+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

PLA2-mediated catalytic activation of its inhibitor 25-acetyl-petrosaspongiolide M: serendipitous identification of a new PLA2 suicide inhibitor



PLA2-mediated catalytic activation of its inhibitor 25-acetyl-petrosaspongiolide M: serendipitous identification of a new PLA2 suicide inhibitor



Febs Letters 578(3): 269-274



25-Acetyl-petrosaspongiolide M (PMAc) (1), a mild non-covalent PLA(2) inhibitor, unexpectedly recovers, after incubation with bvPLA(2), the ability to covalently modify the enzyme target. This study demonstrates the catalytic effect of bvPLA(2) in converting 1 in its deacetylated congener petrosaspongiolide M (PM) (2), a strong covalent PLA(2) inhibitor whose molecular mechanism of inhibition has already been clarified. Moreover, our findings outline the potential role of PMAc as anti-inflammatory pro-drug, by virtue of its ability of delivering the active PM agent at the site of inflammation, functioning as a suicide inhibitor.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 012391436

Download citation: RISBibTeXText

PMID: 15589831

DOI: 10.1016/j.febslet.2004.10.100


Related references

Studies on the measurement of phospholipase A2 (PLA2) and PLA2 inhibitor activities in ram semen. Animal Reproduction Science 56(2): 107-121, 1999

Contribution of Type II PLA2 to prostaglandin formation: A study using a Type II PLA2 specific inhibitor SB 203347. Prostaglandins & Other Lipid Mediators 57(5-6): 361-370, 1999

Isolation of a snake venom phospholipase A2 (PLA2) inhibitor (AIPLAI) from leaves of Azadirachta indica (Neem): mechanism of PLA2 inhibition by AIPLAI in vitro condition. Toxicon 51(8): 1548-1553, 2008

Type IIA secretory PLA2-mediated delayed PGE2 biosynthesis is regulated by the products of the cytosolic PLA2. Advances in Experimental Medicine and Biology 507: 9, 2002

Evidence that phospholipase A2 (PLA2) inhibitors can selectively block PLA2-mediated contractions of guinea pig lung pleural strips. Journal of Pharmacology and Experimental Therapeutics 262(3): 1147-1153, 1992

Activation by P2X7 agonists of two phospholipases A2 (PLA2) in ductal cells of rat submandibular gland. Coupling of the calcium-independent PLA2 with kallikrein secretion. Journal of Biological Chemistry 273(46): 30208-30217, 1998

Toward understanding interfacial activation of secretory phospholipase A2 (PLA2): membrane surface properties and membrane-induced structural changes in the enzyme contribute synergistically to PLA2 activation. Biophysical Journal 80(2): 789-800, 2001

Development of a monoclonal antibody capable of differentiating platelet PLA1/PLA1, PLA1/PLA2 and PLA2/PLA2 genotypes. British Journal of Haematology 81(1): 113-117, 1992

PLA2 inhibitor complexes at high resolution. Biophysical Journal 78(1 Part 2): 414A, 2000

Apical ANG II-stimulated PLA2 activity and Na+ flux: a potential role for Ca2+-independent PLA2. American Journal of Physiology 273(4): F554-F562, 1997

Inhibition of endosome fusion by phospholipase A2 (PLA2) inhibitors points to a role for PLA2 in endocytosis. Proceedings of the National Academy of Sciences of the United States of America 90(21): 10255-9, 1993

P9a(Cdt-PLA2) from Crotalus durissus terrificus as good immunogen to be employed in the production of crotalic anti-PLA2 IgG. Toxicology Letters 238(1): 7, 2015

Interleukin-1 beta stimulates ovarian phosphoipase A2 (PLA2) expression and activity: up-regulation of both secretory and cytosolic PLA2. Endocrinology 138(1): 314-321, 1997

Crystal structure of a class XIB phospholipase A2 (PLA2): rice (oryza sativa) isoform-2 pla2 and an octanoate complex. Journal of Biological Chemistry 284(29): 19371-9, 2009

Detection of two phospholipase A2(PLA2) activities in leaves of higher plant Vicia faba and comparison with mammalian PLA2's. Febs Letters 343(3): 213-218, 1994