Target intelligence / Profile preview

Anionic serum and extracellular proteins (ASEP)

Target
ASEP
Molecular classification
Other, Serum proteins, Extracellular matrix proteins
01

Overview

Anionic serum and extracellular proteins represent a broad class of negatively charged molecules, including human serum albumin and various components of the extracellular matrix, that play a critical role in the pharmacokinetics of cationic drugs. At physiological pH, these proteins carry a net negative charge, allowing them to interact electrostatically with polycationic compounds such as aminoglycoside antibiotics. This interaction is a primary determinant of the volume of distribution and the tissue-specific accumulation of these drugs, particularly in the kidneys and inner ear. While not a traditional signaling receptor, this 'target' group acts as a significant physiological sink and a mediator of drug-induced toxicities. In clinical practice, the binding of drugs to these proteins can influence both the therapeutic efficacy and the safety profile, as seen in the competitive binding and subsequent endocytosis that leads to aminoglycoside-induced nephrotoxicity.

Other names
Anionic serum proteinsExtracellular anionic sitesSerum albumin and anionic globulinsAnionic extracellular matrix components
02

Mechanism of action

Drugs, particularly polycationic aminoglycosides, bind electrostatically to these anionic proteins, which can lead to sequestration in the extracellular space or facilitate uptake into specific tissues like the renal proximal tubules via endocytosis.

03

Biological functions

Osmotic pressure regulationLigand transportBufferingMolecular sequestrationCell adhesion
04

Disease associations

InfectionDrug toxicityEdemaProteinuria
05

Safety considerations

NephrotoxicityOtotoxicityReduced drug bioavailability due to non-specific bindingDisplacement of endogenous ligands
06

Interacting drugs

Gentamicin

5 more in the full profile.

07

Biomarkers

Serum albumin levelsTotal serum proteinUrinary protein excretion

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