Article
Biology
Lauren M. Ashwood, Khaled A. Elnahriry, Zachary K. Stewart, Thomas Shafee, Muhammad Umair Naseem, Tibor G. Szanto, Chloe A. van der Burg, Hayden L. Smith, Joachim M. Surm, Eivind A. B. Undheim, Bruno Madio, Brett R. Hamilton, Shaodong Guo, Dorothy C. C. Wai, Victoria L. Coyne, Matthew J. Phillips, Kevin J. Dudley, David A. Hurwood, Gyorgy Panyi, Glenn F. King, Ana Pavasovic, Raymond S. Norton, Peter J. Prentis
Summary: This study reveals the unique gene family SA8 in Actiniarians, which has therapeutic potential similar to the ShK toxin from Stichodactyla helianthus. The genomic arrangement and expression patterns of SA8 in Actinia tenebrosa and Telmatactis stephensoni were characterized, and the structure and function of SA8 in T. stephensoni venom were examined.
Article
Zoology
Fu-Chu Yuan, Fu-De Sun, Lin Zhang, Biao Huang, Hai-Long An, Ming-Qiang Rong, Can-Wei Du
Summary: Various peptide toxins in animal venom, including Nay-targeting spider toxin (NaSpTx) Family I, can inhibit voltage-gated sodium ion channel Nav1.7. This study investigated the binding properties of NaSpTx Family I toxins using Mu-theraphotoxin-Ca2a (Ca2a) as a template and identified the key residues involved in binding to Nav1.7.
ZOOLOGICAL RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Yashad Dongol, Phil M. Choi, David T. Wilson, Norelle L. Daly, Fernanda C. Cardoso, Richard J. Lewis
Summary: Through screening Australian spider venom, a peptide inhibiting Na-V channels was isolated, showing effects on various neuronal subtypes and potential for developing subtype selective inhibitors in the future.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Yixiang Liu, Naixin Liu, Wenxin Bian, Yue Zhang, Yutong Wu, Ying Peng, Zeqiong Ru, Zhe Fu, Yinglei Wang, Chao Li, Xinwang Yang, Ying Wang
Summary: A short peptide (NCTX15) from Nephila clavata spider toxin gland homogenates was found to lower uric acid levels, inhibit inflammatory responses, and alleviate renal injury, showing potential for treating gout and hyperuricemia.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Article
Multidisciplinary Sciences
Li Zhou, Rui He, Peining Fang, Mengqi Li, Haisheng Yu, Qiming Wang, Yi Yu, Fubing Wang, Yi Zhang, Aidong Chen, Nanfang Peng, Yong Lin, Rui Zhang, Mirko Trilling, Ruth Broering, Mengji Lu, Ying Zhu, Shi Liu
Summary: The alpha-toxin LqhIII from the deathstalker scorpion inhibits fast inactivation of cardiac Na(V)1.5 channels. The cryo-EM structure of LqhIII bound to Na(V)1.5 shows that it traps the gating charges of the S4 segment in a unique intermediate-activated state, explaining why LqhIII slows inactivation of Na-V channels but does not open them.
NATURE COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Maryam Asadi, Hoda Ayat, Ali Mohammad Ahadi, Mohammad Sharif Ranjbar
Summary: In this study, the genomic organization of two toxins targeting Kv1.3 channel from animal venom was characterized, and a chimeric peptide shtx-k/MeuKTX was designed and constructed with higher inhibitory effect on Kv1.3 channel. Molecular docking studies indicated that key amino acids from both toxins were involved in the interaction of the chimeric peptide with the channel, suggesting the potential of shtx-k/MeuKTX as an effective agent to target Kv1.3 channel.
BIOCHEMICAL GENETICS
(2022)
Article
Biochemistry & Molecular Biology
Qiao-Na Chi, Shi-Xi Jia, Hao Yin, Li-E Wang, Xing-Yan Fu, Yan-Nan Ma, Ming-Pu Sun, Yun-Kun Qi, Zhibo Li, Shan-Shan Du
Summary: Cytotoxic peptides derived from spider venoms, such as LVTX-8, have potential as anticancer treatments. However, LVTX-8 is easily degraded and has a short half-life. In this study, ten analogs of LVTX-8 were designed and synthesized. Some of these analogs showed high cytotoxicity against cancer cells, and two derivatives, 825 and 827, exhibited improved stability and anticancer efficiency.
BIOORGANIC CHEMISTRY
(2023)
Article
Environmental Sciences
Jinxing Fu, Yanbin He, Chao Peng, Tianle Tang, Aihua Jin, Yanling Liao, Qiong Shi, Bingmiao Gao
Summary: Sea anemone venom is a valuable marine drug resource library that contains diverse and complex peptide neurotoxins. This study identified a large number of protein and peptide toxin sequences from different developmental stages of Exaiptasia diaphana, a type of sea anemone. The proteins were classified into known superfamilies based on predicted functions, and the 3D structure and pharmacological activity of the peptide neurotoxins were predicted. These findings provide a valuable high-throughput method for obtaining sea anemone proteins and peptides, and lay the foundation for targeted studies on the diversity and pharmacological effects of sea anemone peptide neurotoxins.
FRONTIERS IN MARINE SCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Jinxing Fu, Yanling Liao, Ai-Hua Jin, Bingmiao Gao
Summary: Sea anemones, as primitive metazoa, are rich in bioactive peptide neurotoxins, which have potential applications in neuroscience research and marine drug development. However, only a small percentage of sea anemone species have been utilized for isolating and identifying these neurotoxins, highlighting the need for systematic discovery and study. This review provides an overview of various methods for discovering novel sea anemone peptide neurotoxins, from crude venom purification to gene cloning, and summarizes their three-dimensional structures and targets.
FRONTIERS IN BIOSCIENCE-LANDMARK
(2021)
Article
Pharmacology & Pharmacy
Steve Peigneur, Cristina da Costa Oliveira, Flavia Cristina de Sousa Fonseca, Kirsten L. McMahon, Alexander Mueller, Olivier Cheneval, Ana Cristina Nogueira Freitas, Hana Starobova, Igor Dimitri Gama Duarte, David J. Craik, Irina Vetter, Maria Elena de Lima, Christina I. Schroeder, Jan Tytgat
Summary: This study aims to downsize larger venom-derived Na-V inhibitors into smaller, more drug-like molecules to bridge the gap between drug leads and candidates. By designing a series of small, stable and novel Na-V probes through molecular engineering, the researchers were able to demonstrate potent analgesic activity and subtype selectivity in vitro and in vivo.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Jian Tao, Saige Yin, Yongli Song, Lin Zeng, Shanshan Li, Naixin Liu, Huiling Sun, Zhe Fu, Yinglei Wang, Yilin Li, Yixiang Liu, Jun Sun, Ying Wang, Xinwang Yang
Summary: The novel peptide HsTx2 derived from the scorpion Heterometrus spinifer showed significant anti-apoplectic effects in rats with ischemic stroke, likely exerted through activation of the MAPK signaling pathway. This study highlights HsTx2 as a potential neuroprotective agent for stroke.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Article
Chemistry, Multidisciplinary
Yin Hao, Chen Xitong, Fu Xingyan, Ma Yannan, Xu Yimei, Te Zhang, Liang Shuai, Du Shanshan, Qi Yunkun, Wang Kewei
Summary: This article investigates the coupling reagents for promoting the condensation of carboxylic acids with amines and the impact of different reaction temperatures on the coupling efficiency and oxidation degree of amino acids. A stable and efficient condensation system is validated, and active peptides are successfully synthesized. The results provide important references for solid phase peptide synthesis and the synthesis of peptides with easily oxidizable groups.
ACTA CHIMICA SINICA
(2022)
Article
Food Science & Technology
Qingyi Liao, Xiangjin Kong, Guoqing Luo, Xiangyue Wu, Yinping Li, Qicai Liu, Cheng Tang, Zhonghua Liu
Summary: In this study, the molecular diversity of peptide toxins in the venom of the spider Heteropoda pingtungensis was uncovered using a combinatory strategy of venom gland cDNA library and transcriptome sequencing. A total of 190 non-redundant toxin-like peptides were identified, forming 13 families based on their sequence homology. The toxins in H. pingtungensis venom show high sequence variability and unpredictable biological targets.
Article
Chemistry, Medicinal
Gege Zhang, Huixia Jia, Lei Luo, Yang Zhang, Xitong Cen, Gaoyou Yao, Hua Zhang, Maoxian He, Wenguang Liu
Summary: It has been reported that the giant triton snail (Charonia tritonis) injects venom or acid saliva from its salivary gland into its prey, the crown-of-thorns starfish Acanthaster planci, paralyzing it. Researchers obtained the full-length cDNA sequence of the Ct-kunitzin gene and evaluated its potential function, suggesting it could be a possible agent for novel drug development.
Article
Food Science & Technology
Xiangyue Wu, Yan Chen, Hao Liu, Xiangjin Kong, Xinyao Liang, Yu Zhang, Cheng Tang, Zhonghua Liu
Summary: In the struggle for existence competition, venomous animals have developed a smart strategy called envenomation for predation and defense. Animal venoms contain proteinases, peptide toxins, and small organic molecules with various biological activities. Peptide toxins, in particular, show great diversity and have the ability to modulate ion channels, making them a valuable resource for developing peptide drugs. This study focused on the venom of the spider Lycosa coelestis and identified 98 non-redundant toxins encoded by 597 toxin-like expressed sequence tags (ESTs) through cDNA library and transcriptomic sequencing. Additionally, analysis of the venom composition detected 147 different peptides, and electrophysiology confirmed its inhibitory effect on voltage-gated calcium channels in rat dorsal root ganglion neurons.
Article
Biochemistry & Molecular Biology
Samantha A. Nixon, Zoltan Dekan, Samuel D. Robinson, Shaodong Guo, Irina Vetter, Andrew C. Kotze, Paul F. Alewood, Glenn F. King, Volker Herzig
Article
Chemistry, Medicinal
Alicia Peschel, Fernanda C. Cardoso, Andrew A. Walker, Thomas Durek, M. Rhia L. Stone, Nayara Braga Emidio, Philip E. Dawson, Markus Muttenthaler, Glenn F. King
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Austin B. Schwartz, Anshika Kapur, Zhenbo Huang, Raveendra Anangi, John M. Spear, Scott Stagg, Erminia Fardone, Zolan Dekan, Jens T. Rosenberg, Samuel C. Grant, Glenn F. King, Hedi Mattoussi, Debra Ann Fadool
Summary: The olfactory system is modulated by metabolic factors to drive changes in feeding behavior and energy homeostasis. Inhibiting Kv1.3 in the olfactory bulb can enhance excitability of output neurons and lead to metabolic responses, resulting in changes in body weight and energy metabolism.
JOURNAL OF NEUROCHEMISTRY
(2021)
Article
Anesthesiology
Fernanda C. Cardoso, Joel Castro, Luke Grundy, Gudrun Schober, Sonia Garcia-Caraballo, Tianjiao Zhao, Volker Herzig, Glenn F. King, Stuart M. Brierley, Richard J. Lewis
Summary: The discovery of two novel tarantula-venom peptides, Tap1a and Tap2a, provides potential treatment for chronic visceral pain by modulating the activity of Na-v and Ca(v)3 channels. Tap1a, in particular, shows significant analgesic effects in a mouse model, suggesting a new therapeutic approach for chronic pain.
Article
Multidisciplinary Sciences
Volker Herzig, Kartik Sunagar, David T. R. Wilson, Sandy S. Pineda, Mathilde R. Israel, Sebastien Dutertre, Brianna Sollod McFarland, Eivind A. B. Undheim, Wayne C. Hodgson, Paul F. Alewood, Richard J. Lewis, Frank Bosmans, Irina Vetter, Glenn F. King, Bryan G. Fry
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2020)
Review
Biochemical Research Methods
Andrew A. Walker, Samuel D. Robinson, Brett F. Hamilton, Eivind A. B. Undheim, Glenn F. King
Article
Food Science & Technology
Rachael Y. M. Ryan, Viviana P. Lutzky, Volker Herzig, Taylor B. Smallwood, Jeremy Potriquet, Yide Wong, Paul Masci, Martin F. Lavin, Glenn F. King, J. Alejandro Lopez, Maria P. Ikonomopoulou, John J. Miles
Review
Pharmacology & Pharmacy
David A. Eagles, Chun Yuen Chow, Glenn F. King
Summary: This review examines the role of Na(V)1.7 channels in nociception, their history as a therapeutic target, and the challenges in developing potent inhibitors. Despite significant progress in drug development, effective analgesia remains elusive in clinical trials.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Article
Medicine, Research & Experimental
Junior Gonzales, Javier Hernandez-Gil, Thomas C. Wilson, Dauren Adilbay, Mike Cornejo, Paula Demetrio de Souza Franca, Navjot Guru, Christina Schroeder, Glenn F. King, Jason S. Lewis, Thomas Reiner
Summary: Due to the potential severity and persistence of chemotherapy-induced peripheral neuropathy, there is an urgent need for a tool to quantitatively measure this nerve damage. This study demonstrates a novel approach to localize peripheral nerves using in-cell heat imaging and fluorescence imaging, laying the groundwork for future clinical diagnostics and treatments.
MOLECULAR PHARMACEUTICS
(2021)
Article
Food Science & Technology
Laura C. Wait, Andrew A. Walker, Glenn F. King
Summary: Assassin bugs possess venom that contains proteins with a solitary CUB domain and cystatins, which may contribute to the insecticidal activity of their venom. These components have unknown functions in assassin bug venoms but have been found to cause paralysis and death in certain prey species upon injection.
Article
Biotechnology & Applied Microbiology
Markus Muttenthaler, Glenn E. King, David J. Adams, Paul E. Alewood
Summary: This Perspective summarizes key trends in peptide drug discovery and development, including human hormones, elegant medicinal chemistry and rational design strategies, peptide drugs derived from nature, and major breakthroughs in molecular biology and peptide chemistry. It also emphasizes lessons from earlier approaches that are still relevant today and discusses emerging strategies impact on peptide drug discovery.
NATURE REVIEWS DRUG DISCOVERY
(2021)
Article
Food Science & Technology
Lauren M. Ashwood, Michela L. Mitchell, Bruno Madio, David A. Hurwood, Glenn F. King, Eivind A. B. Undheim, Raymond S. Norton, Peter J. Prentis
Summary: This study found that morphological variations in tentacles are associated with distinct toxin gene expression levels. Sea anemones with spherical tentacular structures may use specific venom cocktails to protect branched structures hosting a large number of photosynthetic symbionts.
Article
Biochemistry & Molecular Biology
Volker Herzig, Yong-Cyuan Chen, Yanni K-Y Chin, Zoltan Dekan, Yu-Wang Chang, Hui-Ming Yu, Paul F. Alewood, Chien-Chang Chen, Glenn F. King
Summary: This study identified a tarantula venom from Avicularia spec. that can inhibit specific subtypes of T-type calcium channels, with the active toxin being omega-Avsp1a. The research suggests that omega-Avsp1a can inhibit specific subtypes of T-type calcium channels, and the domain-1 of Ca(V)3.3 is crucial for this inhibitory effect.
Article
Biochemistry & Molecular Biology
Fernanda C. Cardoso, Sandy S. Pineda, Volker Herzig, Kartik Sunagar, Naeem Yusuf Shaikh, Ai-Hua Jin, Glenn F. King, Paul F. Alewood, Richard J. Lewis, Sebastien Dutertre
Summary: Australian tree-dwelling funnel-web spiders have venom that induces deadly symptoms and exhibits different venom composition compared to ground-dwelling species. The venom of tree-dwellers strongly modulates human voltage-gated sodium and calcium channels, while also showing potent insecticidal effects. This study contributes to understanding the molecular and pharmacological basis for severe envenomation by Australian tree-dwelling funnel-web spiders.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemical Research Methods
Andrew A. Walker, Lynda E. Perkins, Andrea Battisti, Myron P. Zalucki, Glenn F. King
Summary: Ochrogaster lunifer is an Australian caterpillar that has detachable urticating setae with defensive function. These setae can cause inflammation on human skin and equine foetal loss syndrome in gravid horses if accidentally ingested. Transcriptomics and proteomics analysis identified 37 putative toxins, including multiple homologues of honeybee venom peptide secapin and proteins with similarity to odorant binding proteins, arylphorins, and the insect immune modulator Diedel. This study reveals candidate molecules that may contribute to the adverse effects of processionary caterpillar setae on human and animal health.
Article
Pharmacology & Pharmacy
Mohammadhossein Movassaghghazani, Nazanin Shabansalmani
Summary: The study revealed high levels of AFM1 in both breast milk and powdered milk samples in Tehran, with some samples exceeding the established limits. Therefore, monitoring and regulating toxin levels in these products is crucial for maternal and infant health.
Article
Pharmacology & Pharmacy
Defeng Wen, Wantong Han, Quan Chen, Guanhui Qi, Mengling Gao, Pu Guo, Yu Liu, Zhongyuan Wu, Shulin Fu, Qirong Lu, Yinsheng Qiu
Summary: Luteolin can inhibit FB1-induced intestinal inflammatory injury by inhibiting the activation of NF-kappa B and ERK signaling pathways, according to network pharmacology and in vitro experiments.
