title: A novel minor groove binding reagent designed to serve as a "truck" to carry DNA modifying moieties into the major groove.
abstract: A site selective DNA minor groove binding tripyrrole peptide has been synthesized as a "truck" to place chemical functionalities into the major groove which are capable of physically modifying DNA, acting as catalysts to hydrolyze DNA, or effectively protecting DNA from various DNA modifying enzymes. The equilibrium dissociation constants for the binding of this peptide to an A3T3 dsDNA binding site have been determined to be nanomolar, and they are compared to the constants for other minor groove binding agents.
authors.affiliation: Department of Chemistry, University of California, Santa Barbara 93106, USA.
authors.forename: T
authors.initials: T
authors.lastname: Xue
authors.forename: K A
authors.initials: KA
authors.lastname: Browne
authors.forename: T C
authors.initials: TC
authors.lastname: Bruice
mesh_terms: D001483:Base Sequence; D004247:DNA / Q000737:chemistry*; D004268:DNA-Binding Proteins / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D004214:Distamycins / Q000493:pharmacokinetics; D007202:Indicators and Reagents / Q000737:chemistry*; D008969:Molecular Sequence Data; D009690:Nucleic Acid Conformation; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
chemical_list: D004268:DNA-Binding Proteins; D004214:Distamycins; D007202:Indicators and Reagents; C093047:N,N-dimethyl-3-(1-methyl-4-(1-(3-aminopropyl)-4-(1-methyl-4-acetamido-2-pyrrolecarboxamido)-2-pyrrolecarboxamido)-2-pyrrolecarboxamido)propylamine; D011758:Pyrroles; C030000:stallimycin; D004247:DNA