HMG-CoA Reductase (HMGCR)

The rate-limiting enzyme of the mevalonate pathway that catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol biosynthesis. Statins competitively inhibit this enzyme, reducing hepatic cholesterol synthesis and upregulating LDL receptors to increase LDL clearance from blood. HMG-CoA reductase is one of the most commercially successful drug targets in history.

Ejemplos

• Atorvastatin (Lipitor) — most prescribed statin worldwide
• Rosuvastatin (Crestor) — highest potency statin
• Simvastatin — prodrug activated by hepatic hydrolysis