Article
Zoology
Zichang Li, Ingi Agnarsson, Yu Peng, Jie Liu
Summary: This paper reports on eight cobweb spider species building a detritus-based, bell-shaped retreat in China, including five new species and three known species. The type of bell-shaped retreat is rare in theridiids and is found only in four related genera. This study suggests future research on the evolution of the retreat and related traits.
Article
Environmental Sciences
Nazife Yigit Kayhan, Ilkay Corak Ocal, Kader Akdeniz
Summary: Spider venoms contain various chemicals with pharmacologically important molecules. This study found that the crude venom of Agelena orientalis spider has anti-tumor and cytotoxic effects, and can slow down the proliferation of breast cancer cells.
FRESENIUS ENVIRONMENTAL BULLETIN
(2022)
Article
Integrative & Complementary Medicine
Amine Assouguem, Mohammed Kara, Amal Ramzi, Saoussan Annemer, Alicja Kowalczyk, Essam A. Ali, Bushra Abdulkarim Moharram, Abderrahim Lazraq, Abdellah Farah
Summary: With growing concerns over the impact of chemical acaricides, the use of essential oils as eco-friendly alternatives for pest management is gaining traction. Experimental results demonstrate the efficacy of various plant-derived essential oils against crop pests, particularly when combined with the active ingredient acequinocyl. These findings suggest the potential for developing botanical pesticides for integrated pest management.
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
M. Yu. Myshkin, A. S. Paramonov, D. S. Kulbatskii, E. A. Surkova, A. A. Berkut, A. A. Vassilevski, E. N. Lyukmanova, M. P. Kirpichnikov, Z. O. Shenkarev
Summary: Voltage-gated sodium channels have modular architecture with five membrane domains, where peripheral voltage-sensing domains are responsible for channel activation and rapid inactivation. Gating modifier toxins from arthropod venoms interact with these domains, potentially serving as prototypes for new drugs. In this study, the toxin Hm-3 showed high affinity to VSD-III of human skeletal muscle Na(V)1.4 channel, with specific residues likely interacting with the channel and the lipid bilayer.
Article
Biochemistry & Molecular Biology
Unchaleeporn Ameamsri, Arunrat Chaveerach, Runglawan Sudmoon, Tawatchai Tanee, Steve Peigneur, Jan Tytgat
Summary: The study aimed to investigate the oleamide content in different plants and test their bioactivity. Results showed that leaf extracts of Ipomoea aquatica and Dillenia ovata had high oleamide content, while the Dillenia formulation exhibited anti-inflammatory activity.
CURRENT PHARMACEUTICAL BIOTECHNOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Marianne van Cann, Alexey Kuzmenkov, Jorg Isensee, Alexander Andreev-Andrievskiy, Steve Peigneur, Georgii Khusainov, Antonina Berkut, Jan Tytgat, Alexander Vassilevski, Tim Hucho
Summary: The study identified a scorpion toxin, MeuNaTx alpha-1, from Mesobuthus eupeus venom, which modulates pain sensitization signaling in rat primary sensory neurons. The toxin showed dose-dependent effects on sensory neurons and its mechanism of action involves the Na(V)1.2 sodium channel.
Article
Biochemistry & Molecular Biology
Konstantin S. Mineev, Alexey Kuzmenkov, Alexander S. Arseniev, Alexander A. Vassilevski
Summary: Old world scorpions produce a variety of toxins called alpha-NaTx, which affect voltage-gated sodium channels. The selectivity of these toxins to mammals or insects is determined by a part called the specificity module. The spatial structure of a major toxin MeuNaTx alpha-1 from the venom of Mesobuthus eupeus shows a unique specificity module and structural diversity influenced by protein motifs such as the nest and niche.
PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS
(2021)
Article
Biophysics
Valentin M. Tabakmakher, Andrei M. Gigolaev, Steve Peigneur, Nikolay A. Krylov, Jan Tytgat, Anton O. Chugunov, Alexander A. Vassilevski, Roman G. Efremov
Summary: In this study, a combined molecular modeling approach was utilized to design a series of Tk-hefu-2 derivatives with improved affinity to K(V)1.3 while maintaining specificity. The most active mutant Tk-hefu-10 showed significantly higher inhibitory activity, demonstrating the potential of alpha-hairpinins as a scaffold for rational design of ion channel inhibitors. This work represents a promising strategy for increasing the success rate in molecular design of ion channel inhibitors.
BIOPHYSICAL JOURNAL
(2021)
Article
Biochemistry & Molecular Biology
V. M. Tabakmakher, A. Kuzmenkov, A. M. Gigolaev, E. L. Pinheiro, S. Peigneur, R. G. Efremov, J. Tytgat, A. A. Vassilevski
Summary: The study reports the isolation of a peptide toxin MeKTx13-3 from scorpion venom and its artificial derivative MeKTx13-3_RMRH, which shows increased selectivity towards K(V)1.1. Through computer simulations, researchers demonstrate that the preference of the new ligand for K(V)1.1 can be achieved through specific positioning of the toxin in complex with the channel.
JOURNAL OF EVOLUTIONARY BIOCHEMISTRY AND PHYSIOLOGY
(2021)
Review
Chemistry, Medicinal
Spela Gubic, Louise A. Hendrickx, Zan Toplak, Masa Sterle, Steve Peigneur, Tihomir Tomasic, Luis A. Pardo, Jan Tytgat, Anamarija Zega, Lucija P. Masic
Summary: The K(V)1.3 voltage-gated potassium ion channel plays a crucial role in immune and nervous systems, and targeting it with specific peptides and small molecule inhibitors shows potential for treating cancers and autoimmune diseases. Strategies for improving selectivity and discovering new K(V)1.3 inhibitors are discussed, with promising candidates being evaluated for clinical development. Optimized small-molecule inhibitors with defined structure-activity relationships may offer therapeutic potential for cancer treatment.
MEDICINAL RESEARCH REVIEWS
(2021)
Article
Biochemistry & Molecular Biology
M. Yu. Myshkin, A. S. Paramonov, D. S. Kulbatskii, E. A. Surkova, A. A. Berkut, A. A. Vassilevski, E. N. Lyukmanova, M. P. Kirpichnikov, Z. O. Shenkarev
Summary: Voltage-gated sodium channels have modular architecture with five membrane domains, where peripheral voltage-sensing domains are responsible for channel activation and rapid inactivation. Gating modifier toxins from arthropod venoms interact with these domains, potentially serving as prototypes for new drugs. In this study, the toxin Hm-3 showed high affinity to VSD-III of human skeletal muscle Na(V)1.4 channel, with specific residues likely interacting with the channel and the lipid bilayer.
Article
Biochemistry & Molecular Biology
M. A. Chernykh, N. A. Kuldyushev, S. Peigneur, A. A. Berkut, J. Tytgat, R. G. Efremov, A. A. Vassilevski, A. O. Chugunov
Summary: The study showed that the double mutant derivative BeM9(EG) lost its activity on mammalian channels and became an insect toxin. Molecular dynamics simulations suggested that residues K8 and Y17 play an important role in stabilizing a specific conformation of BeM9 loops, and it is hypothesized that the replacement of these residues allosterically affects the efficiency of toxin binding to channels.
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Igor E. Kasheverov, Alexey I. Kuzmenkov, Denis S. Kudryavtsev, Ivan S. Chudetskiy, Irina V. Shelukhina, Evgeny P. Barykin, Igor A. Ivanov, Andrei E. Siniavin, Rustam H. Ziganshin, Mikhail S. Baranov, Victor I. Tsetlin, Alexander A. Vassilevski, Yuri N. Utkin
Summary: The study found that the introduction of a synthetic GFP chromophore induced a considerably lower decrease in affinity between protein and peptide neurotoxins and receptors compared to full-length GFP attachment. This new method can be used for visualizing nAChR in tissue slices and cell cultures.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2021)
Review
Cardiac & Cardiovascular Systems
Anne-Sophie Depuydt, Steve Peigneur, Jan Tytgat
Summary: Pacemaker cells are crucial for the rhythm of the heart, and cardiovascular diseases and arrhythmias are major causes of hospital admissions and sudden death. The prevalence of arrhythmias will increase due to an aging population and risk factors. HCN channels, the molecular correlate of the pacemaker activity, have shown potential as targets for drug development to lower heart rate. However, there is still limited understanding of their pharmacology compared to other ion channels. Ivabradine is currently the only approved drug targeting HCN channels. This review focuses on the pacemaking process in the heart and summarizes current knowledge on HCN channels.
CURRENT CARDIOLOGY REVIEWS
(2022)
Article
Pharmacology & Pharmacy
Alexey I. Kuzmenkov, Steve Peigneur, Joshua A. Nasburg, Konstantin S. Mineev, Maxim V. Nikolaev, Ernesto Lopes Pinheiro-Junior, Alexander S. Arseniev, Heike Wulff, Jan Tytgat, Alexander A. Vassilevski
Summary: Apamin is a selective inhibitor of K(Ca)2 channels with no significant effects on other molecular targets. The spatial structure of apamin and its potential use as a pharmacological tool and drug design template for K(Ca)2 channels are supported by this study.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
A. M. Gigolaev, E. L. Pinheiro-Junior, S. Peigneur, J. Tytgat, A. A. Vassilevski
Summary: In this study, a highly potent and selective ligand for the potassium channel K(V)1.2 was obtained by modifying a scorpion peptide toxin. The modified peptide showed increased affinity and activity against K(V)1.2, while having lower affinity for other isoforms.
JOURNAL OF EVOLUTIONARY BIOCHEMISTRY AND PHYSIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Junyu Liu, Michael Maxwell, Thom Cuddihy, Theo Crawford, Madeline Bassetti, Cameron Hyde, Steve Peigneur, Jan Tytgat, Eivind A. B. Undheim, Mehdi Mobli
Summary: Receptor avidity through multivalency is difficult to engineer in synthetic molecules, but can be found in natural bivalent antibodies. The discovery of bivalent venom peptides with tandem repeat domains has provided insight into multivalency in biomolecules. ScrepYard, an online resource, assists in identifying SCREP sequences and characterizing this emerging class of biomolecules.
Meeting Abstract
Biochemistry & Molecular Biology
A. Kuzmenkov, I. Chudetskiy, D. Prudnikova, A. Vassilevski
Meeting Abstract
Pharmacology & Pharmacy
M. van Cann, A. Kuzmenkov, J. Isensee, A. Andreev-Andrievskiy, S. Peigneur, G. Khusainov, A. Berkut, J. Tytgat, A. Vassilevski, T. Hucho
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2021)