Sequence-selective binding of C8-conjugated pyrrolobenzodiazepines (PBDs) to DNA.
Biophys Chem
; 230: 53-61, 2017 11.
Article
em En
| MEDLINE
| ID: mdl-28941814
ABSTRACT
DNA footprinting and melting experiments have been used to examine the sequence-specific binding of C8-conjugates of pyrrolobenzodiazepines (PBDs) and benzofused rings including benzothiophene and benzofuran, which are attached using pyrrole- or imidazole-containing linkers. The conjugates modulate the covalent attachment points of the PBDs, so that they bind best to guanines flanked by A/T-rich sequences on either the 5'- or 3'-side. The linker affects the binding, and pyrrole produces larger changes than imidazole. Melting studies with 14-mer oligonucleotide duplexes confirm covalent attachment of the conjugates, which show a different selectivity to anthramycin and reveal that more than one ligand molecule can bind to each duplex.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Benzodiazepinas
/
DNA
Idioma:
En
Revista:
Biophys Chem
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
Reino Unido