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Related Concept Videos

Phosphoinositides and PIPs01:42

Phosphoinositides and PIPs

Phosphoinositides are a group of phospholipids containing a glycerol backbone with two fatty acid chains and a phosphate attached to a myoinositol sugar ring. The inositol head group extends into the cytoplasm, where it is modified by adding phosphate groups to form phosphatidylinositol phosphates or PIPs.
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
IP3/DAG Signaling Pathway01:11

IP3/DAG Signaling Pathway

Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the  phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and produces two-second...
Lipid-Lowering Drugs: Statins and Miscellaneous Agents01:20

Lipid-Lowering Drugs: Statins and Miscellaneous Agents

Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...

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Related Experiment Video

Updated: Jun 22, 2026

A Liposome Membrane Permeability Assay for Investigating the Effects of Phosphatidylinositol Phosphate Groups on Membranotropic Action of Venom PLA2
10:31

A Liposome Membrane Permeability Assay for Investigating the Effects of Phosphatidylinositol Phosphate Groups on Membranotropic Action of Venom PLA2

Published on: September 26, 2025

Phospholipase A2 inhibitors.

Hector M Garcia-Garcia1, Patrick W Serruys

  • 1Thoraxcenter, Erasmus Medical Center, Rotterdam, The Netherlands.

Current Opinion in Lipidology
|June 25, 2009
PubMed
Summary
This summary is machine-generated.

Novel treatments targeting inflammation and lipids in atherosclerosis are being explored. Inhibiting phospholipase A2 (PLA2) and lipoprotein-associated phospholipase A2 (Lp-PLA2) shows promise for treating cardiovascular disease.

More Related Videos

Defining Substrate Specificities for Lipase and Phospholipase Candidates
08:59

Defining Substrate Specificities for Lipase and Phospholipase Candidates

Published on: November 23, 2016

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Last Updated: Jun 22, 2026

A Liposome Membrane Permeability Assay for Investigating the Effects of Phosphatidylinositol Phosphate Groups on Membranotropic Action of Venom PLA2
10:31

A Liposome Membrane Permeability Assay for Investigating the Effects of Phosphatidylinositol Phosphate Groups on Membranotropic Action of Venom PLA2

Published on: September 26, 2025

Defining Substrate Specificities for Lipase and Phospholipase Candidates
08:59

Defining Substrate Specificities for Lipase and Phospholipase Candidates

Published on: November 23, 2016

Area of Science:

  • Cardiovascular Research
  • Inflammation and Immunology
  • Pharmacology

Background:

  • Atherosclerosis is increasingly recognized as a complex disease involving both lipid accumulation and inflammatory processes.
  • Secreted phospholipase A2 (sPLA2) and lipoprotein-associated phospholipase A2 (Lp-PLA2) play significant roles in atherogenesis and its complications.
  • These enzymes generate bioactive metabolites that influence multiple stages of atherosclerotic development.

Purpose of the Study:

  • To review novel treatment strategies for atherosclerosis targeting both lipid and inflammatory pathways.
  • To investigate the role of sPLA2 and Lp-PLA2 in atherosclerosis.
  • To evaluate the therapeutic potential of inhibiting sPLA2 and Lp-PLA2 in cardiovascular disease.

Main Methods:

  • Review of animal, pathological, and epidemiological studies.
  • Analysis of the association between phospholipase levels and cardiovascular events.
  • Examination of pharmacological inhibitors targeting sPLA2 and Lp-PLA2.

Main Results:

  • Elevated levels of sPLA2 and Lp-PLA2 correlate with complex coronary lesions and major adverse cardiovascular events.
  • Inhibition of these enzymes is a key research focus.
  • Pharmacological agents like darapladib and varespladib are emerging as potential treatments.

Conclusions:

  • sPLA2 and Lp-PLA2 are implicated in atherosclerosis progression and clinical outcomes.
  • Inhibiting these enzymes represents a promising therapeutic avenue for coronary artery disease.
  • Further clinical trials are necessary to confirm the efficacy of novel inhibitors.