Results 1 to 10 of about 721 (146)

Exploration of the Inhibitory Potential of Varespladib for Snakebite Envenomation [PDF]

Molecules, 2018
Phospholipase A2s (PLA2) is a major component of snake venom with diverse pathologic toxicities and, therefore, a potential target for antivenom therapy. Varespladib was initially designed as an inhibitor of mammal PLA2s, and was recently repurposed to a
Chunhong Huang, Huixiang Xiao
exaly   +6 more sources

Varespladib (LY315920) and Methyl Varespladib (LY333013) Abrogate or Delay Lethality Induced by Presynaptically Acting Neurotoxic Snake Venoms [PDF]

Toxins, 2020
The phospholipase A2 (PLA2) inhibitor Varespladib (LY315920) and its orally bioavailable prodrug, methyl-Varespladib (LY333013) inhibit PLA2 activity of a wide variety of snake venoms.
José Maria Gutierrez, David Williams, Bruno Lomonte   +2 more
exaly   +9 more sources

A Combined Bioassay and Nanofractionation Approach to Investigate the Anticoagulant Toxins of Mamba and Cobra Venoms and Their Inhibition by Varespladib [PDF]

Toxins, 2022
Envenomation by elapid snakes primarily results in neurotoxic symptoms and, consequently, are the primary focus of therapeutic research concerning such venoms. However, mounting evidence suggests these venoms can additionally cause coagulopathic symptoms,
Jeroen Kool, Taline Kazandjian, Arif Arrahman   +2 more
exaly   +7 more sources

Varespladib in the Treatment of Snakebite Envenoming: Development History and Preclinical Evidence Supporting Advancement to Clinical Trials in Patients Bitten by Venomous Snakes

Toxins, 2022
The availability of effective, reliably accessible, and affordable treatments for snakebite envenoming is a critical and long unmet medical need. Recently, small, synthetic toxin-specific inhibitors with oral bioavailability used in conjunction with ...
Bryan Fry, Lewin Mr, Rebecca W Carter
exaly   +4 more sources

Varespladib attenuates Naja atra-induced acute liver injury via reversing Nrf2 signaling-mediated ferroptosis and mitochondrial dysfunction [PDF]

Redox Report
Objective: To investigate the protective effects of varespladib against Naja atra-induced acute liver injury (ALI) and to elucidate the toxic mechanism of snake venom phospholipase A2 (SVPLA2)-induced hepatic oxidative stress, with a particular focus on ...
Jiahao Liu, Linfeng Wang, Mengxia Xie, Wenjie Zhao, Jiaqi Sun, Yuji Jin, Meiling Liu, Jianqi Zhao, Lixia Cheng, Cheng Wen, Xiaowen Bi, Chunhong Huang   +11 more
doaj   +3 more sources

Feasibility study: Varespladib protects CD-1 mice from lethal doses of whole bee (Apis mellifera) venom [PDF]

Toxicon: X
Swarming Hymenoptera attacks can deliver high cumulative doses of venom resulting in death and life-threatening or chronically disabling injuries. Varespladib, a potent inhibitor of snake venom secretory PLA2 (sPLA2), is a relatively weak inhibitor of ...
Lewin Mr
exaly   +4 more sources

In vitro-in vivo discord: A preclinical study of AZD2716 and its racemate with comparison to varespladib for the development of snake venom sPLA2 inhibitors [PDF]

Toxicon: X
We evaluated a family of repurposed sPLA2 inhibitors as novel candidate snakebite envenoming therapeutics. Stereospecific (R)-7 AZD2716 and its racemic mixture were compared to varespladib in an in vitro sPLA2 assay against a sample of 26 venoms from ...
James L. Hearth, Yulia Surovtseva, Zuzana Karjala, Nicholas R. Casewell, Kate Giang, Matthew R. Lewin   +5 more
doaj   +2 more sources

Repurposed small molecule toxin inhibitors neutralise a diversity of venoms from the Neotropical viperid snake genus Bothrops [PDF]

eLife
Snakebite globally claims more than 100,000 lives per year and results in morbidity for 400,000 survivors. Current treatment uses antibody-based antivenoms which are constrained by their efficacy, safety, and cost. In this study we evaluated the efficacy
Rachel H Clare, Adam Westhorpe, Emma Stars, Taline D Kazandjian, Laura-Oana Albulescu, Stefanie K Menzies, Nicholas R Casewell   +6 more
doaj   +2 more sources

Lessons Learned from a Military–Biotechnology Partnership to Develop a Broad-Spectrum Small-Molecule Inhibitor for Snakebite Envenoming [PDF]

Toxins
Snakebite envenoming causes an estimated 138,000 deaths annually worldwide, with approximately 75% of fatalities occurring prior to arrival at definitive medical care.
Kendra L. Lawrence, Jeffery L. Owen, Lindsey S. Garver, Brandi A. Ritter, Christopher M. Wilson, Ginger R. Boatright, F. Y. Bowling, Timothy F. Platts-Mills, Andrea K. Renner, Rebecca W. Carter   +9 more
doaj   +2 more sources

Naja atra SVPLA2 contributes to venom-induced AKI via HRAS palmitoylation-dependent PI3K-AKT inactivation [PDF]

Journal of Lipid Research
Clinically, acute kidney injury (AKI) is one of the most frequent complications of Naja atra (N. atra) envenomation, primarily attributed to snake venom phospholipase A2 (SVPLA2). Although the SVPLA2 inhibitor varespladib shows great therapeutic promise,
Jiahao Liu, Sitong Chen, Jiajia Wu, Sunkun Tang, Zejing Wen, Xiaowen Bi, Yang Yang, Chunhong Huang   +7 more
doaj   +2 more sources