-
Article
Repression of the transcriptional activity of ERRα with sequence-specific DNA-binding polyamides
The orphan nuclear receptors estrogen-related receptors (ERRs) bind to the estrogen-related receptor response element (ERRE) to regulate transcriptional programs in cellular metabolism and cancer cell growth. ...
-
Article
Structural basis for the initiation of eukaryotic transcription-coupled DNA repair
Cryo-electron microscopy analysis of yeast Rad26 bound to RNA polymerase II provides insight into the initiation of the transcription-coupled DNA repair mechanism in eukaryotes.
-
Article
Open AccessSingle-dose pharmacokinetic and toxicity analysis of pyrrole–imidazole polyamides in mice
Pyrrole–imidazole (Py-Im) polyamides are programmable, sequence-specific DNA minor groove–binding ligands. Previous work in cell culture has shown that various polyamides can be used to modulate the transcript...
-
Chapter
Regulation of Gene Expression by Synthetic DNA-Binding Ligands
During the past 20 years, polyamides have evolved from the natural product distamycin to a new class of programmable heterocyclic oligomers that bind a broad repertoire of DNA sequences with high affinity and ...
-
Article
Structural basis for G•C recognition in the DNA minor groove
Small molecules that target specific DNA sequences offer a potentially general approach for the regulation of gene expression. Pyrrole–imidazole polyamides represent the only class of synthetic small molecules...
-
Article
Recognition of the four Watson–Crick base pairs in the DNA minor groove by synthetic ligands
The design of synthetic ligands that read the information stored in the DNA double helix has been a long-standing goal at the interface of chemistry and biology1,2,3,4,5. Cell-permeable small molecules that targe...
-
Article
Regulation of gene expression by small molecules
Small molecules that target specific DNA sequences have the potential to control gene expression. Ligands designed for therapeutic application must bind any predetermined DNA sequence with high affinity and pe...
-
Article
Recognition of DNA by designed ligands at subnanomolar concentrations
SMALL molecules that specifically bind with high affinity to any predetermined DNA sequence in the human genome would be useful tools in molecular biology and potentially in human medicine. Simple rules have b...
-
Article
Extending the recognition site of designed minor groove binding molecules
A linked, imazole/pyrrole minor-groove ligand has been shown to bind sequence specif icially to a 13 base-pair target sequence in a mixed 1:1/2:1 mode.
-
Article
Reagents for the site-specific cleavage of megabase DNA
The physical map** of chromosomes will be facilitated by methods of breaking large DNA into manageable fragments, or cutting uniquely at genetic markers of interest. Key issues in the design of sequence-spec...
-
Article
Single-site enzymatic cleavage of yeast genomic DNA mediated by triple helix formation
PHYSICAL map** of chromosomes would be facilitated by methods of breaking large DNA into manageable fragments, or cutting uniquely at genetic markers of interest. Key issues in the design of sequence-specific D...
-
Chapter
Oligonucleotide Recognition of Double-helical DNA by Triple-helix Formation
The sequence-specific recognition of double-helical DNA is an essential biological process responsible for the regulation of cellular functions including transcription, replication and cell division. The abili...
