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Receptor Blocking

Meaning

Receptor Blocking is a pharmacological strategy involving the use of a drug, known as an antagonist, to bind to a specific cellular receptor site without activating it, thereby preventing the binding and action of the receptor’s natural ligand or an agonist drug. This mechanism is therapeutically employed to inhibit or modulate an excessive or undesirable hormonal signal, such as blocking androgen receptors to treat prostate cancer or blocking estrogen receptors to treat breast cancer. The efficacy of the block is determined by the antagonist’s affinity and concentration.