Target intelligence / Profile preview

Human serum albumin (subdomain IIIA) (HSA-IIIA)

Target
HSA-IIIA
Molecular classification
Transport protein, Plasma protein, Carrier protein
01

Overview

Human serum albumin (HSA) is the most abundant protein in human plasma, and its subdomain IIIA, also known as Sudlow's Site II, is a principal binding site for various ligands (UniProt P02768). This subdomain contains a hydrophobic pocket that preferentially binds small, aromatic carboxylic acids and neutral drugs such as ibuprofen and diazepam (Ghuman et al., 2005, PMID: 16039571). Its primary biological function involves the transport and distribution of endogenous substances like fatty acids and exogenous pharmaceuticals, thereby modulating their pharmacokinetics (Fanali et al., 2012, PMID: 22235837). In clinical practice, subdomain IIIA is a critical site for drug-drug interactions, as competition for binding can increase the free fraction of drugs, potentially leading to toxicity (Sudlow et al., 1976, PMID: 1252658).

Other names
Sudlow's Site IIAlbumin Subdomain IIIAHSA Site IIDomain III of Human Serum Albumin
02

Mechanism of action

Reversible non-covalent binding of small molecules to a hydrophobic pocket, facilitating systemic transport and modulating the free fraction of drugs in plasma.

03

Biological functions

Ligand transportMaintenance of oncotic pressureFatty acid bindingDrug distribution
04

Disease associations

HypoalbuminemiaLiver cirrhosisNephrotic syndromeDrug-drug interactions
05

Safety considerations

Competitive displacement leading to drug toxicityAltered binding capacity in uremia or liver failureHypoalbuminemia-induced changes in drug clearance
06

Interacting drugs

Ibuprofen

6 more in the full profile.

07

Biomarkers

Serum albumin concentrationAlbumin-to-globulin ratio

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