Results 11 to 20 of about 161 (74)

Neutralizing properties of LY315920 toward snake venom group I and II myotoxic phospholipases A2

Toxicon, 2018
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. LY315920 (Varespladib, S-5920, A-001), a low molecular weight drug developed to inhibit several human secreted ...
Wendy Bryan-Quirós, Julián Fernández, José Marı́a Gutiérrez, Matthew R. Lewin, Bruno Lomonte   +4 more
semanticscholar   +5 more sources

Secretory phospholipase A2-IIa upregulates HER/HER2-elicited signaling in lung cancer cells. [PDF]

Int J Oncol, 2014
Lung cancer is the leading cause of cancer death worldwide. There is an urgent need for early diagnostic tools and novel therapies in order to increase lung cancer survival.
Dong Z, Meller J, Succop P, Wang J, Wikenheiser-Brokamp K, Starnes S, Lu S.   +6 more
europepmc   +2 more sources

Developing Small Molecule Therapeutics for the Initial and Adjunctive Treatment of Snakebite. [PDF]

J Trop Med, 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.
Bulfone TC, Samuel SP, Bickler PE, Lewin MR.   +3 more
europepmc   +2 more sources

Suppressive effect of secretory phospholipase A2 inhibitory peptide on interleukin-1beta-induced matrix metalloproteinase production in rheumatoid synovial fibroblasts, and its antiarthritic activity in hTNFtg mice. [PDF]

Arthritis Res Ther, 2009
IntroductionSecretory phospholipase A2 (sPLA2) and matrix metalloproteinase (MMP) inhibitors are potent modulators of inflammation with therapeutic potential, but have limited efficacy in rheumatoid arthritis (RA).
Thwin MM, Douni E, Arjunan P, Kollias G, Kumar PV, Gopalakrishnakone P.   +5 more
europepmc   +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

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

Regioselective synthesis of 4- and 7-alkoxyindoles from 2,3-dihalophenols: application to the preparation of indole inhibitors of phospholipase A2.

Journal of Organic Chemistry, 2007
An efficient and regioselective synthesis of 4- and 7-alkoxyindoles has been developed from commercially available starting materials such as 3-halophenols and 3-chloroanisole.
R. Sanz, M. Castroviejo, V. Guilarte, A. Perez, F. Fañanás   +4 more
semanticscholar   +1 more source

The Search for Natural and Synthetic Inhibitors That Would Complement Antivenoms as Therapeutics for Snakebite Envenoming. [PDF]

Toxins (Basel), 2021
Gutiérrez JM, Albulescu LO, Clare RH, Casewell NR, Abd El-Aziz TM, Escalante T, Rucavado A.   +6 more
europepmc   +1 more source