This is the process of characterizing the binding strength, or affinity, of endogenous hormones and exogenous compounds to their cognate cellular receptors across various tissues under different physiological states. Accurate mapping is clinically vital because hormonal action depends not just on circulating levels but on the strength of the ligand-receptor interaction. It quantifies the actual signaling potential at the target site.
Origin
The concept is drawn from pharmacology and receptor biology, where ‘affinity’ quantifies the tightness of molecular binding. Mapping implies a systematic, often comparative, measurement across the endocrine system to determine functional receptor status.
Mechanism
Mapping is achieved using radioligand binding assays or competitive binding studies that measure the concentration of a hormone required to occupy 50% of the available receptors ($K_d$). Changes in receptor density or conformational structure, often induced by chronic hormone exposure or inflammation, directly alter this affinity. A low affinity suggests receptor downregulation, meaning higher circulating hormone concentrations are required to achieve a normal physiological effect.
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