title: A revisit of the mode of interaction of small transcription inhibitors with genomic DNA.
abstract: One class of small molecules with therapeutic potential for treatment of cancer functions as transcription inhibitors via interaction with double-stranded DNA. Majority of the studies of the interaction with DNA have so far been reported under conditions nonexistent in vivo. Inside the cell, DNA is present in the nucleus as a complex with proteins known as chromatin. For the last few years we have been studying the interaction of these DNA-binding small molecules at the chromatin level with emphasis on the drug-induced structural alterations in chromatin. Our studies have shown that at the chromatin level these molecules could be classified in two broad categories: single-binding and dual-binding molecules. Single-binding molecules access only DNA in the chromatin, while the dual-binding molecules could bind to both DNA and the associated histone(s). Structural effects of the DNA-binding molecules upon chromatin in light of the above broad categories and the associated biological implications of the two types of binding are discussed.
authors: Biophysics Division, Saha Institute of Nuclear Physics, Bidhan Nagar, Kolkata 700 064, India. dipak.dasgupta@saha.ac.in
authors: Dipak
authors: D
authors: Dasgupta
authors: Parijat
authors: P
authors: Majumder
authors: Amrita
authors: A
authors: Banerjee
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D002843:Chromatin / Q000737:chemistry; D004247:DNA / Q000737:chemistry*; D016678:Genome; D006801:Humans; D006860:Hydrogen Bonding; D007364:Intercalating Agents / Q000737:chemistry / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy; D009690:Nucleic Acid Conformation; D019384:Nucleic Acid Synthesis Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D014158:Transcription, Genetic / Q000187:drug effects*
chemical_list: D000970:Antineoplastic Agents; D002843:Chromatin; D007364:Intercalating Agents; D019384:Nucleic Acid Synthesis Inhibitors; D004247:DNA