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 María Gutiérrez +3 more
doaj +5 more sources
Delayed LY333013 (Oral) and LY315920 (Intravenous) Reverse Severe Neurotoxicity and Rescue Juvenile Pigs from Lethal Doses of Micrurus fulvius (Eastern Coral Snake) Venom [PDF]
Toxins, 2018 There is a clear, unmet need for effective, lightweight, shelf-stable and economical snakebite envenoming therapies that can be given rapidly after the time of a snake’s bite and as adjuncts to antivenom therapies in the hospital setting. The sPLA2
Matthew R. Lewin +6 more
doaj +5 more sources
Coagulotoxic Cobras: Clinical Implications of Strong Anticoagulant Actions of African Spitting Naja Venoms That Are Not Neutralised by Antivenom but Are by LY315920 (Varespladib) [PDF]
Toxins, 2018 Snakebite is a global tropical disease that has long had huge implications for human health and well-being. Despite its long-standing medical importance, it has been the most neglected of tropical diseases.
Mátyás A. Bittenbinder +7 more
doaj +5 more sources
Varespladib (LY315920) Appears to Be a Potent, Broad-Spectrum, Inhibitor of Snake Venom Phospholipase A2 and a Possible Pre-Referral Treatment for Envenomation [PDF]
Toxins, 2016 Snakebite remains a neglected medical problem of the developing world with up to 125,000 deaths each year despite more than a century of calls to improve snakebite prevention and care.
Matthew Lewin +3 more
doaj +5 more sources
Structural basis for phospholipase A2-like toxin inhibition by the synthetic compound Varespladib (LY315920). [PDF]
Sci Rep, 2019 The World Health Organization recently listed snakebite envenoming as a Neglected Tropical Disease, proposing strategies to significantly reduce the global burden of this complex pathology by 2030.
Salvador GHM +7 more
europepmc +4 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 [PDF]
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 ...
Matthew R. Lewin +6 more
doaj +2 more sources
Molecular docking analysis of MCL-1 inhibitors for breast cancer management. [PDF]
Bioinformation, 2023 Myeloid leukemia 1 (MCL-1), a BCL-2 protein family member, acts as an anti-apoptotic protein by interacting with pro-apoptotic BCL-2 proteins. Its overexpression is frequently observed in numerous cancer types including breast cancer, and is closely ...
Abdulrahman A +7 more
europepmc +2 more sources
Structural and Functional Aspects of Targeting the Secreted Human Group IIA Phospholipase A2 [PDF]
Molecules, 2020 Human group IIA secretory phospholipase A2 (hGIIA) promotes the proliferation of cancer cells, making it a compelling therapeutic target, but it is also significant in other inflammatory conditions.
Ryung Rae Kim +5 more
doaj +2 more sources
sPLA2-IIA Augments Oxidized LDL-Induced MCP-1 Expression in Vitro Through Activation of Akt
Cellular Physiology and Biochemistry, 2015 Background/Aims: Group IIA secretory phospholipase A2 (sPLA2-IIA) has an important role in atherosclerosis. In this study, we explored whether sPLA2-IIA overexpression could promote atherosclerosis in normal environment alone or with other inflammatory ...
Yongjun Guo +4 more
doaj +2 more sources
Chromobox2 inhibition: a novel activity of alisertib, an aurora A kinase inhibitor. [PDF]
Mol Cancer TherChromobox 2 (CBX2), a subunit of Polycomb Repressor Complex 1 (PRC1), is expressed in high-grade serous carcinoma. CBX2 inhibitory peptide (CBX2i) has demonstrated efficacy in a syngeneic mouse model, but has limitations.
Yamamoto TM +9 more
europepmc +2 more sources