Enzymes and Transporters

Enzymes and Transporters represent broad functional categories of proteins rather than a single molecular target. Enzymes are biological catalysts that facilitate nearly all chemical reactions in the body, including metabolism, DNA replication, and signal transduction (Nature Reviews Drug Discovery, 2002). Transporters are membrane-bound proteins that control the movement of ions, nutrients, and drugs across cellular boundaries, playing a vital role in maintaining cellular homeostasis and determining pharmacokinetics (Nature Reviews Drug Discovery, 2010). While many specific enzymes (e.g., cyclooxygenase) and transporters (e.g., serotonin transporter) are major therapeutic targets, the collective term is too broad for specific drug development. Therapeutic intervention typically involves small molecule inhibitors or activators designed to modulate specific pathways (IUPHAR/BPS Guide to Pharmacology, 2024). Due to their ubiquitous nature and diverse roles, targeting these proteins requires high selectivity to avoid systemic toxicity and complex drug-drug interactions.

Other names

EnzymesTransportersBiocatalystsMembrane transport proteinsDrug-metabolizing enzymes and transporters

Enzymes are typically targeted via competitive, non-competitive, or irreversible inhibition to block specific biochemical pathways, while transporters are targeted to modulate the influx or efflux of ions and molecules across biological membranes (IUPHAR/BPS Guide to Pharmacology, 2024).