Results 11 to 20 of about 157 (83)

Neutralizing properties of Varespladib toward group I and II myotoxic phospholipases A2

Toxicon, 2019
A need exists to develop specific and clinically useful inhibitors of toxic enzymes present in snake venoms, responsible for severe tissue damage and life-threatening effects occurring in thousands of people suffering envenomations globally.
Bryan Quirós, Wendy, Fernández Ulate, Julián, Lewin, Matthew R., Lomonte, Bruno, Gutiérrez, José María   +4 more
core   +3 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, Zheng Chen, Timothy J. Mann, Karine Bastard, Kieran F. Scott, W. Bret Church   +5 more
doaj   +2 more sources

Modulation of immunity by the secreted phospholipase A2 family

Immunological Reviews, Volume 317, Issue 1, Page 42-70, August 2023., 2023
Summary Among the phospholipase A2 (PLA2) superfamily, which typically catalyzes the sn‐2 hydrolysis of phospholipids to yield fatty acids and lysophospholipids, the secreted PLA2 (sPLA2) family contains 11 isoforms in mammals. Individual sPLA2s have unique enzymatic specificity toward fatty acids and polar heads of phospholipid substrates and display ...
Makoto Murakami, Hiroyasu Sato, Yoshitaka Taketomi   +2 more
wiley   +1 more source

Action of Varespladib (LY-315920), a Phospholipase A2 Inhibitor, on the Enzymatic, Coagulant and Haemorrhagic Activities of Lachesis muta rhombeata (South-American Bushmaster) Venom

Frontiers in Pharmacology, 2022
Varespladib (VPL) was primarily developed to treat inflammatory disturbances associated with high levels of serum phospholipase A2 (PLA2). VPL has also demonstrated to be a potential antivenom support agent to prevent PLA2-dependent effects produced by ...
Pamella G. Gutierres, Diego R. Pereira, Nataly L. Vieira, Lilian F. Arantes, Nelson J. Silva, Kristian A. Torres-Bonilla, Stephen Hyslop, Karen Morais-Zani, Rosa M. B. Nogueira, Edward G. Rowan, Rafael S. Floriano   +10 more
doaj   +1 more source

Developing Small Molecule Therapeutics for the Initial and Adjunctive Treatment of Snakebite

Journal of Tropical Medicine, Volume 2018, Issue 1, 2018., 2018
The World Health Organization (WHO) recently added snakebite envenoming to the priority list of Neglected Tropical Diseases (NTD). It is thought that ~75% of mortality following snakebite occurs outside the hospital setting, making the temporal gap between a bite and antivenom administration a major therapeutic challenge.
Tommaso C. Bulfone, Stephen P. Samuel, Philip E. Bickler, Matthew R. Lewin, Marcel Tanner   +4 more
wiley   +1 more source

Snake Venom PLA2, a Promising Target for Broad‐Spectrum Antivenom Drug Development

BioMed Research International, Volume 2017, Issue 1, 2017., 2017
Snakebite envenomation is a neglected global health problem, causing substantial mortality, disability, and psychological morbidity, especially in rural tropical and subtropical zones. Antivenin is currently the only specific medicine for envenomation. However, it is restricted by cold storage, snakebite diagnosis, and high price.
Huixiang Xiao, Hong Pan, Keren Liao, Mengxue Yang, Chunhong Huang, Ji-Fu Wei   +5 more
wiley   +1 more source

Acute Phase Reactants as Novel Predictors of Cardiovascular Disease

International Scholarly Research Notices, Volume 2012, Issue 1, 2012., 2012
Acute phase reaction is a systemic response which usually follows a physiological condition that takes place in the beginning of an inflammatory process. This physiological change usually lasts 1‐2 days. However, the systemic acute phase response usually lasts longer. The aim of this systemic response is to restore homeostasis.
M. S. Ahmed, A. B. Jadhav, A. Hassan, Qing H. Meng, N. Ortego-Centeno, S. Pender   +5 more
wiley   +1 more source

Anticoagulant toxicity of black snake (Elapidae: Pseudechis) venoms: Potency, mechanisms, and antivenom efficacy

, 2020
Pseudechis species (Australian black snakes) within the Elapidae family are rich in anticoagulant PLA toxins, with the exception of one species (P. porphyriacus) that possesses procoagulant mutated forms of the clotting enzyme Factor Xa.
Zdenek, Christina N., Youngman, Nicholas J., Hay, Chris, Milanovic, Leontina, Dobson, James, Dunstan, Nathan, Allen, Luke, Fry, Bryan G.   +7 more
core   +1 more source

Interactions of small molecule inhibitors with secreted phospholipase A2: A review of the structural data

Chemical Biology &Drug Design, Volume 103, Issue 2, February 2024.
Due to their roles in inflammation, the sPLA2 enzymes are of much medicinal interest. sPLA2 inhibitors have been developed for the treatment of inflammatory and other conditions such as cardiovascular disease, arteriosclerosis and rheumatoid arthritis.
Chantalle Crous, Anél Petzer, Jacobus P. Petzer   +2 more
wiley   +1 more source

Highly Specific and Broadly Potent Inhibitors of Mammalian Secreted Phospholipases A₂

, 2016
We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor.
Michael H. Gelb (257901), Rob C. Oslund (1335195), Nathan Cermak (429374)   +2 more
core   +1 more source