Peptide Antagonism describes a molecular interaction where one peptide molecule competitively or non-competitively blocks the biological activity of another, typically endogenous, signaling peptide at its specific receptor site. In clinical practice, this is relevant when managing conditions driven by overactive hormonal axes or excessive signaling, such as blocking an excess growth hormone effect. It is the deliberate neutralization of a specific signal.
Origin
This concept stems directly from receptor pharmacology, where the definition of an antagonist is a substance that binds to a receptor without activating it, thereby preventing the natural agonist peptide from exerting its effect. The ‘peptide’ specification narrows the focus to these biomolecules.
Mechanism
The mechanism involves the antagonist peptide possessing sufficient structural homology to the natural ligand to occupy the receptor binding pocket but lacking the necessary conformational change required to initiate the downstream intracellular signaling cascade. This competitive binding effectively lowers the functional concentration of the active endogenous peptide signal available to the cell.
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