ArticleBMC molecular biology2003
The p53-inhibitor pifithrin-alpha inhibits firefly luciferase activity in vivo and in vitro.
Article in BMC molecular biology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 55 citations in OpenAlex.
- TGF-β inhibitor SB431542 suppresses SARS-CoV-2 replication through multistep inhibition.Journal of virology · 2025Article
- The small-molecule pifithrin-α deactivates ETR1 to repress shade avoidance inScience advances · 2025Article
- SLC35F2-SYVN1-TRIM59 axis critically regulates ferroptosis of pancreatic cancer cells by inhibiting endogenous p53.Oncogene · 2023Article
- TAF1A and ZBTB41 serve as novel key genes in cervical cancer identified by integrated approaches.Cancer gene therapy · 2021Article
- Examining multiple cellular pathways at once using multiplex hextuple luciferase assaying.Nature communications · 2019Article
- p53 upregulated by HIF-1α promotes hypoxia-induced G2/M arrest and renal fibrosis in vitro and in vivo.Journal of molecular cell biology · 2019Article
- Tannic acid-stabilized gold nano-particles are superior to native tannic acid in inducing ROS-dependent mitochondrial apoptosis in colorectal carcinoma cellsRSC advances · 2019Article
- Reversible LSD1 inhibition with HCI-2509 induces the p53 gene expression signature and disrupts the MYCN signature in high-risk neuroblastoma cells.Oncotarget · 2018Article
- TP53 Modulates Oxidative Stress in Gata1Stem cell reports · 2017Article
- Cezanne (OTUD7B) regulates HIF-1α homeostasis in a proteasome-independent manner.EMBO reports · 2014Article
- A nanobody modulates the p53 transcriptional program without perturbing its functional architecture.Nucleic acids research · 2014Article
- MicroRNA-21 silencing enhances the cytotoxic effect of the antiangiogenic drug sunitinib in glioblastoma.Human molecular genetics · 2013Article
- The nuclear factor κB inhibitor (E)-2-fluoro-4'-methoxystilbene inhibits firefly luciferase.Bioscience reports · 2012Article
- Firefly luciferase: an adenylate-forming enzyme for multicatalytic functions.Cellular and molecular life sciences : CMLS · 2010Review
- The cAMP-dependent protein kinase inhibitor H-89 attenuates the bioluminescence signal produced by Renilla Luciferase.PloS one · 2009Article
- Androgen receptor activity is inhibited in response to genotoxic agents in a p53-independent manner.Oncogene · 2006Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
backgroundPifithrin-alpha is a small molecule inhibitor of p53 transcriptional activity. It has been proposed that the use of pifithrin-alpha in conjunction with chemotherapeutic and radiation therapies for cancer will reduce the side effects of these treatments in normal tissue that still contains wild type p53. In addition, pifithrin-alpha provides a useful tool in the laboratory to investigate the function of p53 in model systems.
resultsWhile investigating the effects of pifithrin-alpha on the transcriptional activity of NF-kappaB, we observed a strong inhibition of reporter plasmids containing the firefly luciferase gene. Firefly luciferase is one of the most commonly used enzymes in reporter gene assays. In contrast, no inhibition of reporter plasmids containing Renilla luciferase or chloramphenicol acetyltransferase was observed. The inhibition of firefly luciferase activity by pifithrin-alpha was observed both in vivo and in vitro. Pifithrin-alpha did not inhibit firefly luciferase protein expression, but rather suppressed light production/emission, since addition of exogenous pifithrin-alpha to active extracts inhibited this activity. Furthermore, pifithrin-alpha also inhibited recombinant firefly luciferase protein activity.
conclusionsAmong its other biological activities, pifithrin-alpha is an inhibitor of firefly luciferase activity. Caution must therefore be taken when using this compound, which has been characterised as an inhibitor of p53 transcriptional activity, to investigate effects on gene expression using transiently transfected reporter plasmids. Furthermore, these results demonstrate that when using novel compounds, the choice of vectors used in the experimental procedures might be of great importance for the correct conclusions to be made.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.