Target intelligence / Profile preview

Anionic phospholipid membrane

Molecular classification
Lipid, Cell membrane component
01

Overview

Anionic phospholipid membranes are biological bilayers containing a high proportion of negatively charged lipids, including phosphatidylserine (PS), phosphatidylglycerol, and cardiolipin. In healthy mammalian cells, PS is typically restricted to the inner leaflet of the plasma membrane, but it is externalized to the outer leaflet during apoptosis and in the tumor microenvironment, where it acts as an immunosuppressive signal and a marker for cell clearance (Birge et al., 2016). Bacterial membranes differ significantly from mammalian membranes by maintaining a high density of anionic lipids on their exterior, providing a basis for the selective action of cationic antibiotics like daptomycin and polymyxins (Humphries et al., 2013). Targeting these membranes allows for the development of therapies that distinguish between pathological and healthy states based on surface charge and lipid composition. Current research focuses on using these membranes as docking sites for targeted drug delivery and as targets for monoclonal antibodies in oncology and infectious diseases.

Other names
Negatively charged phospholipid membraneAcidic phospholipid membranePhosphatidylserine-exposed membraneAnionic lipid bilayer
02

Mechanism of action

Therapeutic agents target anionic phospholipid membranes through electrostatic attraction between cationic domains and negatively charged lipid headgroups, such as phosphatidylserine or phosphatidylglycerol (Yeung et al., 2008). This interaction can result in membrane depolarization, physical disruption (pore formation), or the induction of immune-mediated clearance like antibody-dependent cellular cytotoxicity (ADCC) (Birge et al., 2016).

03

Biological functions

Apoptosis signalingBlood coagulationMembrane recruitment of proteinsPhagocytosis inductionCell signaling
04

Disease associations

CancerBacterial infectionViral infectionAntiphospholipid syndromeInflammation
05

Safety considerations

Potential nephrotoxicityNon-specific membrane disruptionHemolytic activityOff-target binding to mitochondrial membranes
06

Interacting drugs

Bavituximab

6 more in the full profile.

07

Biomarkers

Annexin V bindingPhosphatidylserine externalizationAnti-phospholipid antibodies

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