Enzymetargeted

Enzymetargeted refers to strategies that specifically exploit or modulate enzymatic activity to achieve selective biological effects. In this context, targeting may involve inhibiting disease‑associated enzymes, activating prodrugs or imaging agents with enzyme action, or delivering therapeutics in response to local enzyme activity. The concept overlaps with enzyme-responsive drug delivery, prodrug design, and targeted therapy.

Common approaches include selective enzyme inhibition by small molecules or biologics; enzyme-activated prodrugs that are converted into active drugs by disease-associated enzymes; and enzyme-responsive delivery systems in which drug release is triggered by enzymatic cleavage. Some strategies use ligands that bind particular enzymes to guide payloads to specific tissues.

In cancer, enzymes such as matrix metalloproteinases and cathepsins are frequently overexpressed and exploited to activate prodrugs or to modulate the tumor microenvironment. Beta-glucuronidase in tumor tissues has been used to activate glucuronide prodrugs or imaging agents, enhancing tumor selectivity.

Challenges include achieving true selectivity given enzyme expression heterogeneity, avoiding off‑target activation, optimizing pharmacokinetics, and managing possible resistance or immunogenicity. The field spans pharmacology, medicinal chemistry, and bioengineering, with ongoing research into safer, more effective enzyme-targeted therapies.

Related topics include targeted therapy, prodrug design, enzyme-responsive materials, and biomarker-based diagnostics.