Based on -cyclobutylaminoluciferin (cybLuc), a set of high and efficient caged bioluminescent derivatives (Clucs) as firefly luciferase pro-substrates has been developed herein. After careful examination, these molecules exhibited low cytotoxicity and prolonged bioluminescence imaging up to 6 h and . Importantly, these caged luciferin derivatives have the potential to serve as long-term tracking tools to explore some biological process by using bioluminescent imaging.
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http://dx.doi.org/10.1039/c8ra02312c | DOI Listing |
ACS Chem Biol
December 2024
Department of Molecular Physiology and Biological Physics, University of Virginia School of Medicine, Charlottesville, Virginia 22908, United States.
Bioluminescence imaging (BLI) is a powerful, noninvasive imaging method for animal studies. NanoLuc luciferase and its derivatives are attractive bioluminescent reporters recognized for their efficient photon production and ATP independence. However, utilizing them for animal imaging poses notable challenges.
View Article and Find Full Text PDFExpert Opin Drug Metab Toxicol
November 2024
Research and Development Department, Promega Corporation, Madison, WI, USA.
Background: Adverse drug-drug interactions (DDI) may occur when one drug accelerates or slows a second drug's metabolism by, respectively, inducing or inhibiting a cytochrome P450 (CYP) that metabolizes that second drug. We developed an method employing urinalysis to complement CYP induction and inhibition measurements widely used to predict DDIs.
Research Design And Methods: Focusing on Cyp3a enzymes, the major mammalian drug metabolizers, we applied luciferin-IPA, a selective Cyp3a probe substrate to mice after Cyp3a inducers and inhibitor treatments.
NanoLuc luciferase and its derivatives are attractive bioluminescent reporters recognized for their efficient photon production and ATP independence. However, utilizing them for imaging poses notable challenges. Low substrate solubility has been a prominent problem, limiting brightness, while substrate instability hampers consistent results and handling.
View Article and Find Full Text PDFJ Photochem Photobiol B
April 2024
University of Zagreb School of Medicine, BIMIS - Biomedical Research Center Šalata, and Croatian Institute for Brain Research, Zagreb, Croatia. Electronic address:
Programmed cell death or apoptosis is a critically important mechanism of tissue remodeling and regulates conditions such as cancer, neurodegeneration or stroke. The aim of this research article was to assess the caged Z-DEVD-aminoluciferin substrate for in vivo monitoring of apoptosis after ischemic stroke in TLR2-deficient mice and their TLR2-expressing counterparts. Postischemic inflammation is a significant contributor to ischemic injury development and apoptosis, and it is modified by the TLR2 receptor.
View Article and Find Full Text PDFChemistry
January 2024
Institute for Molecules and Materials, Radboud University, 6525 AJ, Nijmegen, The Netherlands.
Measuring glycosidase activity is important to monitor any aberrations in carbohydrate hydrolase activity, but also for the screening of potential glycosidase inhibitors. To this end, synthetic substrates are needed which provide an enzyme-dependent read-out upon hydrolysis by the glycosidase. Herein, we present two new routes for the synthesis of caged luminescent carbohydrates, which can be used for determining glycosidase activity with a luminescent reporter molecule.
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