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- Publications
- Influence
Selective spider toxins reveal a role for Nav1.1 channel in mechanical pain
- Jeremiah D. Osteen, V. Herzig, +17 authors David Julius
- Chemistry, Medicine
- Nature
- 13 April 2016
Voltage-gated sodium (Nav) channels initiate action potentials in most neurons, including primary afferent nerve fibres of the pain pathway. Local anaesthetics block pain through non-specific actions… Expand
Pharmacological characterisation of the highly NaV1.7 selective spider venom peptide Pn3a
- Jennifer R Deuis, Z. Dekan, +18 authors I. Vetter
- Medicine
- Scientific reports
- 20 January 2017
Human genetic studies have implicated the voltage-gated sodium channel NaV1.7 as a therapeutic target for the treatment of pain. A novel peptide, μ-theraphotoxin-Pn3a, isolated from venom of the… Expand
Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain
- Jennifer R Deuis, Joshua S. Wingerd, +10 authors I. Vetter
- Medicine
- Toxins
- 1 March 2016
Loss-of-function mutations of NaV1.7 lead to congenital insensitivity to pain, a rare condition resulting in individuals who are otherwise normal except for the inability to sense pain, making… Expand
α-Conotoxin ImI incorporating stable cystathionine bridges maintains full potency and identical three-dimensional structure.
- Z. Dekan, I. Vetter, N. Daly, D. Craik, R. Lewis, P. Alewood
- Chemistry, Medicine
- Journal of the American Chemical Society
- 15 September 2011
The two disulfide bonds of α-conotoxin ImI, a peptide antagonist of the α7 nicotinic acetylcholine receptor (nAChR), were systematically replaced with isosteric redox-stable cystathionine thioethers.… Expand
Isolation, characterization and total regioselective synthesis of the novel μO-conotoxin MfVIA from Conus magnificus that targets voltage-gated sodium channels.
- I. Vetter, Z. Dekan, O. Knapp, David John Adams, P. Alewood, R. Lewis
- Chemistry, Medicine
- Biochemical pharmacology
- 15 August 2012
The μO-conotoxins are notable for their unique selectivity for Na(v)1.8 over other sodium channel isoforms, making them attractive drug leads for the treatment of neuropathic pain. We describe the… Expand
A Tarantula-Venom Peptide Antagonizes the TRPA1 Nociceptor Ion Channel by Binding to the S1–S4 Gating Domain
- Junhong Gui, Boyi Liu, +11 authors M. Nitabach
- Biology, Medicine
- Current Biology
- 3 March 2014
BACKGROUND
The venoms of predators have been an excellent source of diverse highly specific peptides targeting ion channels. Here we describe the first known peptide antagonist of the nociceptor ion… Expand
Modulating oxytocin activity and plasma stability by disulfide bond engineering.
- Markus Muttenthaler, Å. Andersson, Aline D. de Araujo, Z. Dekan, Richard J. Lewis, Paul F. Alewood
- Chemistry, Medicine
- Journal of medicinal chemistry
- 30 November 2010
Disulfide bond engineering is an important approach to improve the metabolic half-life of cysteine-containing peptides. Eleven analogues of oxytocin were synthesized including disulfide bond… Expand
Selenoether oxytocin analogues have analgesic properties in a mouse model of chronic abdominal pain.
- A. D. de Araujo, M. Mobli, +9 authors P. Alewood
- Chemistry, Medicine
- Nature communications
- 30 January 2014
Poor oral availability and susceptibility to reduction and protease degradation is a major hurdle in peptide drug development. However, drugable receptors in the gut present an attractive niche for… Expand
Identification and Characterization of ProTx-III [μ-TRTX-Tp1a], a New Voltage-Gated Sodium Channel Inhibitor from Venom of the Tarantula Thrixopelma pruriens
- F. Cardoso, Z. Dekan, +7 authors R. Lewis
- Chemistry, Medicine
- Molecular Pharmacology
- 1 August 2015
Spider venoms are a rich source of ion channel modulators with therapeutic potential. Given the analgesic potential of subtype-selective inhibitors of voltage-gated sodium (NaV) channels, we screened… Expand
Modulatory features of the novel spider toxin μ‐TRTX‐Df1a isolated from the venom of the spider Davus fasciatus
- F. Cardoso, Z. Dekan, +6 authors R. Lewis
- Biology, Medicine
- British journal of pharmacology
- 1 August 2017
Naturally occurring dysfunction of voltage‐gated sodium (NaV) channels results in complex disorders such as chronic pain, making these channels an attractive target for new therapies. In the pursuit… Expand