365d

Publication Abstract from PubMed

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 that can bind predetermined DNA sequences with affinities and specificities comparable to DNA binding proteins. Antiparallel side-by-side pairings of two aromatic amino acids, imidazole (Im) and pyrrole (Py), distinguish G.C from C.G, and both from A.T/T.A base pairs. A high resolution X-ray crystal structure of a four-ring pyrrole-imidazole polyamide specifically bound as a dimer to a six-base pair predetermined DNA site reveals a structural framework of hydrogen bonds and interactions with the walls of the minor groove that underlies the pairing rules for DNA recognition.

Structural basis for G.C recognition in the DNA minor groove.,Kielkopf CL, Baird EE, Dervan PB, Rees DC Nat Struct Biol. 1998 Feb;5(2):104-9. PMID:9461074^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.