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Design, synthesis, and biophysical and biological evaluation of a series of pyrrolobenzodiazepine-poly(N-methylpyrrole) conjugates.
A novel series of methyl ester-terminated C8-linked pyrrolobenzodiazepine (PBD)-poly(N-methylpyrrole) conjugates (50a-f) has been synthesized and their DNA interaction evaluated by thermal
SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug that cross-links DNA and exerts highly potent antitumor activity.
TLDR
SG2285 is defined as a highly active cytotoxic compound with antitumor properties desirable for further development and shown in several human tumor xenograft models, including ovarian, non-small cell lung, prostate, pancreatic, and melanoma, with cures obtained in the latter model with a single dose.
DNase I footprinting of small molecule binding sites on DNA.
TLDR
The method is described and technical details are given for performing deoxyribonuclease (DNase) I footprinting with DNA-binding drugs for probing sequence-selective binding of small molecules to DNA.
A 96-well DNase I footprinting screen for drug–DNA interactions
TLDR
The dramatic increase in throughput, quantified data and decreased handling time allow, for the first time, DNase I footprinting to be used as a screening tool to assess DNA-binding agents.
Preferential binding to DNA sequences of peptides related to a novel XPRK motif.
Unusually Strong Positive Cooperativity in Binding of Peptides to Latent Membrane Protein‐1 DNA Fragments of the Epstein–Barr Viral Gene
TLDR
The evidence of sequence selectivity and strong cooperativity discovered in this work may prove to be a general feature of peptide interactions with some nucleic acids.
SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug with potent antitumor activity
TLDR
A modification of the single cell gel electrophoresis (comet) assay has shown SG2285 to be highly efficient at producing ICLs in cells, which form more slowly than those produced by SG2202.
Articles Sequence-Selective Interaction of the Minor-Groove Interstrand Cross-Linking Agent SJG-136 with Naked and Cellular DNA: Footprinting and Enzyme Inhibition
TLDR
Footprinting studies have confirmed that high-affinity adducts do form at 5'-G-GATC-C-3' sequences and that these can inhibit RNA polymerase in a sequence-selective manner, and SJG-136 efficiently inhibits the action of restriction endonuclease BglII.
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