors. Toxins 2023, 15 (1) , 28.
    30. Francesco Margiotta, Laura Micheli, Clara Ciampi, Carla Ghelardini, J. Michael McIntosh, Lorenzo Di Cesare Mannelli. Conus regius-Derived Conotoxins: Novel Therapeutic Opportunities from a Marine Organism. Marine Drugs 2022, 20 (12) , 773.
    31. Peter N. Huynh, Sean B. Christensen, J. Michael McIntosh. RgIA4 Prevention of Acute Oxaliplatin-Induced Cold Allodynia Requires α9-Containing Nicotinic Acetylcholine Receptors and CD3+ T-Cells. Cells 2022, 11 (22) , 3561.
    32. Arik J. Hone, J. Michael McIntosh. Alkaloid ligands enable function of homomeric human α10 nicotinic acetylcholine receptors. Frontiers in Pharmacology 2022, 13
    33. Toshiaki Okada, Hikaru Taira, Tadashi Kimura. Current Ion Channel-targeted Drugs and Potential of Venom-derived Peptides as a Therapeutic New Modality. Venoms and Toxins 2022, 2 (2)
    34. Yuan Ma, Qiushi Cao, Mengke Yang, Yue Gao, Shuiping Fu, Wenhao Du, David Adams, Tao Jiang, Han-Shen Tae, Rilei Yu. Single-Disulfide Conopeptide Czon1107, an Allosteric Antagonist of the Human α3β4 Nicotinic Acetylcholine Receptor. Marine Drugs 2022, 20 (8) , 497.
    35. Arisaí C. Hernández-Sámano, Andrés Falcón, Fernando Zamudio, Jesús Emilio Michel-Morfín, Víctor Landa-Jaime, Estuardo López-Vera, Michael C. Jeziorski, Manuel B. Aguilar. A short framework-III (mini-M-2) conotoxin from the venom of a vermivorous species, Conus archon, inhibits human neuronal nicotinic acetylcholine receptors. Peptides 2022, 153 , 170785.
    36. Thomas Fischer, Rainer Riedl. Paracelsus’ legacy in the faunal realm: Drugs deriving from animal toxins. Drug Discovery Today 2022, 27 (2) , 567-575.
    37. Susanna Pucci, Michele Zoli, Francesco Clementi, Cecilia Gotti. α9-Containing Nicotinic Receptors in Cancer. Frontiers in Cellular Neuroscience 2022, 15
    38. Victor Tsetlin, Yves Haufe, Valentina Safronova, Dmitriy Serov, PranavKumar Shadamarshan, Lina Son, Irina Shelukhina, Denis Kudryavtsev, Elena Kryukova, Igor Kasheverov, Annette Nicke, Yuri Utkin. Interaction of α9α10 Nicotinic Receptors With Peptides and Proteins From Animal Venoms. Frontiers in Cellular Neuroscience 2021, 15
    39. Si Pan, Yingxu Fan, Xiaopeng Zhu, Yi Xue, Sulan Luo, Xinquan Wang. From Crystal Structures of RgIA4 in Complex with Ac-AChBP to Molecular Determinants of Its High Potency of α9α10 nAChR. Marine Drugs 2021, 19 (12) , 709.
    40. Fernando Fisher, Yuanyuan Zhang, Philippe F. Y. Vincent, Joanna Gajewiak, Thomas J. Gordon, Elisabeth Glowatzki, Paul Albert Fuchs, J. Michael McIntosh. Cy3-RgIA-5727 Labels and Inhibits α9-Containing nAChRs of Cochlear Hair Cells. Frontiers in Cellular Neuroscience 2021, 15
    41. Xiao Li, Han-Shen Tae, Yanyan Chu, Tao Jiang, David J. Adams, Rilei Yu. Medicinal chemistry, pharmacology, and therapeutic potential of α-conotoxins antagonizing the α9α10 nicotinic acetylcholine receptor. Pharmacology & Therapeutics 2021, 222 , 107792.
    42. Ayaulym Bekbossynova, Albina Zharylgap, Olena Filchakova. Venom-Derived Neurotoxins Targeting Nicotinic Acetylcholine Receptors. Molecules 2021, 26 (11) , 3373.
    43. Zhiguo Li, Xiaolu Han, Xiaoxuan Hong, Xianfu Li, Jing Gao, Hui Zhang, Aiping Zheng. Lyophilization Serves as an Effective Strategy for Drug Development of the α9α10 Nicotinic Acetylcholine Receptor Antagonist α-Conotoxin GeXIVA[1,2]. Marine Drugs 2021, 19 (3) , 121.
    44. Tatiana I. Terpinskaya, Alexey V. Osipov, Elena V. Kryukova, Denis S. Kudryavtsev, Nina V. Kopylova, Tatsiana L. Yanchanka, Alena F. Palukoshka, Elena A. Gondarenko, Maxim N. Zhmak, Victor I. Tsetlin, Yuri N. Utkin. α-Conotoxins and α-Cobratoxin Promote, while Lipoxygenase and Cyclooxygenase Inhibitors Suppress the Proliferation of Glioma C6 Cells. Marine Drugs 2021, 19 (2) , 118.
    45. Shane Dennis Hellyer. Marine-derived nicotinic receptor antagonist toxins: Pinnatoxins and alpha conotoxins. 2021, 105-191.
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    47. Thao N. T. Ho, Nikita Abraham, Richard J. Lewis. Structure-Function of Neuronal Nicotinic Acetylcholine Receptor Inhibitors Derived From Natural Toxins. Frontiers in Neuroscience 2020, 14
    48. Ashlin Turner, Quentin Kaas, David J. Craik. Hormone-like conopeptides – new tools for pharmaceutical design. RSC Medicinal Chemistry 2020, 11 (11) , 1235-1251.
    49. Peter N. Huynh, Peta J. Harvey, Joanna Gajewiak, David J. Craik, J. Michael McIntosh. Critical residue properties for potency and selectivity of α-Conotoxin RgIA towards α9α10 nicotinic acetylcholine receptors. Biochemical Pharmacology 2020, 181 , 114124.
    50. Shakir D. AlSharari, Wisam Toma, Hafiz M. Mahmood, J. Michael McIntosh, M. Imad Damaj. The α9α10 nicotinic acetylcholine receptors antagonist α-conotoxin RgIA reverses colitis signs in murine dextran sodium sulfate model. European Journal of Pharmacology 2020, 883 , 173320.
    51. Zhou Yu, J. Michael McIntosh, Soroush G. Sadeghi, Elisabeth Glowatzki. Efferent synaptic transmission at the vestibular type II hair cell synapse. Journal of Neurophysiology 2020, 124 (2) , 360-374.
    52. Walden E. Bjørn-Yoshimoto, Iris Bea L. Ramiro, Mark Yandell, J. Michael McIntosh, Baldomero M. Olivera, Lars Ellgaard, Helena Safavi-Hemami. Curses or Cures: A Review of the Numerous Benefits Versus the Biosecurity Concerns of Conotoxin Research. Biomedicines 2020, 8 (8) , 235.
    53. Yanli Liu, Yifeng Yin, Yunyang Song, Kang Wang, Fanghui Wu, Hui Jiang. α-Conotoxin as Potential to α7-nAChR Recombinant Expressed in Escherichia coli. Marine Drugs 2020, 18 (8) , 422.
    54. Adam C. Kennedy, Alessia Belgi, Benjamin W. Husselbee, David Spanswick, Raymond S. Norton, Andrea J. Robinson. α-Conotoxin Peptidomimetics: Probing the Minimal Binding Motif for Effective Analgesia. Toxins 2020, 12 (8) , 505.
    55. Peter N. Huynh, Denise Giuvelis, Sean Christensen, Kerry L. Tucker, J. Michael McIntosh. RgIA4 Accelerates Recovery from Paclitaxel-Induced Neuropathic Pain in Rats. Marine Drugs 2020, 18 (1) , 12.
    56. Qiang Liu, Minshu Li, Paul Whiteaker, Fu-Dong Shi, Barbara J. Morley, Ronald J. Lukas. Attenuation in Nicotinic Acetylcholine Receptor α9 and α10 Subunit Double Knock-Out Mice of Experimental Autoimmune Encephalomyelitis. Biomolecules 2019, 9 (12) , 827.
    57. Heike Wulff, Palle Christophersen, Paul Colussi, K. George Chandy, Vladimir Yarov-Yarovoy. Antibodies and venom peptides: new modalities for ion channels. Nature Reviews Drug Discovery 2019, 18 (5) , 339-357.
    58. Marios Zouridakis, Athanasios Papakyriakou, Igor A. Ivanov, Igor E. Kasheverov, Victor Tsetlin, Socrates Tzartos, Petros Giastas. Crystal Structure of the Monomeric Extracellular Domain of α9 Nicotinic Receptor Subunit in Complex With α-Conotoxin RgIA: Molecular Dynamics Insights Into RgIA Binding to α9α10 Nicotinic Receptors. Frontiers in Pharmacology 2019, 10
    59. Jie Ren, Xiaopeng Zhu, Pan Xu, Rui Li, Ying Fu, Shuai Dong, Dongting Zhangsun, Yong Wu, Sulan Luo. d-Amino Acid Substitution of α-Conotoxin RgIA Identifies its Critical Residues and Improves the Enzymatic Stability. Marine Drugs 2019, 17 (3) , 142.
    60. Veronika Grau, Katrin Richter, Arik J. Hone, J. Michael McIntosh. Conopeptides [V11L;V16D]ArIB and RgIA4: Powerful Tools for the Identification of Novel Nicotinic Acetylcholine Receptors in Monocytes. Frontiers in Pharmacology 2019, 9
    61. Helena Safavi-Hemami, Shane E. Brogan, Baldomero M. Olivera. Pain therapeutics from cone snail venoms: From Ziconotide to novel non-opioid pathways. Journal of Proteomics 2019, 190 , 12-20.
    62. M. Jesús Pérez de Vega, Antonio Ferrer-Montiel, Rosario González-Muñiz. Recent progress in non-opioid analgesic peptides. Archives of Biochemistry and Biophysics 2018, 660 , 36-52.
    63. Julien Giribaldi, Sébastien Dutertre. α-Conotoxins to explore the molecular, physiological and pathophysiological functions of neuronal nicotinic acetylcholine receptors. Neuroscience Letters 2018, 679 , 24-34.
    64. Mathilde R. Israel, Michael Morgan, Bryan Tay, Jennifer R. Deuis. Toxins as tools: Fingerprinting neuronal pharmacology. Neuroscience Letters 2018, 679 , 4-14.
    65. Michael W. Pennington, Andrzej Czerwinski, Raymond S. Norton. Peptide therapeutics from venom: Current status and potential. Bioorganic & Medicinal Chemistry 2018, 26 (10) , 2738-2758.
    66. Arik J Hone, Denis Servent, J Michael McIntosh. α9‐containing nicotinic acetylcholine receptors and the modulation of pain. British Journal of Pharmacology 2018, 175 (11) , 1915-1927.
    67. Vanessa Mucchietto, Francesca Fasoli, Susanna Pucci, Milena Moretti, Roberta Benfante, Annalisa Maroli, Simona Di Lascio, Cristiano Bolchi, Marco Pallavicini, Cheryl Dowell, Michael McIntosh, Francesco Clementi, Cecilia Gotti. α9‐ and α7‐containing receptors mediate the pro‐proliferative effects of nicotine in the A549 adenocarcinoma cell line. British Journal of Pharmacology 2018, 175 (11) , 1957-1972.
    68. Nikita Abraham, Richard J. Lewis. Neuronal Nicotinic Acetylcholine Receptor Modulators from Cone Snails. Marine Drugs 2018, 16 (6) , 208.
    69. Mousa K. Hamad, Kevin He, Hael F. Abdulrazeq, Ali M. Mustafa, Robert Luceri, Naveed Kamal, Mohsin Ali, Jonathan Nakhla, Mohammad M. Herzallah, Antonios Mammis. Potential Uses of Isolated Toxin Peptides in Neuropathic Pain Relief: A Literature Review. World Neurosurgery 2018, 113 , 333-347.e5.
    70. Arik J. Hone, J. Michael McIntosh. Nicotinic acetylcholine receptors in neuropathic and inflammatory pain. FEBS Letters 2018, 592 (7) , 1045-1062.
    71. Sébastien Dutertre, Annette Nicke, Victor I. Tsetlin. Nicotinic acetylcholine receptor inhibitors derived from snake and snail venoms. Neuropharmacology 2017, 127 , 196-223.
    72. Xiaosa Wu, Yen-Hua Huang, Quentin Kaas, Peta J. Harvey, Conan K. Wang, Han-Shen Tae, David J. Adams, David J. Craik. Backbone cyclization of analgesic conotoxin GeXIVA facilitates direct folding of the ribbon isomer. Journal of Biological Chemistry 2017, 292 (41) , 17101-17112.
    73. Haylie K. Romero, Sean B. Christensen, Lorenzo Di Cesare Mannelli, Joanna Gajewiak, Renuka Ramachandra, Keith S. Elmslie, Douglas E. Vetter, Carla Ghelardini, Shawn P. Iadonato, Jose L. Mercado, Baldomera M. Olivera, J. Michael McIntosh. Inhibition of α9α10 nicotinic acetylcholine receptors prevents chemotherapy-induced neuropathic pain. Proceedings of the National Academy of Sciences 2017, 114 (10)
    74. Juan Carlos Boffi, Irina Marcovich, JasKiran K. Gill-Thind, Jeremías Corradi, Toby Collins, María Marcela Lipovsek, Marcelo Moglie, Paola V. Plazas, Patricio O. Craig, Neil S. Millar, Cecilia Bouzat, Ana Belén Elgoyhen. Differential Contribution of Subunit Interfaces to α 9 α 10 Nicotinic Acetylcholine Receptor Function. Molecular Pharmacology 2017, 91 (3) , 250-262.
    75. Elsie C. Jimenez, Lourdes J. Cruz. Conotoxins as Tools in Research on Nicotinic Receptors. 2017, 189-204.
    76. Bo Lin, Shihua Xiang, Mengsen Li. Residues Responsible for the Selectivity of α-Conotoxins for Ac-AChBP or nAChRs. Marine Drugs 2016, 14 (10) , 173.
    77. Alessandra Pacini, Laura Micheli, Mario Maresca, Jacopo Juno Valerio Branca, J. Michael McIntosh, Carla Ghelardini, Lorenzo Di Cesare Mannelli. The α9α10 nicotinic receptor antagonist α-conotoxin RgIA prevents neuropathic pain induced by oxaliplatin treatment. Experimental Neurology 2016, 282 , 37-48.
    78. Isabelle Roux, Jingjing Sherry Wu (武靜靜), J. Michael McIntosh, Elisabeth Glowatzki. Assessment of the expression and role of the α 1 -nAChR subunit in efferent cholinergic function during the development of the mammalian cochlea. Journal of Neurophysiology 2016, 116 (2) , 479-492.
    79. Xiaosa Wu, Yen‐Hua Huang, Quentin Kaas, David J. Craik. Cyclisation of Disulfide‐Rich Conotoxins in Drug Design Applications. European Journal of Organic Chemistry 2016, 2016 (21) , 3462-3472.
    80. Bodil B. Carstens, Géza Berecki, James T. Daniel, Han Siean Lee, Kathryn A. V. Jackson, Han‐Shen Tae, Mahsa Sadeghi, Joel Castro, Tracy O'Donnell, Annemie Deiteren, Stuart M. Brierley, David J. Craik, David J. Adams, Richard J. Clark. Structure–Activity Studies of Cysteine‐Rich α‐Conotoxins that Inhibit High‐Voltage‐Activated Calcium Channels via GABA B Receptor Activation Reveal a Minimal Functional Motif. Angewandte Chemie 2016, 128 (15) , 4770-4774.
    81. Bodil B. Carstens, Géza Berecki, James T. Daniel, Han Siean Lee, Kathryn A. V. Jackson, Han‐Shen Tae, Mahsa Sadeghi, Joel Castro, Tracy O'Donnell, Annemie Deiteren, Stuart M. Brierley, David J. Craik, David J. Adams, Richard J. Clark. Structure–Activity Studies of Cysteine‐Rich α‐Conotoxins that Inhibit High‐Voltage‐Activated Calcium Channels via GABA B Receptor Activation Reveal a Minimal Functional Motif. Angewandte Chemie International Edition 2016, 55 (15) , 4692-4696.
    82. Elsie C. Jimenez, Lourdes J. Cruz. Conotoxins as Tools in Research on Nicotinic Receptors. 2016, 1-17.
    83. Elsie C. Jimenez, Lourdes J. Cruz. Conotoxins as Tools in Research on Nicotinic Receptors. 2016, 1-17.
    84. Eric Schmidt. Biosynthetic Approaches to Marine Drug Discovery and Development. 2015, 43-64.
    85. Sarasa Mohammadi, MacDonald Christie. Conotoxin Interactions with α9α10-nAChRs: Is the α9α10-Nicotinic Acetylcholine Receptor an Important Therapeutic Target for Pain Management?. Toxins 2015, 7 (10) , 3916-3932.
    86. Sean B. Christensen, Pradip K. Bandyopadhyay, Baldomero M. Olivera, J. Michael McIntosh. αS-conotoxin GVIIIB potently and selectively blocks α9α10 nicotinic acetylcholine receptors. Biochemical Pharmacology 2015, 96 (4) , 349-356.
    87. Layla Azam, Athanasios Papakyriakou, Marios Zouridakis, Petros Giastas, Socrates J. Tzartos, J. Michael McIntosh. Molecular Interaction of α -Conotoxin RgIA with the Rat α 9 α 10 Nicotinic Acetylcholine Receptor. Molecular Pharmacology 2015, 87 (5) , 855-864.
    88. J. Chris Holt, Kevin Kewin, Paivi M. Jordan, Peter Cameron, Marcin Klapczynski, J. Michael McIntosh, Peter A. Crooks, Linda P. Dwoskin, Anna Lysakowski. Pharmacologically Distinct Nicotinic Acetylcholine Receptors Drive Efferent-Mediated Excitation in Calyx-Bearing Vestibular Afferents. The Journal of Neuroscience 2015, 35 (8) , 3625-3643.
    89. Andrew B. Wright, Yohei Norimatsu, J. Michael McIntosh, Keith S. Elmslie. Limited Efficacy of α-Conopeptides, Vc1.1 and RgIA, To Inhibit Sensory Neuron Ca V Current. eneuro 2015, 2 (1) , ENEURO.0057-14.2015.
    90. Lorenzo Di Cesare Mannelli, Lorenzo Cinci, Laura Micheli, Matteo Zanardelli, Alessandra Pacini, Michael J. McIntosh, Carla Ghelardini. α-Conotoxin RgIA protects against the development of nerve injury-induced chronic pain and prevents both neuronal and glial derangement. Pain 2014, 155 (10) , 1986-1995.
    91. Parashar Thapa, Michael J. Espiritu, Chino C. Cabalteja, Jon-Paul Bingham. Conotoxins and their regulatory considerations. Regulatory Toxicology and Pharmacology 2014, 70 (1) , 197-202.
    92. Eline Lebbe, Steve Peigneur, Isuru Wijesekara, Jan Tytgat. Conotoxins Targeting Nicotinic Acetylcholine Receptors: An Overview. Marine Drugs 2014, 12 (5) , 2970-3004.
    93. Sravanthi Gundavarapu, Neerad C. Mishra, Shashi P. Singh, Raymond J. Langley, Ali Imran Saeed, Carol A. Feghali-Bostwick, J. Michael McIntosh, Julie Hutt, Ramakrishna Hegde, Shilpa Buch, Mohan L. Sopori, . HIV gp120 Induces Mucus Formation in Human Bronchial Epithelial Cells through CXCR4/α7-Nicotinic Acetylcholine Receptors. PLoS ONE 2013, 8 (10) , e77160.
    94. Xiaosa Wu, Yong Wu, Furong Zhu, Qiuyuan Yang, Qianqian Wu, Dongting Zhangsun, Sulan Luo. Optimal Cleavage and Oxidative Folding of α-Conotoxin TxIB as a Therapeutic Candidate Peptide. Marine Drugs 2013, 11 (9) , 3537-3553.
    95. Maria Cristina Vianna Braga, Arthur Andrade Nery, Henning Ulrich, Katsuhiro Konno, Juliana Mozer Sciani, Daniel Carvalho Pimenta. α -RgIB: A Novel Antagonist Peptide of Neuronal Acetylcholine Receptor Isolated from Conus regius Venom. International Journal of Peptides 2013, 2013 , 1-9.
    96. JC Boffi, C Wedemeyer, M Lipovsek, E Katz, DJ Calvo, AB Elgoyhen. Positive modulation of the α9α10 nicotinic cholinergic receptor by ascorbic acid. British Journal of Pharmacology 2013, 168 (4) , 954-965.
    97. Sulan Luo, Dongting Zhangsun, Yong Wu, Xiaopeng Zhu, Yuanyan Hu, Melissa McIntyre, Sean Christensen, Muharrem Akcan, David J. Craik, J. Michael McIntosh. Characterization of a Novel α-Conotoxin from Conus textile That Selectively Targets α6/α3β2β3 Nicotinic Acetylcholine Receptors. Journal of Biological Chemistry 2013, 288 (2) , 894-902.
    98. Sravanthi Gundavarapu, Julie A. Wilder, Neerad C. Mishra, Jules Rir-sima-ah, Raymond J. Langley, Shashi P. Singh, Ali Imran Saeed, Richard J. Jaramillo, Katherine M. Gott, Juan Carlos Peña-Philippides, Kevin S. Harrod, J. Michael McIntosh, Shilpa Buch, Mohan L. Sopori. Role of nicotinic receptors and acetylcholine in mucous cell metaplasia, hyperplasia, and airway mucus formation in vitro and in vivo. Journal of Allergy and Clinical Immunology 2012, 130 (3) , 770-780.e11.
    99. Layla Azam, J Michael McIntosh. Molecular basis for the differential sensitivity of rat and human α9α10 nAChRs to α‐conotoxin RgIA. Journal of Neurochemistry 2012, 122 (6) , 1137-1144.
    100. Hartmut Cuny, Andrew de Faoite, Thuan G. Huynh, Takahiro Yasuda, Géza Berecki, David J. Adams. γ-Aminobutyric Acid Type B (GABAB) Receptor Expression Is Needed for Inhibition of N-type (Cav2.2) Calcium Channels by Analgesic α-Conotoxins. Journal of Biological Chemistry 2012, 287 (28) , 23948-23957.
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