What are phospholipase inhibitors?
Phospholipase A2 (PLA2) inhibitors are drugs used to treat conditions associated with excessive platelet production and aggregation of platelets such as peripheral vascular disease.
What drug inhibits phospholipase A2?
Compounds that inhibit or block the activity of a PHOSPHOLIPASE A2 enzyme….Phospholipase A2 Inhibitors.
| Drug | Target | Type |
|---|---|---|
| Varespladib methyl | Phospholipase A2, membrane associated | target |
| Varespladib methyl | Group 10 secretory phospholipase A2 | target |
| Darapladib | Cytosolic phospholipase A2 | target |
What is the function of phospholipase A2?
Phospholipase A2 (PLA2) plays crucial roles in diverse cellular responses, including phospholipid digestion and metabolism, host defense and signal transduction.
Does aspirin inhibit phospholipase A2?
We have shown previously that aspirin (ASA) ingestion by normal human volunteers inhibits peripheral blood monocyte phospholipase C (PLC) activities ex vivo. This PLC inhibitory protein induced by ASA appears distinct from lipocortin, a phospholipase A2 inhibitory protein inducible by corticosteroids.
Are corticosteroids phospholipase inhibitors?
Steroids increase the synthesis of lipocortin (annexin) 1, a phospholipase A2 inhibitor, decreasing the production of inflammatory mediators. Corticosteroids suppress spontaneous ectopic neural discharge originating in experimental neuromas.
What happens when phospholipase A2 is inhibited?
Steroids increase the synthesis of lipocortin (annexin) 1, a phospholipase A2 inhibitor, and thus decrease the production of inflammatory mediators such as leukotrienes, prostaglandins, and platelet-activating factor.
Does steroid inhibit phospholipase A2?
The steroids do not appear to inhibit the phospholipase directly since they do not work in cell-free homogenates. It is too early to say whether or not the antiinflammatory activity of steroids depends on the actions.
Do Corticosteroids inhibit phospholipase A2?
28.4. Corticosteroids inhibit phospholipase A2 production by boosting production of lipocortin, an inhibitor protein.
How is phospholipase A2 activated?
Lipid–Protein Interactions in Membranes Phospholipase A2 hydrolyzes the fatty acid at position 2′ of the glycerol of a phospholipid, producing a lysophospholipid. To act on the phospholipid substrate residing in a biological membrane, the phospholipase must gain access to the cleavage site on the lipid.
How does phospholipase A2 cause inflammation?
sPLA2 has been shown to promote inflammation in mammals by catalyzing the first step of the arachidonic acid pathway by breaking down phospholipids, resulting in the formation of fatty acids including arachidonic acid. This arachidonic acid is then metabolized to form several inflammatory and thrombogenic molecules.
What activates phospholipase A2?
Phospholipase A2 hydrolyzes the fatty acid at position 2′ of the glycerol of a phospholipid, producing a lysophospholipid. To act on the phospholipid substrate residing in a biological membrane, the phospholipase must gain access to the cleavage site on the lipid.
Do steroids inhibit pla2?
The steroids do not appear to inhibit the phospholipase directly since they do not work in cell-free homogenates.