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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. SimpleExpand
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 smallExpand
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 biology. Cell-permeable small molecules thatExpand
Solid phase synthesis of polyamides containing imidazole and pyrrole amino acids
The solid phase synthesis of sequence specific DNA binding polyamides containing N-methylimidazole (Im) and N-methylpyrrole (Py) amino acids is described. Two monomer building blocks, Boc-Py-OBtExpand
A structural basis for recognition of A.T and T.A base pairs in the minor groove of B-DNA.
Polyamide dimers containing three types of aromatic rings-pyrrole, imidazole, and hydroxypyrrole-afford a small-molecule recognition code that discriminates among all four Watson-Crick base pairs inExpand
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 highExpand
Inhibition of Ets-1 DNA Binding and Ternary Complex Formation between Ets-1, NF-κB, and DNA by a Designed DNA-binding Ligand*
Sequence-specific pyrrole-imidazole polyamides can be designed to interfere with transcription factor binding and to regulate gene expression, both in vitro and in living cells. Polyamides boundExpand
Inhibition of RNA polymerase II transcription in human cells by synthetic DNA-binding ligands.
Sequence-specific DNA-binding small molecules that can permeate human cells potentially could regulate transcription of specific genes. Multiple cellular DNA-binding transcription factors areExpand
Aliphatic/aromatic amino acid pairings for polyamide recognition in the minor groove of DNA
Selective placement of an aliphatic β-alanine (β) residue paired side-by-side with either a pyrrole (Py) or imidazole (Im) aromatic amino acid is found to compensate for sequence composition effectsExpand
Fmoc solid phase synthesis of polyamides containing pyrrole and imidazole amino acids.
[structure: see text]. Polyamides containing N-methylimidazole (Im) and N-methylpyrrole (Py) amino acids are synthetic ligands that have an affinity and specificity for DNA comparable to those ofExpand
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