Article
Biochemistry & Molecular Biology
Luis Felipe Santos Menezes, Mariza Mendanha Maranha, Diogo Vieira Tibery, Adolfo Carlos Barros de Souza, Daniel Oliveira da Mata, Leandro Ambrosio Campos, Amanda Araujo Souza, Sonia Maria de Freitas, Elisabeth Ferroni Schwartz
Summary: Ts17, purified from the venom of Tityus serrulatus, showed beta-toxin activity by altering the kinetics of Nav1.1-Nav1.7 channels. Nav1.2 and Nav1.5 were the most affected subtypes. Circular dichroism spectra revealed a predominance of beta-sheet and unordered structures in Ts17 at all pHs, with the highest alpha-helix content observed at pH 4.0 (13.3%).
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
(2023)
Article
Biochemistry & Molecular Biology
Pavel Andrei Montero-Dominguez, Gerardo Corzo
Summary: This study investigates the interaction mechanism between scorpion beta-neurotoxins and the human sodium channel. Computational techniques were used to reveal that the toxins bind to specific regions of the sodium channel, leading to voltage sensor entrapment.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Jie Yu, Hongtao Zhu, Remigijus Lape, Timo Greiner, Juan Du, Wei Lu, Lucia Sivilotti, Eric Gouaux
Summary: Using electrophysiology and cryo-EM reconstructions, this study investigated the mechanism of partial agonist action on neurotransmitter receptors, revealing new conformational states along the receptor reaction pathway. The results demonstrated that partial agonists can occupy closed channel states bound by agonists, affecting the receptor channel's open probability.
Article
Biochemical Research Methods
Ana Carolina Martins Magalha, Carlos Jose Correia de Santana, Rafael D. Melani, Gilberto B. Domont, Mariana S. Castro, Wagner Fontes, Peter Roepstorff, Osmindo Rodrigues Pires Junior
Summary: In this study, the composition of venom proteins from the scorpion Rhopalurus agamemnon was explored, and 230 proteins were identified, including new enzyme reports. These findings highlight the unique diversity of venom proteins from the scorpion R. agamemnon, offering insights into new mechanisms of envenomation and expanding the protein database of scorpion venoms. The discovery of new proteins opens up possibilities for the development of new drugs and suggests potential molecular targets for venom components.
JOURNAL OF PROTEOMICS
(2021)
Article
Pharmacology & Pharmacy
Minzhi Chen, Minjuan Lu, Xujun Feng, Meijing Wu, Xiaoqing Luo, Ruiqi Xiang, Ren Luo, Hang Wu, Zhonghua Liu, Meichi Wang, Xi Zhou
Summary: Polypeptide toxins are bioactive components in venomous animals that can specifically act on targets in the nervous, muscle, and cardiovascular systems. A novel polypeptide toxin, LmNaTx15, was isolated from scorpion venom and shown to have a modulatory effect on specific Nav channel subtypes and induce pain in mice.
Article
Biochemistry & Molecular Biology
Boris S. Zhorov, Yuzhe Du, Weizhong Song, Ningguang Luo, Dalia Gordon, Michael Gurevitz, Ke Dong
Summary: This study investigated the interaction between insect-selective scorpion depressant beta-toxins and the Blattella germanica sodium channel, revealing the specific mechanisms by which these toxins affect channel sensitivity through mutations, electrophysiology, and structural modeling. The findings highlighted the importance of certain residues in the voltage-sensing domain II for toxin sensitivity and provided insights into the structural basis of the interaction between the toxins and the sodium channel.
BIOCHEMICAL JOURNAL
(2021)
Article
Biochemistry & Molecular Biology
Daniel Oliveira da Mata, Diogo Vieira Tibery, Matheus F. Fernandes-Pedrosa, Elisabeth Ferroni Schwartz
Summary: This study characterized the modulation of hNa+-channels by Tst1, a peptide purified from the venom of Tityus stigmurus scorpion. Tst1 inhibited Nav 1.3, Nav 1.2, and Nav 1.4 channels, and affected the activation voltage, steady-state inactivation, and recovery from inactivation of the channels. The effect of Tst1 on Nav 1.3 was dose-dependent.
Article
Anesthesiology
Wuguang Lu, Xiaoyang Cheng, Jiao Chen, Mingyuan Wang, Yonggen Chen, Jinman Liu, Ming Sang, Ningwei Zhao, Huaijiang Yan, Xiaolan Cheng, Qian Zhou, Juan Ye, Jin Wang, Erjin Xu, Zongxiang Tang, Xi Zhou, Mingqiang Rong, Erik A. Nilsen, Sulayman D. Dib-Hajj, Stephen G. Waxman, Ye Yu, Peng Cao
Summary: Na(v)1.7 plays a crucial role in pain perception. The study reveals that Buthus martensii Karsch scorpion venom enhances Na(v)1.7 activity, leading to pain responses. Additionally, the key structural elements and interactions between scorpion toxins and Na(v)1.7 are identified.
Article
Biochemistry & Molecular Biology
Mohammad Ali Bayatzadeh, Abbas Zare Mirakabadi, Nahid Babaei, Abdolhassan Doulah, Abbas Doosti
Summary: This study successfully constructed the toxin peptide and plasmid containing the gene coding for mammalian toxin AnCra1, achieving efficient expression and purification in Escherichia coli. The recombinant AnCra1 selectively inhibits the fast inactivation of hNav1.7 channel, demonstrating its potential as a tool for studying ion channel function and physiological responses.
MOLECULAR BIOLOGY REPORTS
(2021)
Article
Food Science & Technology
Aimee Bowman, Chloe Fitzgerald, Jeff F. Pummill, Douglas D. Rhoads, Tsunemi Yamashita
Summary: This study shows that venom toxicity in scorpion populations may be affected by toxin gene diversity, specific toxin transcript variation, and subsequent protein production, highlighting the importance of understanding the molecular constituents of scorpion venom.
Article
Chemistry, Medicinal
Shana L. Geffeney, Jennie Ann Cordingley, Kenyon Mitchell, Charles T. Hanifin
Summary: Multiple animal species have developed resistance to the neurotoxin tetrodotoxin (TTX) by altering the amino acid substitutions in voltage-gated sodium ion channels (VGSCs). This study demonstrates that positionally convergent substitutions of amino acids do not generate similar patterns among TTX-resistant animal lineages, suggesting that flexibility and movement of the protein may play a greater role in causing changes in TTX block.
Article
Clinical Neurology
Andrea Cippitelli, Gilles Zribi, Lawrence Toll
Summary: PPL-103 has shown potential as a pharmacotherapy for the treatment of cocaine use disorder (CUD). It reduces self-administration of cocaine, decreases motivation for cocaine, and attenuates binge-like cocaine taking. PPL-103 also reduces priming- and cue-induced reinstatement of cocaine seeking. Tolerance development was not observed with repeated PPL-103 treatment.
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
(2022)
Article
Neurosciences
Ran Yang, Yongbo Song, Haipeng Wang, Chunyun Chen, Fei Bai, Chunli Li
Summary: This study evaluates the antinociceptive effect of DKK13 on trigeminal neuralgia in rats. The results show that DKK13 significantly increases pain thresholds and inhibits pain-related behavioral activities in rats. It also alters the characteristics of the Nav1.8 channel and the phosphorylation levels of proteins in the MAPKs/CREB signaling pathway.
MOLECULAR NEUROBIOLOGY
(2022)
Review
Toxicology
Sylvie Diochot
Summary: The toxins from spiders and scorpions can affect the activity of ion channels, with some able to relieve pain, providing a potential basis for future analgesic development. Some toxins have been shown to impact pain modalities in animal models, revealing the role of these channels in the pain process. The interaction of gating-modifier toxins with membrane phospholipids near ion channels is also examined.
JOURNAL OF VENOMOUS ANIMALS AND TOXINS INCLUDING TROPICAL DISEASES
(2021)
Article
Dermatology
Renata Lucas, Johanna Mihaly, Janine Gericke, Angel R. de Lera, Susana Alvarez, Zsuzsanna Veleczki, Daniel Torocsik, Ralph Ruhl
Summary: The study found that providing vitamin D receptor antagonist/partial agonist to mouse skin can lead to epidermal hyperproliferation, which is mediated by increased retinoic acid synthesis and RAR gamma pathways.