Bioluminescence is the biologically active luminescence light producing event encountered in nature. In recent years several new screening methods utilizing bioluminescent cell-based biosensors have been designed demonstrating their utility towards dynamic monitoring of a variety of cellular functions. Because luciferase is unnatural to mammalian physiology, assays utilizing specific substrates to yield a luminescent signal are attractive and serve the purpose with high sensitivity and specificity. Often genetic or chemical modifications in different luciferase-substrate system in use have afforded new functionalities making these assays even more robust. Finally, in the evolving paradigm of molecular imaging, in vivo bioluminescence imaging (BLI) has evolved as a very attractive tool for interrogating human cellular biology in rodent models. In this short review we explore various bioluminescence screening strategies developed and analyze their scope in future drug screening processes.
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