What is the Origin of Suicide Inhibitor?

The term originated in the field of pharmacology and medicinal chemistry in the mid-20th century, describing the unique and self-destructive action of the drug against its target. The name reflects the fact that the enzyme essentially catalyzes its own irreversible inhibition, akin to a biological self-destruct mechanism. This concept is fundamental to the development of several hormonal and metabolic therapeutic agents, including certain aromatase inhibitors.

What is the Mechanism of Suicide Inhibitor?

The process begins with the inhibitor binding to the enzyme like a normal substrate, fitting into the active site. The enzyme attempts its typical catalytic reaction on the molecule, but instead of completing the turnover, the resulting intermediate chemically traps the enzyme. This irreversible covalent binding permanently blocks the active site, rendering the enzyme non-functional and requiring the cell to synthesize new enzyme molecules to restore activity.

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Suicide Inhibitor

Meaning

A Suicide Inhibitor, also formally known as a mechanism-based inhibitor, is a type of pharmaceutical agent that is metabolically inert until it binds to its specific target enzyme, where it is then chemically activated by the enzyme’s catalytic action. This unique modification converts the inhibitor into a highly reactive molecule that forms a permanent, irreversible covalent bond with the active site of the enzyme. This binding permanently inactivates the enzyme, which is a key strategy in rational drug design to achieve sustained therapeutic effect.