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Selective spider toxins reveal a role for Nav1.1 channel in mechanical pain
TLDR
This work identifies and characterize spider (Heteroscodra maculata) toxins that selectively activate the Nav1.1 subtype, and establishes an unexpected role for Nav 1.1 channels in regulating the excitability of sensory nerve fibres that mediate mechanical pain.
Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain
TLDR
A novel mouse model of NaV1.7-mediated pain based on intraplantar injection of the scorpion toxin OD1 is suitable for the rapid in vivo characterization of the analgesic efficacy of Na.7 inhibitors and significantly reduced OD1-induced spontaneous pain when delivered locally and systemically.
Pharmacological characterisation of the highly NaV1.7 selective spider venom peptide Pn3a
TLDR
The results suggest that in inflammatory models, acute administration of peripherally restricted NaV1.7 inhibitors can only produce analgesia when administered in combination with an opioid.
Anti-allodynic effects of the selective NaV1.7 inhibitor Pn3a in a mouse model of acute post-surgical pain: evidence for analgesic synergy with opioids and baclofen.
TLDR
Findings suggest that pain after surgery can be successfully treated with NaV1.7 inhibitors alone or in combination with baclofen or opioids, which may present a novel and safe treatment strategy for this frequent and poorly managed condition.
α-Conotoxin ImI incorporating stable cystathionine bridges maintains full potency and identical three-dimensional structure.
TLDR
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 to investigate the effect of oxidation of the thio ethers to sulfoxides.
Identification and Characterization of ProTx-III [μ-TRTX-Tp1a], a New Voltage-Gated Sodium Channel Inhibitor from Venom of the Tarantula Thrixopelma pruriens
TLDR
Tp1a proved to be analgesic by reversing spontaneous pain induced in mice by intraplantar injection in OD1, a scorpion toxin that potentiates hNaV1.7.
Isolation, characterization and total regioselective synthesis of the novel μO-conotoxin MfVIA from Conus magnificus that targets voltage-gated sodium channels.
TLDR
A novel regioselective approach is developed for the synthesis of μO-conotoxins that will facilitate the optimization of μ O-conOToxins as novel analgesic molecules to improve pain management.
A Tarantula-Venom Peptide Antagonizes the TRPA1 Nociceptor Ion Channel by Binding to the S1–S4 Gating Domain
TLDR
Protoxin-I (ProTx-I), a 35-residue peptide from the venom of the Peruvian green-velvet tarantula, Thrixopelma pruriens, is identified as the first known high-affinity peptide TRPA1 antagonist, establishing the approach, which is termed "toxineering," as a generally applicable method for isolation of novel ion channel modifiers and design of ion channel modifying with altered specificity.
Modulating oxytocin activity and plasma stability by disulfide bond engineering.
TLDR
Eleven analogues of oxytocin were synthesized including disulfide bond replacements by thioether, selenylsulfide, diselenide, and ditelluride bridges, and their stabilities in human plasma and activity at the human Oxytocin receptor were assessed.
Modulatory features of the novel spider toxin μ‐TRTX‐Df1a isolated from the venom of the spider Davus fasciatus
TLDR
Spider venoms are investigated for new inhibitors of voltage‐gated sodium channels in the pursuit of novel NaV modulators in order to develop new therapies for chronic pain.
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