Target intelligence / Profile preview

Plasma membrane phospholipid bilayer

Molecular classification
Other
01

Overview

The plasma membrane phospholipid bilayer is a fundamental biological structure composed of two layers of amphipathic phospholipids that forms the primary barrier between the interior of a cell and the external environment. It serves as a matrix for membrane proteins and is critical for maintaining cellular integrity, regulating the transport of ions and molecules, and facilitating signal transduction through various receptors and lipid rafts (StatPearls, 2023). In pharmacology, the bilayer is a significant therapeutic target, particularly for antimicrobial and antifungal agents that exploit differences in lipid composition—such as the presence of ergosterol in fungi or specific anionic lipids in bacteria—to induce membrane leakage and cell death (Nature Reviews Microbiology, 2017). Beyond direct disruption, the physical properties of the bilayer, such as fluidity and thickness, can be modulated by general anesthetics and certain lipophilic drugs to alter the function of embedded proteins. However, targeting the bilayer presents significant safety challenges, as many agents can cause off-target damage to human host cell membranes, leading to side effects like nephrotoxicity or hemolysis (Journal of Biological Chemistry, 2020).

Other names
Cell membraneCytoplasmic membraneLipid bilayerPlasmalemma
02

Mechanism of action

Membrane permeabilization, pore formation, sequestration of essential lipids, alteration of membrane fluidity, and disruption of electrochemical gradients.

03

Biological functions

Barrier functionCell compartmentalizationSignal transductionIon homeostasisEndocytosisExocytosisMolecular transport
04

Disease associations

InfectionCancerNeurodegenerative diseaseCardiovascular diseaseInflammation
05

Safety considerations

Low therapeutic index due to lack of specificity between pathogen and host membranesHemolysisNephrotoxicityNeurotoxicitySystemic toxicity
06

Interacting drugs

Daptomycin

8 more in the full profile.

07

Biomarkers

Phosphatidylserine exposureLipid peroxidation levelsMembrane fluidity indexCirculating oxysterols

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