Description
PTK is an analog of palmitic acid in which the COOH group is replaced by trifluoromethyl ketone. In P388D1 cells, PTK inhibits iPLA
2 activity with an IC
50 value of 3.8 μM. A related compound, ATK is a less potent inhibitor of iPLA
2 with an IC
50 value of 15 μM. PTK also inhibits the activity of cPLA
2 with an IC
50 value almost identical to that of ATK.
Uses
PACOCF3 is an inductors of BLM, an artificial lipid membranes and liposome permeabilization. Phospholipase A2 inhibitor.
Definition
ChEBI: Palmityl Trifluoromethyl Ketone is an alpha-haloketone.
Biological Activity
Phospholipase A 2 inhibitor. Can also alter Ca 2+ signaling in renal tubular cells.
References
1. murakami m et al.emerging roles of secreted phospholipase a2 enzymes: the 3rd edition.biochimie. 2014 sep 16. pii: s0300-9084(14)00252-1.2. quach nd et al. secretory phospholipase a2 enzymes as pharmacological targets for treatment of disease. biochem pharmacol. 2014 aug 15;90(4):338-48. 3. chalimoniuk m. secretory phospholipase a2 and its role in oxidative stress and inflammation]. postepy biochem. 2012;58(2):204-8.4. persaud sj.et al. the role of arachidonic acid and its metabolites in insulin secretion from human islets of langerhans. diabetes. 2007 jan;56(1):197-203.5. khakpour h et al. lipoprotein-associated phospholipase a2: an independent predictor of cardiovascular risk and a novel target for immunomodulation therapy. cardiol rev. 2009 sep-oct;17(5):222-9. 6. narendra sharath chandra jn1 et al. chemistry and structural evaluation of different phospholipase a2 inhibitors in arachidonic acid pathway mediated inflammation and snake venom toxicity. curr top med chem. 2007;7(8):787-800.7. packard cj. lipoprotein-associated phospholipase a2 as a biomarker of coronary heart disease and a therapeutic target. curr opin cardiol. 2009 jul;24(4):358-63.8. lucas r et al. synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases a2. bioorg med chem lett. 2000 feb 7;10(3):285-8.
