Richard J Lewis

Summary

Affiliation: University of Queensland
Country: Australia

Publications

  1. ncbi Venomics: a new paradigm for natural products-based drug discovery
    Irina Vetter
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD, 4072, Australia
    Amino Acids 40:15-28. 2011
  2. ncbi Venom peptides as a rich source of cav2.2 channel blockers
    Silmara R Sousa
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia
    Toxins (Basel) 5:286-314. 2013
  3. ncbi Therapeutic potential of cone snail venom peptides (conopeptides)
    Irina Vetter
    Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland, 4072, Brisbane, Australia
    Curr Top Med Chem 12:1546-52. 2012
  4. ncbi Discovery and development of the χ-conopeptide class of analgesic peptides
    Richard J Lewis
    Institute for Molecular Bioscience, The University of Queensland, Australia
    Toxicon 59:524-8. 2012
  5. ncbi Conus venom peptide pharmacology
    Richard J Lewis
    Institute for Molecular Bioscience, University of Queensland, Q4072, Australia
    Pharmacol Rev 64:259-98. 2012
  6. ncbi Rapid extraction combined with LC-tandem mass spectrometry (CREM-LC/MS/MS) for the determination of ciguatoxins in ciguateric fish flesh
    Richard J Lewis
    Institute for Molecular Bioscience, The University of Queensland, QLD 4072, Australia
    Toxicon 54:62-6. 2009
  7. ncbi Conotoxins as selective inhibitors of neuronal ion channels, receptors and transporters
    Richard J Lewis
    Institute for Molecular Biosciences, The University of Queensland, 4072, Australia
    IUBMB Life 56:89-93. 2004
  8. ncbi Therapeutic potential of venom peptides
    Richard J Lewis
    Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Australia
    Nat Rev Drug Discov 2:790-802. 2003
  9. ncbi Conotoxin venom peptide therapeutics
    Richard J Lewis
    Xenome Ltd, Indooroopilly 4068 and Institute for Molecular Biosciences, The University of Queensland, 4072, Brisbane, Australia
    Adv Exp Med Biol 655:44-8. 2009
  10. ncbi Conotoxins: molecular and therapeutic targets
    Richard J Lewis
    Institute for Molecular Biosciences, The University of Queensland, Brisbane 4072, Australia
    Prog Mol Subcell Biol 46:45-65. 2009

Detail Information

Publications94

  1. ncbi Venomics: a new paradigm for natural products-based drug discovery
    Irina Vetter
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD, 4072, Australia
    Amino Acids 40:15-28. 2011
    ..Here, we discuss these technological developments in the context of establishing a high-throughput pipeline for venoms-based drug discovery...
  2. ncbi Venom peptides as a rich source of cav2.2 channel blockers
    Silmara R Sousa
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia
    Toxins (Basel) 5:286-314. 2013
    ..2 inhibitors. However, side effects in humans currently limit their clinical use. Here we review Ca(v)2.2 inhibitors from venoms and their potential as drug leads...
  3. ncbi Therapeutic potential of cone snail venom peptides (conopeptides)
    Irina Vetter
    Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland, 4072, Brisbane, Australia
    Curr Top Med Chem 12:1546-52. 2012
    ..In addition to their therapeutic potential, conopeptides have been valuable probes for studying the role of a number of key membrane proteins in normal and disease physiology...
  4. ncbi Discovery and development of the χ-conopeptide class of analgesic peptides
    Richard J Lewis
    Institute for Molecular Bioscience, The University of Queensland, Australia
    Toxicon 59:524-8. 2012
    ..Currently, Xen2174 is entering a Phase IIb double-blind study to determine safety and efficacy in bunionectomy pain...
  5. ncbi Conus venom peptide pharmacology
    Richard J Lewis
    Institute for Molecular Bioscience, University of Queensland, Q4072, Australia
    Pharmacol Rev 64:259-98. 2012
    ....
  6. ncbi Rapid extraction combined with LC-tandem mass spectrometry (CREM-LC/MS/MS) for the determination of ciguatoxins in ciguateric fish flesh
    Richard J Lewis
    Institute for Molecular Bioscience, The University of Queensland, QLD 4072, Australia
    Toxicon 54:62-6. 2009
    ..The approach is designed to simplify the extraction and analysis of multiple samples per day...
  7. ncbi Conotoxins as selective inhibitors of neuronal ion channels, receptors and transporters
    Richard J Lewis
    Institute for Molecular Biosciences, The University of Queensland, 4072, Australia
    IUBMB Life 56:89-93. 2004
    ....
  8. ncbi Therapeutic potential of venom peptides
    Richard J Lewis
    Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Australia
    Nat Rev Drug Discov 2:790-802. 2003
    ..Here we survey the pharmacology of venom peptides and assess their therapeutic prospects...
  9. ncbi Conotoxin venom peptide therapeutics
    Richard J Lewis
    Xenome Ltd, Indooroopilly 4068 and Institute for Molecular Biosciences, The University of Queensland, 4072, Brisbane, Australia
    Adv Exp Med Biol 655:44-8. 2009
    ..A number of these conopeptides reduce pain in animals models and several are now in preclinical and clinical development for the treatment of severe pain often associated with diseases such as cancer...
  10. ncbi Conotoxins: molecular and therapeutic targets
    Richard J Lewis
    Institute for Molecular Biosciences, The University of Queensland, Brisbane 4072, Australia
    Prog Mol Subcell Biol 46:45-65. 2009
    ..Less than 1% of cone snail venom peptides are pharmacologically characterised...
  11. ncbi Isolation and structure-activity of mu-conotoxin TIIIA, a potent inhibitor of tetrodotoxin-sensitive voltage-gated sodium channels
    Richard J Lewis
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, QLD 4072, Australia
    Mol Pharmacol 71:676-85. 2007
    ..TIIIA and analogs provide new biochemical probes as well as insights into the structure-activity of mu-conotoxins...
  12. ncbi Ciguatera: Australian perspectives on a global problem
    Richard J Lewis
    Institute for Molecular Biosciences, The University of Queensland, QLD 4072, Australia
    Toxicon 48:799-809. 2006
    ....
  13. ncbi The alpha2delta auxiliary subunit reduces affinity of omega-conotoxins for recombinant N-type (Cav2.2) calcium channels
    Jorgen Mould
    Institute for Molecular Bioscience, University of Queensland, Queensland 4072, Australia
    J Biol Chem 279:34705-14. 2004
    ..These results may have implications for the antinociceptive properties of omega-conotoxins, given that the alpha(2)delta subunit is up-regulated in certain pain states...
  14. ncbi Neuronally micro-conotoxins from Conus striatus utilize an alpha-helical motif to target mammalian sodium channels
    Christina I Schroeder
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland 4072, Australia
    J Biol Chem 283:21621-8. 2008
    ..The structure of SIIIA provides a new structural template for the development of neuronally selective inhibitors of TTX-sensitive VGSCs based on the smaller mu-conotoxin pharmacophore...
  15. ncbi Omega-conotoxin CVIB differentially inhibits native and recombinant N- and P/Q-type calcium channels
    Leonid Motin
    School of Biomedical Sciences, The University of Queensland, Brisbane, Queensland 4072, Australia
    Eur J Neurosci 25:435-44. 2007
    ..Omega-conotoxins CVIB and CVID may be useful as antagonists of N- and P/Q-type VGCCs, particularly in sensory neurons involved in processing primary nociceptive information...
  16. ncbi Solution structure of chi-conopeptide MrIA, a modulator of the human norepinephrine transporter
    K Peter R Nilsson
    Institute for Molecular Bioscience, University of Queensland, Brisbane 4072, Australia
    Biopolymers 80:815-23. 2005
    ..The N-terminus also affects activity, as a single N-terminal deletion introduced additional pharmacology at rat vas deferens, while deleting the first two amino acids reduced chi-conopeptide potency...
  17. ncbi Chemical and functional identification and characterization of novel sulfated alpha-conotoxins from the cone snail Conus anemone
    Marion L Loughnan
    Institute for Molecular Biosciences, The University of Queensland, Brisbane, QLD 4072, Australia
    J Med Chem 47:1234-41. 2004
    ....
  18. ncbi Inhibition of neuronal nicotinic acetylcholine receptor subtypes by alpha-Conotoxin GID and analogues
    Emma L Millard
    Institute for Molecular Bioscience, University of Queensland, Brisbane QLD 4072, Australia
    J Biol Chem 284:4944-51. 2009
    ..Overall, our findings contribute to the understanding of the structure-activity relationships of alpha-conotoxins and may be beneficial for the ongoing attempts to exploit modulators of the neuronal nAChRs as therapeutic agents...
  19. ncbi AChBP-targeted alpha-conotoxin correlates distinct binding orientations with nAChR subtype selectivity
    Sebastien Dutertre
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland, Australia
    EMBO J 26:3858-67. 2007
    ..Together, these results establish a new pharmacophore for the design of novel subtype-selective ligands with therapeutic potential in nAChR-related diseases...
  20. ncbi chi-Conopeptide pharmacophore development: toward a novel class of norepinephrine transporter inhibitor (Xen2174) for pain
    Andreas Brust
    Xenome Ltd, 120 Meiers Road, Indooroopilly, Queensland, Australia 4068
    J Med Chem 52:6991-7002. 2009
    ..On the basis of improved chemical stability and a wide therapeutic index, 3 was selected for further development and is currently in phase II clinical trials...
  21. ncbi Molecular engineering of conotoxins: the importance of loop size to alpha-conotoxin structure and function
    Ai Hua Jin
    Institute for Molecular Bioscience, University of Queensland, Brisbane, QLD 4072 Australia
    J Med Chem 51:5575-84. 2008
    ..Docking simulations identified several hydrogen bonds lost upon truncation that provide an explanation for the reduced affinities observed at the alpha7 nAChR and AChBP...
  22. ncbi Isolation, characterization and total regioselective synthesis of the novel μO-conotoxin MfVIA from Conus magnificus that targets voltage-gated sodium channels
    Irina Vetter
    Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland, St Lucia, Australia
    Biochem Pharmacol 84:540-8. 2012
    ..5>1.6∼1.7∼1.3∼1.1∼1.2). This improved approach to μO-conotoxin synthesis will facilitate the optimization of μO-conotoxins as novel analgesic molecules to improve pain management...
  23. ncbi Beta2 subunit contribution to 4/7 alpha-conotoxin binding to the nicotinic acetylcholine receptor
    Sebastien Dutertre
    Institute for Molecular Bioscience, The University of Queensland, Queensland 4072, Australia
    J Biol Chem 280:30460-8. 2005
    ....
  24. ncbi Determination of alpha-conotoxin binding modes on neuronal nicotinic acetylcholine receptors
    Sebastien Dutertre
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland 4072, Australia
    J Mol Recognit 17:339-47. 2004
    ..These findings, which distinguish alpha-conotoxin and alpha-neurotoxin binding modes, have implications for the rational design of selective nAChR antagonists...
  25. ncbi Identification of a novel class of nicotinic receptor antagonists: dimeric conotoxins VxXIIA, VxXIIB, and VxXIIC from Conus vexillum
    Marion Loughnan
    Institute for Molecular Bioscience, University of Queensland, Brisbane, Queensland 4072, Australia
    J Biol Chem 281:24745-55. 2006
    ..These dimeric conotoxins represent a fifth and highly divergent structural class of conotoxins targeting nAChRs...
  26. ncbi Novel alpha D-conopeptides and their precursors identified by cDNA cloning define the D-conotoxin superfamily
    Marion L Loughnan
    Institute for Molecular Biosciences, The University of Queensland, Brisbane, QLD 4072, Australia
    Biochemistry 48:3717-29. 2009
    ..mustelinus venom. The discovery of the precursors and several novel conotoxins from different species defines this large conotoxin family and expands our understanding of sequence diversification mechanisms in Conus species...
  27. ncbi Inhibition of the norepinephrine transporter by the venom peptide chi-MrIA. Site of action, Na+ dependence, and structure-activity relationship
    Iain A Sharpe
    Institute for Molecular Bioscience and School of Biomedical Sciences, The University of Queensland, St. Lucia 4072, Queensland, Australia
    J Biol Chem 278:40317-23. 2003
    ..From these data, we present a model of the structure of chi-MrIA that shows the relative orientation of the key binding residues. This model provides a new molecular caliper for probing the structure of the NET...
  28. ncbi Allosteric alpha 1-adrenoreceptor antagonism by the conopeptide rho-TIA
    Iain A Sharpe
    Institute for Molecular Bioscience and the School of Biomedical Sciences, The University of Queensland, St. Lucia 4072, Queensland, Australia
    J Biol Chem 278:34451-7. 2003
    ....
  29. ncbi Solution structure of mu-conotoxin PIIIA, a preferential inhibitor of persistent tetrodotoxin-sensitive sodium channels
    Katherine J Nielsen
    Institute for Molecular Bioscience, University of Queensland, Brisbane 4072, Australia
    J Biol Chem 277:27247-55. 2002
    ..Comparison of the structures and activity of PIIIA to muscle-selective mu-conotoxins provides an insight into the structural requirements for inhibition of different TTX-sensitive sodium channels by mu-conotoxins...
  30. ncbi Synthesis, structure elucidation, in vitro biological activity, toxicity, and Caco-2 cell permeability of lipophilic analogues of alpha-conotoxin MII
    Joanne T Blanchfield
    School of Pharmacy, Institute for Molecular Bioscience, and School of Biomedical Sciences, The University of Queensland, Brisbane 4072, Australia
    J Med Chem 46:1266-72. 2003
    ..The active LaaMII analogue was found to exhibit significantly improved permeability across Caco-2 cell monolayers compared to the native MII, and both peptides showed negligible toxicity...
  31. ncbi Solving the alpha-conotoxin folding problem: efficient selenium-directed on-resin generation of more potent and stable nicotinic acetylcholine receptor antagonists
    Markus Muttenthaler
    Institute for Molecular Bioscience, Division of Chemistry and Structural Biology, The University of Queensland, Brisbane, Queensland 4072, Australia
    J Am Chem Soc 132:3514-22. 2010
    ....
  32. ncbi Development of small molecules that mimic the binding of omega-conotoxins at the N-type voltage-gated calcium channel
    Christina I Schroeder
    Institute for Molecular Bioscience, University of Queensland, St Lucia, Australia
    Mol Divers 8:127-34. 2004
    ..Agreeing with the specificity profile of CVID, molecules were inactive at the P/Q-type VGCC...
  33. ncbi Effects of Lys2 to Ala2 substitutions on the structure and potency of ω-conotoxins MVIIA and CVID
    Christina I Schroeder
    Institute for Molecular Bioscience IMB, The University of Queensland, Brisbane 4072, QLD
    Biopolymers 98:345-56. 2012
    ....
  34. ncbi N- and C-terminal extensions of μ-conotoxins increase potency and selectivity for neuronal sodium channels
    Christina I Schroeder
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, Australia
    Biopolymers 98:161-5. 2012
    ....
  35. ncbi Conopeptide ρ-TIA defines a new allosteric site on the extracellular surface of the α1B-adrenoceptor
    Lotten Ragnarsson
    Institute for Molecular Bioscience, University of Queensland, Brisbane, Queensland 4072, Australia
    J Biol Chem 288:1814-27. 2013
    ....
  36. ncbi chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model
    Filip A Paczkowski
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland 4072, Australia
    J Biol Chem 282:17837-44. 2007
    ..In a new model of NET constructed from the bLeuT crystal structure, chi-MrIA-interacting residues were located at the mouth of the transporter near residues affecting the binding of small molecule inhibitors...
  37. ncbi Adenosine triphosphate acts as both a competitive antagonist and a positive allosteric modulator at recombinant N-methyl-D-aspartate receptors
    Anna Kloda
    School of Biomedical Sciences, University of Queensland, Brisbane, Queensland, Australia
    Mol Pharmacol 65:1386-96. 2004
    ..A simple model of the NMDA receptor, with ATP acting both as a competitive antagonist at the glutamate binding site and as a positive allosteric modulator at a separate site, reproduced the main features of the data...
  38. ncbi chi-Conopeptide MrIA partially overlaps desipramine and cocaine binding sites on the human norepinephrine transporter
    Lesley J Bryan-Lluka
    Institute for Molecular Bioscience, The University of Queensland, Brisbane 4072, Queensland, Australia
    J Biol Chem 278:40324-9. 2003
    ....
  39. ncbi Structures of muO-conotoxins from Conus marmoreus. I nhibitors of tetrodotoxin (TTX)-sensitive and TTX-resistant sodium channels in mammalian sensory neurons
    Norelle L Daly
    Institute for Molecular Bioscience and School of Biomedical Sciences, University of Queensland, Brisbane, 4072 Queensland, Australia
    J Biol Chem 279:25774-82. 2004
    ....
  40. ncbi Alpha-conotoxins EpI and AuIB switch subtype selectivity and activity in native versus recombinant nicotinic acetylcholine receptors
    Annette Nicke
    Institute for Molecular Bioscience, University of Queensland, Brisbane, QLD 4072, Australia
    FEBS Lett 554:219-23. 2003
    ..These results indicate that as yet unidentified factors influence alpha-conotoxin pharmacology at native versus oocyte-expressed nAChRs...
  41. ncbi A second extracellular site is required for norepinephrine transport by the human norepinephrine transporter
    Ching I A Wang
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, Brisbane, Queensland, Australia
    Mol Pharmacol 82:898-909. 2012
    ..Our findings are consistent with a multistep model of substrate transport by NET, for which a second, shallow extracellular NE substrate site (NESS-2) is required for efficient NE transport by NET...
  42. ncbi Conotoxin engineering: dual pharmacophoric noradrenaline transport inhibitor/integrin binding peptide with improved stability
    Zoltan Dekan
    Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Queensland, Australia
    Org Biomol Chem 10:5791-4. 2012
    ....
  43. ncbi Chemical synthesis and structure of the prokineticin Bv8
    Rodrigo A V Morales
    Institute for Molecular Bioscience, The University of Queensland, 306 Carmody Road, St Lucia, Brisbane, Australia
    Chembiochem 11:1882-8. 2010
    ....
  44. ncbi α-Conotoxin ImI incorporating stable cystathionine bridges maintains full potency and identical three-dimensional structure
    Zoltan Dekan
    Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Queensland, Australia
    J Am Chem Soc 133:15866-9. 2011
    ..The effect of oxidation of the thioethers to sulfoxides was also investigated, with significant changes in the biological activities observed ranging from a >30-fold reduction (2S═O) to a 3-fold increase (3S═O(B)) in potencies...
  45. ncbi Multiple ciguatoxins present in Indian Ocean reef fish
    Brett Hamilton
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, Brisbane, QLD 4072, Australia
    Toxicon 40:1347-53. 2002
    ..The ratio of CTX-1 and -2 varied depending on the fish extract being analysed. These results suggest that I-CTX-1 and -2 may arise from separate dinoflagellate precursors that may be oxidatively biotransformed to I-CTX-3 and -4 in fish...
  46. ncbi Modulating oxytocin activity and plasma stability by disulfide bond engineering
    Markus Muttenthaler
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, Brisbane, Queensland
    J Med Chem 53:8585-96. 2010
    ..By contrast, the all-D-oxytocin and head to tail cyclic oxytocin analogues, while significantly more stable with half-lives greater than 48 h, had little or no detectable binding or functional activity...
  47. ncbi Towards an integrated venomics approach for accelerated conopeptide discovery
    Jutty Rajan Prashanth
    The Institute for Molecular Bioscience, The University of Queensland, St Lucia, Queensland 4072, Australia
    Toxicon 60:470-7. 2012
    ..In this review, we also highlight the challenges associated with the wealth of data generated with this integrated approach and briefly discuss the impact these methods could have on the field of toxinology...
  48. ncbi Isolation and characterisation of conomap-Vt, a D-amino acid containing excitatory peptide from the venom of a vermivorous cone snail
    Sebastien Dutertre
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, 4072 QLD, Australia
    FEBS Lett 580:3860-6. 2006
    ..Interestingly, the isomerization of L-Phe to D-Phe enhanced biological activity, suggesting that this post-translational modified conopeptide may have evolved for prey capture...
  49. ncbi Computational approaches to understand alpha-conotoxin interactions at neuronal nicotinic receptors
    Sebastien Dutertre
    Institute for Molecular Bioscience, University of Queensland, Brisbane, Queensland, Australia
    Eur J Biochem 271:2327-34. 2004
    ..An accurate determination of their binding modes on the neuronal nAChR may allow the rational design of alpha-conotoxin-based ligands with novel nAChR selectivity...
  50. ncbi Toxin insights into nicotinic acetylcholine receptors
    Sebastien Dutertre
    Institute for Molecular Bioscience, The University of Queensland, Brisbane, QLD 4072, Australia
    Biochem Pharmacol 72:661-70. 2006
    ..In this commentary, we review the structural data on nAChR-toxin interactions and discuss their implications for the design of novel ligands acting at the nAChR...
  51. ncbi Characterisation of Na(v) types endogenously expressed in human SH-SY5Y neuroblastoma cells
    Irina Vetter
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, Australia
    Biochem Pharmacol 83:1562-71. 2012
    ..7-selective response, confirming that endogenously expressed human Na(v)1.7 in SH-SY5Y cells is functional and can be synergistically activated, providing a new assay format for ligand screening...
  52. ncbi Conopressin-T from Conus tulipa reveals an antagonist switch in vasopressin-like peptides
    Sebastien Dutertre
    Institute for Molecular Bioscience, University of Queensland, Brisbane, Queensland 4072, Australia
    J Biol Chem 283:7100-8. 2008
    ..NMR structures of both conopressin-T and L7P analogue revealed a marked difference in the orientation of the exocyclic tripeptide that may serve as templates for the design of novel ligands with enhanced affinity for the V 1a receptor...
  53. ncbi Omega-conotoxin GVIA mimetics based on an anthranilamide core: effect of variation in ammonium side chain lengths and incorporation of fluorine
    Asa Andersson
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia
    Bioorg Med Chem 17:6659-70. 2009
    ..The introduction of a fluoro substituent into the tyrosine mimic produced the most active compound prepared in this study (2g), with an EC(50) at rat brain Ca(v)2.2 channels of 6 microM...
  54. ncbi Overexpressed Ca(v)beta3 inhibits N-type (Cav2.2) calcium channel currents through a hyperpolarizing shift of ultra-slow and closed-state inactivation
    Takahiro Yasuda
    The University of Queensland, Queensland 4072, Australia
    J Gen Physiol 123:401-16. 2004
    ....
  55. ncbi Isolation, structure, and activity of GID, a novel alpha 4/7-conotoxin with an extended N-terminal sequence
    Annette Nicke
    Institute for Molecular Bioscience and School of Biomedical Sciences, University of Queensland, Brisbane, Queensland 4072, Australia
    J Biol Chem 278:3137-44. 2003
    ....
  56. ncbi Anti-allodynic efficacy of the chi-conopeptide, Xen2174, in rats with neuropathic pain
    Carsten K Nielsen
    School of Pharmacy, The University of Queensland, Brisbane, QLD, Australia
    Pain 118:112-24. 2005
    ..Xen2174 appears to be a promising candidate for development as a novel therapeutic for i.t. administration to patients with persistent neuropathic pain...
  57. ncbi Isolation and characterization of peptides from Momordica cochinchinensis seeds
    Lai Y Chan
    The University of Queensland, Institute for Molecular Bioscience, Brisbane QLD 4072, Australia
    J Nat Prod 72:1453-8. 2009
    ..Of the cell lines tested, MCoCC-1 is the most toxic against a human melanoma cell line (MM96L) and is nonhemolytic to human erythrocytes. The role of these peptides within the plant remains to be determined...
  58. ncbi Characterization of endogenous calcium responses in neuronal cell lines
    Irina Vetter
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, Queensland 4072, Australia
    Biochem Pharmacol 79:908-20. 2010
    ....
  59. ncbi Emerging structure-function relationships defining monoamine NSS transporter substrate and ligand affinity
    Ching I Anderson Wang
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, Brisbane, Australia
    Biochem Pharmacol 79:1083-91. 2010
    ....
  60. ncbi Venom Peptide modulators of the immune system
    Marco C Inserra
    The University of Queensland, Institute for Molecular Bioscience, Brisbane 4072, Australia
    Inflamm Allergy Drug Targets 10:399-410. 2011
    ..This review highlights venom peptides with potential to act at immunological targets within the mammalian immune system...
  61. ncbi Oral absorption and in vivo biodistribution of alpha-conotoxin MII and a lipidic analogue
    Joanne T Blanchfield
    School of Molecular and Microbial Sciences, The University of Queensland, Brisbane 4072, Australia
    Biochem Biophys Res Commun 361:97-102. 2007
    ..Neither peptide crossed the blood-brain barrier to any significant extent. This is the first study of the in vivo biodistribution of an alpha-conotoxin after oral administration...
  62. ncbi Omega-conotoxin CVID inhibits a pharmacologically distinct voltage-sensitive calcium channel associated with transmitter release from preganglionic nerve terminals
    David J Adams
    School of Biomedical Sciences, The University of Queensland, Brisbane, Australia
    J Biol Chem 278:4057-62. 2003
    ..Bosey, G. M., Snutch, T. P., and Zamponi, G. W. (2001) J. Biol. Chem. 276, 15728-15735), it is likely that the calcium channel in preganglionic nerve terminals targeted by CVID is a N-type (Ca(v)2.2) calcium channel variant...
  63. ncbi Deep venomics reveals the mechanism for expanded peptide diversity in cone snail venom
    Sebastien Dutertre
    The Institute for Molecular Bioscience, The University of Queensland, St Lucia, Queensland 4072, Australia
    Mol Cell Proteomics 12:312-29. 2013
    ..Variable peptide processing is expected to contribute to the evolution of venoms, and explains how a limited set of ∼ 100 gene transcripts can generate thousands of conopeptides in a single species of cone snail...
  64. ncbi Emerging opportunities for allosteric modulation of G-protein coupled receptors
    Ching I Anderson Wang
    Institute for Molecular Bioscience, University of Queensland, Brisbane, QLD 4072 Australia
    Biochem Pharmacol 85:153-62. 2013
    ..This analysis has identified a new extracellular salt bridge (ESB-2) that might be exploited in the design of allosteric modulators...
  65. ncbi Human fatality associated with Pacific ciguatoxin contaminated fish
    Brett Hamilton
    The Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Queensland, Australia
    Toxicon 56:668-73. 2010
    ..This study confirms the potential of tropical reef fish to accumulate sufficient P-CTX to be lethal to humans, especially if the liver and viscera are consumed as part of the meal...
  66. ncbi Cloning and characterisation of natriuretic peptides from the venom glands of Australian elapids
    Liam St Pierre
    The Queensland Institute of Medical Research, Brisbane, Australia
    Biochimie 88:1923-31. 2006
    ..The data presented in this study represent a significant resource for understanding the role of various natriuretic peptides isoforms during the envenomation process by Australian elapid snakes...
  67. ncbi Isolation and characterisation of Indian Ocean ciguatoxin
    Brett Hamilton
    Institute for Molecular Bioscience and ARC Special Research Centre for Functional and Applied Genomics, The University of Queensland, St Lucia, Brisbane, QLD 4072, Australia
    Toxicon 40:685-93. 2002
    ..Taken together, these results indicate that I-CTX is a new ciguatoxin (CTX) responsible for ciguatera caused by reef fish in the Indian Ocean...
  68. ncbi Natural product ligands of TRP channels
    Irina Vetter
    Institute for Molecular Bioscience, The University of Queensland, Queensland 4072, Australia
    Adv Exp Med Biol 704:41-85. 2011
    ....
  69. ncbi Spermine modulation of the glutamate(NMDA) receptor is differentially responsive to conantokins in normal and Alzheimer's disease human cerebral cortex
    Lotten Ragnarsson
    Department of Biochemistry, University of Queensland, Brisbane 4072, Australia
    J Neurochem 81:765-79. 2002
    ..Modified conantokins are useful for identifying the NMDA receptors involved, and may have potential as protective agents...
  70. ncbi Remarkable inter- and intra-species complexity of conotoxins revealed by LC/MS
    Jasmine Davis
    The University of Queensland, Institute for Molecular Biosciences, Brisbane Q4072, Australia
    Peptides 30:1222-7. 2009
    ..Given this inherent diversity and variability, more sensitive bioassays and sequencing techniques will be required to fully explore conotoxin bioactivity...
  71. ncbi Phorbasins G-K: new cytotoxic diterpenes from a southern Australian marine sponge, Phorbas sp
    Hua Zhang
    Institute for Molecular Bioscience, The University of Queensland, St Lucia, Queensland 4072, Australia
    Org Biomol Chem 6:3811-5. 2008
    ..A preliminary structure activity relationship (SAR) evaluation based on the co-metabolites phorbasins B-K () revealed aspects of the phorbasin pharmacophore...
  72. ncbi Isolation and characterization of a cone snail protease with homology to CRISP proteins of the pathogenesis-related protein superfamily
    Trudy J Milne
    Institute for Molecular Bioscience, The University of Queensland, Queensland 4072, Australia
    J Biol Chem 278:31105-10. 2003
    ..Thus, it is possible that other PR proteins may also be substrate-specific proteases...
  73. ncbi Ciguatoxin-induced catecholamine secretion in bovine chromaffin cells: mechanism of action and reversible inhibition by brevenal
    Truong D Nguyen-Huu
    Queensland Brain Institute and School of Biomedical Sciences, The University of Queensland, St Lucia Campus, Brisbane, Australia
    Toxicon 56:792-6. 2010
    ..This effect is partially reversible. Our results therefore raise the prospect of finding functional antagonists for P-CTX-1B that could be useful for the treatment of ciguatera...
  74. ncbi The novel N-type calcium channel blocker, AM336, produces potent dose-dependent antinociception after intrathecal dosing in rats and inhibits substance P release in rat spinal cord slices
    Maree T Smith
    School of Pharmacy, The University of Queensland, St Lucia, Queensland, Brisbane, Australia
    Pain 96:119-27. 2002
    ....
  75. ncbi Identification of slow and fast-acting toxins in a highly ciguatoxic barracuda (Sphyraena barracuda) by HPLC/MS and radiolabelled ligand binding
    Ivannah Pottier
    Laboratoire de Microbiologie Alimentaire USC INRA, Universite de Caen, Esplanade de la Paix, Caen 14032, France
    Toxicon 42:663-72. 2003
    ..However, FAT active on VSSCs and < 900 Da were suspected to contribute to the overall toxicity...
  76. ncbi Synthesis and biological evaluation of nonpeptide mimetics of omega-conotoxin GVIA
    Jonathan B Baell
    Biomolecular Research Institute, 343 Royal Parade, Parkville, Victoria 3052, Australia
    Bioorg Med Chem 12:4025-37. 2004
    ..1 microM) showed a greater than 25-fold selectivity for the N-type channel...
  77. ncbi Neuroprotectant effects of iso-osmolar D-mannitol to prevent Pacific ciguatoxin-1 induced alterations in neuronal excitability: a comparison with other osmotic agents and free radical scavengers
    Liesl C Birinyi-Strachan
    Neurotoxin Research Group, Department of Health Sciences, University of Technology, Sydney, Broadway, NSW, Australia
    Neuropharmacology 49:669-86. 2005
    ....
  78. ncbi Block of voltage-gated potassium channels by Pacific ciguatoxin-1 contributes to increased neuronal excitability in rat sensory neurons
    Liesl C Birinyi-Strachan
    Neurotoxin Research Group, Department of Health Sciences, University of Technology, Sydney, Broadway NSW, Australia
    Toxicol Appl Pharmacol 204:175-86. 2005
    ..These data indicate that a block of potassium channels contributes to the increase in neuronal excitability, associated with a modulation of Nav channel gating, observed clinically in response to ciguatera poisoning...
  79. ncbi Differential involvement of N-type calcium channels in transmitter release from vasoconstrictor and vasodilator neurons
    Judy L Morris
    Department of Anatomy and Histology, Centre for Neuroscience, Flinders University, GPO Box 2100, Adelaide, SA 5001, Australia
    Br J Pharmacol 141:961-70. 2004
    ..N-type channels are responsible for transmitter release from vasoconstrictor neurons innervating a muscular artery and capacitance vein, but only partly mediate release of nitric oxide and neuropeptides from pelvic vasodilator neurons...
  80. ncbi Alpha-conotoxins as tools for the elucidation of structure and function of neuronal nicotinic acetylcholine receptor subtypes
    Annette Nicke
    Max Planck Institute for Brain Research, Frankfurt, Germany
    Eur J Biochem 271:2305-19. 2004
    ....
  81. ncbi Characterisation of multiple Caribbean ciguatoxins and congeners in individual specimens of horse-eye jack (Caranx latus) by high-performance liquid chromatography/mass spectrometry
    Ivannah Pottier
    Laboratoire de Microbiologie Alimentaire, Universite de Caen, Esplanade de la Paix, 14032 Caen Cedex, France
    Toxicon 40:929-39. 2002
    ..A possible conversion of C-CTX-1 into C-CTX-1a was identified when flesh was cooked, without changes in toxicity. In conclusion, HPLC/MS characterised 12 C-CTXs accumulated by C. latus at variable levels...
  82. ncbi A comparison of capillary-scale LC-NMR with alternative techniques: spectroscopic and practical considerations
    Richard J Lewis
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough, UK
    Magn Reson Chem 43:783-9. 2005
    ..For many real samples, however, the loading is limiting and we found the combination of LC-SPE-MS-NMR with a cryoprobe enables more material to be purified for NMR analysis, while retaining sensitivity...
  83. ncbi Ability of some plant extracts, traditionally used to treat ciguatera fish poisoning, to prevent the in vitro neurotoxicity produced by sodium channel activators
    Raphaële Boydron-Le Garrec
    Laboratoire de Pharmacochimie des Substances Naturelles et Pharmacophores Redox, UMR 152, IRD Université Paul Sabatier, Centre IRD de Noumea, BP A5, 98848 Noumea, New Caledonia
    Toxicon 46:625-34. 2005
    ....
  84. ncbi Probing the structural basis for the difference in thermostability displayed by family 10 xylanases
    Hefang Xie
    The Department of Animal Science, Rongchang Campus, Southwest University, The People s Republic of China, 402460
    J Mol Biol 360:157-67. 2006
    ..The enzymes were more active against AX3 than xylotriose, providing evidence that the arabinose side-chain makes a generic contribution to substrate recognition by GH10 xylanases...
  85. ncbi Differential antagonism by conotoxin rho-TIA of contractions mediated by distinct alpha1-adrenoceptor subtypes in rat vas deferens, spleen and aorta
    Vanessa Lima
    Department of Pharmacology, , UNESP, Botucatu, SP 18618-000, Brazil
    Eur J Pharmacol 508:183-92. 2005
    ..It is concluded that rho-TIA will be useful for distinguishing the role of particular alpha1-adrenoceptor subtypes in native tissues...
  86. ncbi The role of group I metabotropic glutamate receptors in neuronal excitotoxicity in Alzheimer's disease
    Vicky W-W Tsai
    School of Molecular and Microbial Sciences and Institute for Molecular Bioscience, University of Queensland, Brisbane 4072 Australia
    Neurotox Res 7:125-41. 2005
    ..They represent a pharmacological path to a relatively subtle amelioration of neurotoxicity because they serve a modulatory rather than a direct role in excitatory glutamatergic transmission...
  87. ncbi Functional and structural characterization of RsbU, a stress signaling protein phosphatase 2C
    Olivier Delumeau
    Microbiology Unit and Laboratory of Molecular Biophysics, Department of Biochemistry, University of Oxford, Oxford OX1 3QU, United Kingdom
    J Biol Chem 279:40927-37. 2004
    ..quot; Finally, the molecular basis of kinase recruitment by the RsbU phosphatase is discussed by comparing RsbU sequences from bacteria that either possess or lack RsbT...
  88. ncbi Optimization of monocarboxylate transporter 1 blockers through analysis and modulation of atropisomer interconversion properties
    Simon D Guile
    Department of Medicinal Chemistry, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, LE11 5RH, UK
    J Med Chem 50:254-63. 2007
    ..This led to the design of compounds with increased rates of rotamer interconversion. Moreover, some of these compounds also showed improved potency and provided a route to further optimization...
  89. ncbi Which hydroxy? Evidence for species differences in the regioselectivity of glucuronidation in rat, dog, and human in vitro systems and dog in vivo
    Iain J Martin
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, LE11 5RH, UK
    Drug Metab Dispos 34:1502-7. 2006
    ..A clear qualitative species difference in the glucuronidation of AZ11939714 has been demonstrated in vitro. This may have implications for the choice of laboratory species to study the pharmacokinetics and safety of this compound...
  90. ncbi Auxiliary subunit regulation of high-voltage activated calcium channels expressed in mammalian cells
    Takahiro Yasuda
    Department of Physiology and Biophysics, Cellular and Molecular Neurobiology Research Group, University of Calgary, 3330 Hospital Dr. NW, Calgary, T2N 4 N1, Canada
    Eur J Neurosci 20:1-13. 2004
    ..Moreover, the effects of each auxiliary subunit on whole cell conductance and channel gating appear to be specifically tailored to subsets of calcium channel subtypes...
  91. ncbi Subtype-selective noncompetitive or competitive inhibition of human alpha1-adrenergic receptors by rho-TIA
    Zhongjian Chen
    Department of Pharmacology, Emory University School of Medicine, Atlanta, Georgia 30322, USA
    J Biol Chem 279:35326-33. 2004
    ..These differential interactions do not involve the receptor amino termini and are not because of the charged nature of the peptide, and isoleucine 8 is critical for its noncompetitive inhibition at alpha(1B)-ARs...
  92. ncbi Understanding the structural basis for substrate and inhibitor recognition in eukaryotic GH11 xylanases
    Maria Vardakou
    Institute for Cell and Molecular Biosciences, Newcastle University, The Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, UK
    J Mol Biol 375:1293-305. 2008
    ..Finally, the crystal structure of NpXyn11A shows that the resistance of the enzyme to XIP-I is not due solely to insertions in the loop connecting beta strands 11 and 12, as suggested previously, but is highly complex...
  93. ncbi Crystal structure of a cellulosomal family 3 carbohydrate esterase from Clostridium thermocellum provides insights into the mechanism of substrate recognition
    Márcia A S Correia
    CIISA Faculdade de Medicina Veterinaria, Universidade Tecnica de Lisboa, Avenida da Universidade Tecnica, 1300 477 Lisboa, Portugal
    J Mol Biol 379:64-72. 2008
    ..The acetate moiety is accommodated in a hydrophobic pocket and the negative charge of the tetrahedral transition state is stabilized through hydrogen bonds with the backbone N of Ser44 and Gly95 and the side-chain amide of Asn124...
  94. ncbi NMR identification of an S-linked glucuronide of a triazole thione formed in vitro
    Iain J Martin
    Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Bakewell Road, Loughborough, LE11 5RH, UK
    Drug Metab Dispos 31:694-6. 2003
    ..Full NMR data on this unusual metabolite is presented. Substitution or replacement of the sulfur atom resulted in a significant decrease in the observed rate of glucuronidation...