Ligand sequestration

Ligand sequestration is a biophysical and pharmacological process by which ligands (including drugs, signaling molecules, or endogenous compounds) are captured or restricted within biological compartments such as lipid bilayers, vesicles, or other cellular structures, reducing their apparent concentration available for target binding[5]. This process can significantly affect the pharmacodynamics and pharmacokinetics of drugs or endogenous molecules by lowering the observable binding affinity, especially in in vivo systems relative to purified preparations. It does not refer to a discrete protein, receptor, or therapeutic target but is crucial for interpreting binding experiments and drug efficacy under physiologically relevant or complex system conditions[5].

Other names

ligand entrapmentligand compartmentalizationligand partitioning

Reduction of free ligand/drug concentration by sequestration in lipid membranes or other cellular compartments[5]. Alteration of effective drug concentration by compartmentalization, impacting pharmacokinetics[5].