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Related Concept Videos

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...
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...
Amplifying Signals via Enzymatic Cascade01:22

Amplifying Signals via Enzymatic Cascade

When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze the...
Amplifying Signals via Second Messengers01:15

Amplifying Signals via Second Messengers

Many receptor binding ligands are hydrophilic; they do not cross the cell membrane but bind to cell-surface receptors. Thus, their message must be relayed by second messengers present in the cell cytoplasm. There are several second messenger pathways, each with its own way of relaying information. For example, the G protein-coupled receptors can activate both phosphoinositol and cyclic AMP (cAMP) second messenger pathways. The phosphoinositol pathway is active when the receptor induces...
What are Second Messengers?01:12

What are Second Messengers?

Because many receptor binding ligands are hydrophilic, they do not cross the cell membrane and thus their message must be relayed to a second messenger on the inside. There are several second messenger pathways, each with their own way of relaying information. G-protein coupled receptors can activate both phosphoinositol and cyclic AMP (cAMP) second messenger pathways. The phosphoinositol path is active when the receptor induces phospholipase C to hydrolyze the phospholipid,...
What are Second Messengers?01:12

What are Second Messengers?

Because many receptor binding ligands are hydrophilic, they do not cross the cell membrane and thus their message must be relayed to a second messenger on the inside. There are several second messenger pathways, each with their own way of relaying information. G-protein coupled receptors can activate both phosphoinositol and cyclic AMP (cAMP) second messenger pathways. The phosphoinositol path is active when the receptor induces phospholipase C to hydrolyze the phospholipid,...

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Related Experiment Video

Updated: Jun 28, 2026

A Liposome Membrane Permeability Assay for Investigating the Effects of Phosphatidylinositol Phosphate Groups on Membranotropic Action of Venom PLA2
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Published on: September 26, 2025

Phospholipase A2 structure/function, mechanism, and signaling.

John E Burke1, Edward A Dennis

  • 1Department of Chemistry, School of Medicine, University of California, San Diego, La Jolla, CA 92093-0601, USA.

Journal of Lipid Research
|November 18, 2008
PubMed
Summary

Phospholipase A2 (PLA2) enzymes, crucial for lipid signaling, have seen significant research advances. This review covers PLA2 structures, substrate interactions, and inhibitor development for therapeutic applications.

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Area of Science:

  • Biochemistry
  • Enzymology
  • Molecular Biology

Background:

  • The phospholipase A2 (PLA2) enzyme superfamily plays critical roles in cellular lipid metabolism and signaling pathways.
  • Recent decades have yielded substantial progress in elucidating the diverse structures and functions of PLA2 enzymes.

Purpose of the Study:

  • To review the current understanding of the structure and substrate interactions of major phospholipase A2 enzyme types.
  • To provide a brief overview of the development and therapeutic potential of PLA2 inhibitors in lipid signaling.

Main Methods:

  • Literature review of recent advancements in PLA2 research.
  • Analysis of structural and functional data for representative PLA2 enzymes.
  • Summary of inhibitor development strategies and their implications.

Main Results:

  • Detailed examination of four main PLA2 types: secreted sPLA2, cytosolic cPLA2, calcium-independent iPLA2, and LpPLA2.
  • Insights into the membrane-bound substrate interactions of these diverse PLA2 enzymes.
  • Overview of inhibitors targeting PLA2 enzymes for modulating lipid signaling.

Conclusions:

  • Significant progress has been made in understanding PLA2 enzyme superfamily structure and function.
  • PLA2 inhibitors hold promise for therapeutic interventions in various lipid-mediated diseases.