Journal article
A Comparison of DNA-Binding Drugs as Inhibitors of E2F1− and Sp1−DNA Complexes and Associated Gene Expression
Biochemistry (Easton), v 37(9), pp 3109-3115
03 Mar 1998
PMID: 9485464
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
In this study, we examined how DNA-binding drugs prevented formation of transcription factor−DNA complexes and influenced gene transcription from the hamster dihydrofolate reductase promoter, which is regulated by E2F1 and Sp1. Gel mobility shift assay data showed that GC-binding drugs (e.g., mitoxantrone) inhibited the DNA binding of both E2F1 and Sp1. In contrast, AT-binding drugs (e.g., distamycin) interfered only with E2F1−DNA complex formation. In an in vitro transcription assay using HeLa nuclear extracts, inhibition of transcription was observed when mitoxantrone or distamycin was added either before or after assembly of the transcription complex on the DNA, although for the latter, higher drug concentrations were needed. Mitoxantrone, which was a stronger inhibitor of transcription factor−DNA complex, was more effective than distamycin at preventing transcript formation. Time course transcription in a cell-free assay with addition of various drug concentrations indicated that high drug concentrations of either mitoxantrone or distamycin completely blocked transcription, while low drug concentrations could delay the synthesis of transcripts.
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Details
- Title
- A Comparison of DNA-Binding Drugs as Inhibitors of E2F1− and Sp1−DNA Complexes and Associated Gene Expression
- Creators
- Shu-Yuan ChiangJane Clifford AzizkhanTerry A Beerman
- Publication Details
- Biochemistry (Easton), v 37(9), pp 3109-3115
- Publisher
- American Chemical Society; Washington, DC
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Biochemistry and Molecular Biology
- Web of Science ID
- WOS:000072523600044
- Scopus ID
- 2-s2.0-0032478124
- Other Identifier
- 991014877880104721
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- Web of Science research areas
- Biochemistry & Molecular Biology