Format

Send to

Choose Destination
See comment in PubMed Commons below
Chem Biol. 2010 Jun 25;17(6):646-57. doi: 10.1016/j.chembiol.2010.05.012.

Illuminating insights into firefly luciferase and other bioluminescent reporters used in chemical biology.

Author information

1
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892-3370, USA.

Abstract

Understanding luciferase enzymology and the structure of compounds that modulate luciferase activity can be used to improve the design of luminescence-based assays. This review provides an overview of these popular reporters with an emphasis on the commonly used firefly luciferase from Photinus pyralis (FLuc). Large-scale chemical profile studies have identified a variety of scaffolds that inhibit FLuc. In some cell-based assays, these inhibitors can act in a counterintuitive way, leading to a gain in luminescent signal. Although formerly attributed to transcriptional activation, intracellular stabilization of FLuc is the primary mechanism underlying this observation. FLuc inhibition and stabilization can be complex, as illustrated by the compound PTC124, which is converted by FLuc in the presence of ATP to a high affinity multisubstrate adduct inhibitor, PTC124-AMP. The potential influence these findings can have on drug discovery efforts is provided here.

PMID:
20609414
PMCID:
PMC2925662
DOI:
10.1016/j.chembiol.2010.05.012
[Indexed for MEDLINE]
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science Icon for PubMed Central
    Loading ...
    Support Center