Many systems used to discover drugs rely on cells genetically engineered to contain a firefly luciferase reporter gene to gauge the activity of chemical compounds. If the luciferase enzyme emits a bright signal in test readouts, it usually means a compound is active. In such systems, if the signal is dim or nonexistent, the compound usually is not active. In many luciferase-based systems (top illustration), cells produce a low background level of luciferase enzyme that breaks down over time, generating a dim signal in test readouts. NIH researchers have discovered a family of compounds that generate surprisingly bright signals in test readouts even when inactive (bottom illustration). In this situation, the compounds inhibit luciferase in a way that stabilizes the enzyme and slows its breakdown, producing a bright signal that can be mistaken for genuine activity
Share
